Dapagliflozin (BMS-512148)

Catalog No.S1548

For research use only.

Dapagliflozin (BMS-512148) is a potent and selective hSGLT2 inhibitor with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4.

Dapagliflozin (BMS-512148) Chemical Structure

CAS No. 461432-26-8

Selleck's Dapagliflozin (BMS-512148) has been cited by 26 publications

Purity & Quality Control

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Biological Activity

Description Dapagliflozin (BMS-512148) is a potent and selective hSGLT2 inhibitor with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4.
Features More potent stimulator of glucosuria than other SGLT2 inhibitors.
Targets
hSGLT2 [1]
(CHO cells)
1.1 nM(EC50)
In vitro

Dapagliflozin is not sensitive to hSGLT1 with a 1200-fold IC50. [1] Dapagliflozin is 32-fold more potent than phlorizin against hSGLT2 but 4-fold less than phlorizin against hSGLT1. Dapagliflozin is highly selective versus GLUT transporters and displays 8–9% inhibition in protein-free buffer at 20 μM and virtually no inhibition in the presence of 4% bovine serum albumin. [2] Dapagliflozin has good permeability across Caco-2 cell membranes and is a substrate for P-glycoprotein (P-gp) but not a significant P-gp inhibitor. Dapagliflozin is stable in rat, dog, monkey, and human serum at 10 μM. Dapagliflozin shows no inhibitory responses or induction to human P450 enzymes. The in vitro metabolic pathways Dapagliflozin are glucuronidation, hydroxylation, and O-deethylation. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO cells M2r4ZmZ2dmO2aX;uJIF{e2G7 MnXnNkBp NF\ZSZRKdmirYnn0bY9vKG:oIHj1cYFvKFOJTGSyJIV5eHKnc4Pl[EBqdiCFSF:gZ4VtdHNiYYPz[ZN{\WRiYYOgX|E1S12jbIDoZU1u\XSqeXytSE1odHWlb4D5doFvd3OrZHWgeZB1[WunIHHmeIVzKDJiaILzJIJ6KGyrcYXp[EB{[2mwdHnscIF1cW:wIHPveY51cW6pLDDJR|UxRTBwMECwOFkh|ryP NWDwc3RDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC0N|Q6ODlpPkKwOFM1QTB7PD;hQi=>
CHOK1 cells NWHtR2pVTnWwY4Tpc44h[XO|YYm= MonFN{Bp Mn;jTY5pcWKrdHnvckBw\iCqdX3hckBUT0yWMjDlfJBz\XO|ZXSgbY4hS0iRS{GgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCdMUTDYU1CVUdidYD0ZYtmKGGodHXyJFMhcHK|IHL5JI1q[3KxYnX0ZUB{[2mwdHnscIF1cW:wIHPveY51cW6pIHHuZYx6e2m|LDDJR|UxRTBwMECxJO69VQ>? M3O5Z|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OESyOlE5Lz5{NEi0NlYyQDxxYU6=
HEK293.ETN cells M4PDeGZ2dmO2aX;uJIF{e2G7 MUSxMlUhcA>? MVTJcohq[mm2aX;uJI9nKGi3bXHuJHNIVFR{IITyZY5{\mWldHXkJIlvKEiHS{K5N{5GXE5iY3XscJMh[XO|ZYPz[YQh[XNiQV3HJJVxfGGtZTDh[pRmeiBzLkWgbJJ{KGK7IIPjbY51cWyuYYTpc44h[2:3boTpcoctKEmFNUC9NE4xODZ5IN88US=> MnjpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6OU[zO|QoRjF7OEm2N|c1RC:jPh?=
COS-7 cells NIjTNlRHfW6ldHnvckBie3OjeR?= NHO3VlUzKGh? MmLNTY5pcWKrdHnvckBw\iCqdX3hckBUT0yWMTD0doFve2[nY4Tl[EBqdiCFT2OtO{Bk\WyuczDhd5Nme3OnZDDhd{BCVUdidYD0ZYtmKGGodHXyJFIhcHK|IHL5JJNkcW62aXzsZZRqd25iY3;1cpRqdmduIFnDOVA:OC56OTFOwG0> MkHCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6OU[zO|QoRjF7OEm2N|c1RC:jPh?=
CHO MWLGeY5kfGmxbjDhd5NigQ>? MoL1TY5pcWKrdHnvckBw\iCqdX3hckBUT0yWMjDlfJBz\XO|ZXSgbY4hS0iRIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhYzF2Q23BUWch[WOldX31cIF1cW:wLDDFR|UxKD1iMD6wNFEyKM7:TT6= NH;0RXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEK2NFYyQCd-MUiyOlA3OTh:L3G+
CHO M3PSZ2Z2dmO2aX;uJIF{e2G7 NF3kdlVKdmirYnn0bY9vKG:oIILheEBUT0yWMjDlfJBz\XO|ZXSgbY4hS0iRIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhYzF2Q23BUWch[WOldX31cIF1cW:wLDDFR|UxKD1iMD6wNFMh|ryPLh?= MlrEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh{NkC2NVgoRjF6Mk[wOlE5RC:jPh?=
CHO MoHXSpVv[3Srb36gZZN{[Xl? MX;Jcohq[mm2aX;uJI9nKGi3bXHuJHNIVFRzIHX4dJJme3OnZDDpckBEUE9iY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBcOTSFXVHNS{Bi[2O3bYXsZZRqd25uIFXDOVAhRSBzLkO5JO69VS5? NYXHeFluRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiyOlA3OThpPkG4NlYxPjF6PD;hQi=>
HEK293.ETN NF3UNlJHfW6ldHnvckBie3OjeR?= M1PFbWlvcGmkaYTpc44hd2ZiaIXtZY4hW0eOVEKg[ZhxemW|c3XkJIlvKEiHS{K5N{5GXE5iY3XscJMh[XO|ZYPz[YQh[XNibXX0bJltNWGucHjhMWQuY1VvMUTDYYdtfWOxcInyZY5we2mmZTD1dJRic2ViYomgd4NqdnSrbHzheIlwdiClb4XueIlv\yxiSVO1NEA:KDBwMEC2O{DPxE1w NFPVeZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUewNFMyQCd-MUm3NFA{OTh:L3G+
COS7 M2T6N2Z2dmO2aX;uJIF{e2G7 Mnn5TY5pcWKrdHnvckBw\iCqdX3hckBUT0yWMTDlfJBz\XO|ZXSgbY4h[W[{aXPhckBoemWnbjDtc45s\XliQ1;TO{Bk\WyuczDhd5Nme3OnZDDhd{Bu\XSqeXytZYxxcGFvRD3bWU0yPEOfZ3z1Z49xgXKjbn;zbYRmKHWydHHr[UBjgSC|Y3nueIltdGG2aX;uJINwfW62aX7nMEBKSzVyIE2gNE45QDVizszNMi=> NXrP[YRxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm3NFA{OThpPkG5O|AxOzF6PD;hQi=>
HEK293 MXPGeY5kfGmxbjDhd5NigQ>? M{TTWmlvcGmkaYTpc44hd2ZiaIXtZY4hW0eOVEGg[ZhxemW|c3XkJIlvKEiHS{K5N{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIGuxOGNe[WyyaHGtcYV1cHmuZ3z1Z49xgXKjbn;zbYRmKHWydHHr[UwhUUN3MDC9JFAvQDFizszNMi=> NGnSfnA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUe4OVQ{PSd-MUm3PFU1OzV:L3G+
CHO MlHISpVv[3Srb36gZZN{[Xl? M2fFNVIhcHK| MU\Jcohq[mm2aX;uJI9nKGi3bXHuJHNIVFR{IHX4dJJme3OnZDDpckBEUE9iY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB{d2SrdX2t[IVx\W6mZX70JI1mfGi7bD3hcJBp[S2GLWvVMVE1S12pbIXjc5B6emGwb4Pp[IUhfXC2YXvlJIFnfGW{IEKgbJJ{NCCLQ{WwJF0hOC5yMEG0JO69VS5? NWrzd5VyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCxOFk3PTNpPkKwNVQ6PjV|PD;hQi=>
CHO M2X1ZmZ2dmO2aX;uJIF{e2G7 M2q4bVIhcHK| MVjJcohq[mm2aX;uJI9nKGi3bXHuJHNIVFRzIHX4dJJme3OnZDDpckBEUE9iY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB{d2SrdX2t[IVx\W6mZX70JI1mfGi7bD3hcJBp[S2GLWvVMVE1S12pbIXjc5B6emGwb4Pp[IUhfXC2YXvlJIFnfGW{IEKgbJJ{NCCLQ{WwJF0hOS5{IN88UU4> M{XRUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyMUS5OlU{Lz5{MEG0PVY2OzxxYU6=
CHO MoX2SpVv[3Srb36gZZN{[Xl? MV7Jcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KFOJTGSyJIV5eHKnc4Pl[EBqdiCFSF:gZ4VtdHNiYomgcIlyfWmmIIPjbY51cWyuYYTpc44h[2:3boTpcoctKEmFNUCgQUAxNjByMES5JO69VS5? NIj4UHY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEG4NVQ5Pid-MkCxPFE1QDZ:L3G+
HEK293 NG[0fmZHfW6ldHnvckBie3OjeR?= NGrQbnUyNjViaILz MX\Jcohq[mm2aX;uJI9nKGi3bXHuJHNIVFR{IHX4dJJme3OnZDDpckBJTUt{OUOgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCdMUTDYYFteGijLX3leIh6dC2GLXfseYNweHm{YX7vd4ll\SC3cIThb4Uh[W[2ZYKgNU42KGi{czDifUBtcXG3aXSgd4NqdnSrbHzheIlwdiClb4XueIlv\yxiSVO1NEA:KDBwMEC2O{DPxE1w MoewQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB3N{[1O|goRjJyNUe2OVc5RC:jPh?=
COS7 M2XFZ2Z2dmO2aX;uJIF{e2G7 Mom0NkBpenN? NVXHOYFRUW6qaXLpeIlwdiCxZjDoeY1idiCVR1zUNUBmgHC{ZYPz[YQhcW5iYX\ybYNidiCpcnXlckBud26tZYmgR29UPyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJHsyPEOfYXzwbIEudWW2aInsMWQu\2y3Y3;wfZJidm:|aXTlJJVxfGGtZTDh[pRmeiB{IHjyd{BjgSCuaYH1bYQhe2OrboTpcIxifGmxbjDjc5VvfGmwZzygTWM2OCB;IECuPFkh|ryPLh?= M3X5WlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNUe2OVc5Lz5{MEW3OlU4QDxxYU6=
CHO MWrGeY5kfGmxbjDhd5NigQ>? MVeyJIhzew>? M4q0OGlvcGmkaYTpc44hd2ZiaIXtZY4hW0eOVEKg[ZhxemW|c3XkJIlvKEOKTzDj[YxteyCjc4Pld5Nm\CCjczDzc4RqfW1vZHXw[Y5l\W62IGuxOGNeNWGucHjhMY1mfGi7bD3EMYdtfWOxcInyZY5we2mmZTD1dJRic2ViYX\0[ZIhOiCqcoOgZpkhdGmzdXnkJJNkcW62aXzsZZRqd25iY3;1cpRqdmduIFXDOVAhRSByLkCwN{DPxE1w MlW1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjFzMki1PVIoRjJzMUK4OVkzRC:jPh?=
CHO MknOSpVv[3Srb36gZZN{[Xl? Ml3ZNkBpenN? MnHZTY5pcWKrdHnvckBw\iCqdX3hckBUT0yWMTDlfJBz\XO|ZXSgbY4hS0iRIHPlcIx{KGG|c3Xzd4VlKGG|IIPv[Il2dS2mZYDlcoRmdnRiW{G0R30u[WyyaHGtcYV1cHmuLVSt[4x2[2:yeYLhco9{cWSnIIXweIFs\SCjZoTldkAzKGi{czDifUBtcXG3aXSgd4NqdnSrbHzheIlwdiClb4XueIlv\yxiRVO1NEA:KDBwNEK4OUDPxE1w NInyO|c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUGyPFU6Oid-MkGxNlg2QTJ:L3G+
CHO M2DwR2Z2dmO2aX;uJIF{e2G7 MnXJNkBpenN? NUDkXGFLUW6qaXLpeIlwdiCxZjDoeY1idiCVR1zUNkBmgHC{ZYPz[YQhcW5iQ1jPJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiW{G0R31idHCqYT3t[ZRpgWxvRD3ncJVkd3C7cnHuc5Nq\GVidYD0ZYtmKGGodHXyJFIhcHK|IHL5JIxqeXWrZDDzZ4lvfGmubHH0bY9vKGOxdX70bY5oNCCLQ{WwJF0hOC5yMEC0PUDPxE1w Ml;vQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjFzOUOzNFgoRjJzMUmzN|A5RC:jPh?=
CHO MorsSpVv[3Srb36gZZN{[Xl? MoHaOlAhdWmwcx?= MV3Jcohq[mm2aX;uJI9nKGi3bXHuJHNIVFR{IHX4dJJme3OnZDDpckBEUE9iY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBcOTSFXT3hcJBp[S2vZYTofYwuTC2pbIXjc5B6emGwb4Pp[IUhfHKjboPwc5J1KGGodHXyJFYxKG2rboOgZpkhe2OrboTpcIxifGmxbjDjc5VvfGmwZzygTWM2OCB;IECuNFA1KM7:TT6= MkSyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|OUixNlQoRjJzM{m4NVI1RC:jPh?=
CHO M4\KSWZ2dmO2aX;uJIF{e2G7 NXmxPWg5PjBibXnudy=> NUTEZmQyUW6qaXLpeIlwdiCxZjDoeY1idiCVR1zUNkBmgHC{ZYPz[YQhcW5iQ1jPJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiW{G0R30u[WyyaHGtcYV1cHmuLVSt[4x2[2:yeYLhco9{cWSnIITyZY5{eG:{dDDh[pRmeiB4MDDtbY5{KGK7IIPjbY51cWyuYYTpc44h[2:3boTpcochcW5icILld4Vv[2Vib3[gNVAxLSCybHHzcYEtKEmFNUCgQUAxNjB{MjFOwG0v NX3mPFE4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzPVgyOjRpPkKxN|k5OTJ2PD;hQi=>
CHO NV7tcVBXTnWwY4Tpc44h[XO|YYm= NXr3eXJLPjBibXnudy=> MortTY5pcWKrdHnvckBw\iCqdX3hckBUT0yWMTDlfJBz\XO|ZXSgbY4hS0iRIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhYzF2Q22tZYxxcGFvbXX0bJltNURvZ3z1Z49xgXKjbn;zbYRmKHS{YX7zdI9zfCCjZoTldkA3OCCvaX7zJIJ6KHOlaX70bYxt[XSrb36gZ492dnSrbnesJGlEPTBiPTCwMlM4KM7:TT6= NFnTWmM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO5PFEzPCd-MkGzPVgyOjR:L3G+
CHO MV\GeY5kfGmxbjDhd5NigQ>? MnfGOlAhdWmwcx?= MXvJcohq[mm2aX;uJI9nKFOJTGS2JIV5eHKnc4Pl[EBqdiCFSF:gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCdMUTDYU1idHCqYT3t[ZRpgWxvRD3ncJVkd3C7cnHuc5Nq\GVidILhcpNxd3K2IHHmeIVzKDZyIH3pcpMh[nlic3PpcpRqdGyjdHnvckBkd3WwdHnu[{whUUN3MDC9JFAvOzhizszNMi=> MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN7OEGyOEc,OjF|OUixNlQ9N2F-
CHO MWDGeY5kfGmxbjDhd5NigQ>? MX[yJIhzew>? M{nxdWlvcGmkaYTpc44hd2ZiaIXtZY4hW0eOVEKg[ZhxemW|c3XkJIlvKEOKTzDj[YxteyCjc4Pld5Nm\CCjczDbNVREZS2jbIDoZU1u\XSqeXytSE1odHWlb4D5doFvd3OrZHWgeZB1[WunIHHmeIVzKDJiaILzJIJ6KGyrcYXp[EB{[2mwdHnscIF1cW:wIHPveY51\XJuIFnDOVAhRSByLkCwNFQ6KM7:TT6= MmrFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3MUSwNVQoRjJzNUG0NFE1RC:jPh?=
CHO MYjGeY5kfGmxbjDhd5NigQ>? NIrBPZA3OCCvaX7z NVLSb5QyUW6qaXLpeIlwdiCxZjDoeY1idiCVR1zUNkBmgHC{ZYPz[YQhcW5iQ1jPJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiW{G0R30uT2y3Y3;z[UB2eHSja3WgeZNqdmdiW{G0R30udWW2aInsJIdtfWOxcInyZY5we2mmZTDh[pRmeiB4MDDtbY5{KGK7IH3pZ5Jw[mW2YTDwcIF1\SClb4XueIlv\yxiSVO1NEA:KDBwMECzJO69VS5? NFzHWYc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW2OVQ6Pyd-MkG1OlU1QTd:L3G+
CHO M4LFWWZ2dmO2aX;uJIF{e2G7 M2PpSWlvcGmkaYTpc44hd2ZiaIXtZY4hW0eOVEKg[ZhxemW|c3XkJIlvKEOKTzDj[YxteyC3c3nu[{Bu\XSqeXytZYxxcGFvRD3ncJVkd3C7cnHuc5Nq\GViYomgcIlyfWmmIIPjbY51cWyuYYTpc44h[2:3boTpcoctKEmFNUCgQUAxNjByMUO1JO69VS5? MkLKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3OUK3PVQoRjJzNUmyO|k1RC:jPh?=
COS7 NGjxcVNHfW6ldHnvckBie3OjeR?= MnS0NkBpenN? MVrJcohq[mm2aX;uJI9nKGi3bXHuJHNIVFR{IHX4dJJme3OnZDDpckBi\nKrY3HuJIdz\WWwIH3vcotmgSCFT2O3JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiW{G0R30udWW2aInsMYFteGijLVSt[4x2[2:yeYLhco9{cWSnIIXweIFs\SCjZoTldkAzKGi{czDifUB{[2mwdHnscIF1cW:wIHPveY51cW6pIHnuJJBz\XOnbnPlJI9nKDJ3IDWgbJVu[W5icHzhd41iNCCLQ{WwJF0hOC5yMEOyJO69VS5? M335ZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzN{O3NlY3Lz5{MUezO|I3PjxxYU6=
293 MmPKSpVv[3Srb36gZZN{[Xl? M1H1eFEvPSCqcoO= MmnhTY5pcWKrdHnvckBw\iCqdX3hckBUT0yWMTDlfJBz\XO|ZXSgbY4hcHWvYX6gNlk{KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gX|E1S11vbXX0bJltNWGucHjhMWQu\2y3Y3;wfZJidm:|aXTlJJVxfGGtZTDh[pRmeiBzLkWgbJJ{KGK7IIPjbY51cWyuYYTpc44h[2:3boTpcochcW5icILld4Vv[2Vib3[gNlUhLSCqdX3hckBxdGG|bXGsJGlEPTBiPTCzMlEh|ryPLh?= NVLVemljRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG3N|czPjZpPkKxO|M4OjZ4PD;hQi=>
CHO MYHGeY5kfGmxbjDhd5NigQ>? MYeyJIhzew>? MWHJcohq[mm2aX;uJI9nKGi3bXHuJHNIVFR{IHX4dJJme3OnZDDpckBEUE9iY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJHsyPEOfLXzhZoVt\WRiQV3HJIFnfGW{IEKgbJJ{KGK7IHzpdZVq\CC|Y3nueIltdGG2aX;uJINwfW62aX7nMEBKSzVyIE2gNE4xODF|NTFOwG0v M3PXPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOE[4NlM6Lz5{MUi2PFI{QTxxYU6=
CHO M{LESmZ2dmO2aX;uJIF{e2G7 MnrENkBpenN? NF6xTFhKdmirYnn0bY9vKG:oIHj1cYFvKFOJTGSyJIV5eHKnc4Pl[EBqdiCFSF:gZ4VtdHNiYYPz[ZN{\WRiYYOgX|E1S11vYXzwbIEudWW2aInsMWQu\2y3Y3;wfZJidm:|aXTlJJVxfGGtZTDh[pRmeiB{IHjyd{BjgSCuaYH1bYQhe2OrboTpcIxifGmxbjDjc5VvfGmwZzygTWM2OCB;IECuNFAxPDlizszNMi=> NF62Upc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUmwOlk2Oyd-MkG5NFY6PTN:L3G+
CHO-K1 MVPGeY5kfGmxbjDhd5NigQ>? NYTTPVFtUW6qaXLpeIlwdiCxZjDoeY1idiCVR1zUNkBmgHC{ZYPz[YQhcW5iQ1jPMWsyKGOnbHzzJIJ6KFtzNFPdRW1IKHWydHHr[UBie3OjeTygTWM2OCB;IECuNFAyOyEQvF2u NEXrem09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mk[1NlI2PSd-MkK2OVIzPTV:L3G+
CHO-K1 MW\GeY5kfGmxbjDhd5NigQ>? MlPGTY5pcWKrdHnvckBw\iCqdX3hckBUT0yWMTDlfJBz\XO|ZXSgbY4hS0iRLVuxJINmdGy|IHL5JHsyPEOfQV3HJJVxfGGtZTDhd5NigSxiSVO1NEA:KDBwODFOwG0v MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjZ3MkK1OUc,OjJ4NUKyOVU9N2F-
CHO-K1 MYPGeY5kfGmxbjDhd5NigQ>? M{LPTFEzOCCvaX7z NYGzbIFRUW6qaXLpeIlwdiCxZjDoeY1idiCVR1zUNkBmgHC{ZYPz[YQhcW5iQ1jPMWsyKGOnbHzzJIlv[3WkYYTl[EBnd3JiMUKwJI1qdnNiYYSgN|ch\GWpQzDifUBcOTSFXT3BUWchfXC2YXvlJIF{e2G7LDDFR|UxKD1iMD6wNFI1KM7:TT6= M2W1elxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OEG4NFQxLz5{MkixPFA1ODxxYU6=
CHO-K1 MUnGeY5kfGmxbjDhd5NigQ>? MUGxNlAhdWmwcx?= NV[3Z|JFUW6qaXLpeIlwdiCxZjDoeY1idiCVR1zUNUBmgHC{ZYPz[YQhcW5iQ1jPMWsyKGOnbHzzJIlv[3WkYYTl[EBnd3JiMUKwJI1qdnNiYYSgN|ch\GWpQzDifUBcOTSFXT3BUWchfXC2YXvlJIF{e2G7LDDFR|UxKD1iMD61PVMh|ryPLh?= MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjhzOEC0NEc,OjJ6MUiwOFA9N2F-
CHO MlqxSpVv[3Srb36gZZN{[Xl? MlnZOFUhdWmwcx?= MXXJcohq[mm2aX;uJI9nKGi3bXHuJHNIVFR{IHX4dJJme3OnZDDpckBEUE9iY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB{d2SrdX2t[IVx\W6mZX70JHsyPEOfbXX0bJltNWGucHjhMWQu\2y3Y3;wfZJidm:|aXTlJJVxfGGtZTDh[pRmeiB2NTDtbY5{NCCLQ{WwJF0hOC5yMEGzJO69VS5? Mm\nQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ6OEmzOVEoRjJ{OEi5N|UyRC:jPh?=
CHO MWfGeY5kfGmxbjDhd5NigQ>? MmHyOFUhdWmwcx?= MV3Jcohq[mm2aX;uJI9nKGi3bXHuJHNIVFRzIHX4dJJme3OnZDDpckBEUE9iY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB{d2SrdX2t[IVx\W6mZX70JHsyPEOfbXX0bJltNWGucHjhMWQu\2y3Y3;wfZJidm:|aXTlJJVxfGGtZTDh[pRmeiB2NTDtbY5{NCCLQ{WwJF0hOC56IN88UU4> MmTCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ6OEmzOVEoRjJ{OEi5N|UyRC:jPh?=
CHOK1 NUfSfmNITnWwY4Tpc44h[XO|YYm= NYS4NVVsOyCqcoO= M1jOPWlvcGmkaYTpc44hd2ZiaIXtZY4hW0eOVEGg[ZhxemW|c3XkJIlvKEOKT1uxJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiW{G0R30uSU2JIIXweIFs\SCjZoTldkA{KGi{czDifUBucWO{b3LleIEhe2OrboTpcIxifGmxbjDjc5VvfGmwZzDhcoFtgXOrczygTWM2OCB;IECuPFkyKM7:TT6= NXvnfFhURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4OFI3OThpPkK0PFQzPjF6PD;hQi=>
CHO NET2VmFHfW6ldHnvckBie3OjeR?= NFnMT4IzKGi{cx?= NF;4emlKdmirYnn0bY9vKG:oIHj1cYFvKFOJTGSyJIV5eHKnc4Pl[EBqdiCFSF:gZ4VtdHNiYYPz[ZN{\WRiYYOgX|E1S11vYXzwbIEudWW2aInsMWQu\2y3Y3;wfZJidm:|aXTlJJVxfGGtZTDh[pRmeiB{IHjyd{BjgSCuaYH1bYQhe2OrboTpcIxifGmxbjDjc5VvfGmwZzygTWM2OCB;IECuNFAxPDlizszNMi=> MnXoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MECyPVcoRjJ2OUCwNlk4RC:jPh?=
CHO M{jmNmZ2dmO2aX;uJIF{e2G7 MWqyJIhzew>? NETCOVFEd22yZYTpeIl3\SCrbnjpZol1cW:wIH;mJIZ2dGxvbHXu[5RpKGi3bXHuJHNIVFR{IHX4dJJme3OnZDDpckBEUE9iY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB{d2SrdX2t[IVx\W6mZX70JHsyPEOfLXHsdIhiNW2ndHj5cE1FNWeudXPvdJlz[W6xc3nk[UB2eHSja3WgZYZ1\XJiMjDodpMh[nlic3PpcpRqdGyjdHnvckBkd3WwdHnu[{whUUN3MDC9JFAvODB3IN88UU4> NH7CNog9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[1NFI2PCd-MkW2OVAzPTR:L3G+
CHO MWjGeY5kfGmxbjDhd5NigQ>? NWDMfGRbOTJyIH3pcpM> M2LnbWlvcGmkaYTpc44hd2ZiaIXtZY4hW0eOVEKg[ZhxemW|c3XkJIlvKEOKTzDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckB2eHSja3Wgc4YhYzF2Q23BUWch[W[2ZYKgNVIxKG2rboOgZpkhXG:yQ3;1cpQhdWW2aH;kMEBKSzVyIE2gNE4xODF3IN88UU4> NX[zPZY1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0OFc4QTFpPkK4OFQ4PzlzPD;hQi=>
CHO MlHjSpVv[3Srb36gZZN{[Xl? MmfoNVIxKG2rboO= MYPJcohq[mm2aX;uJI9nKGi3bXHuJHNIVFRzIHX4dJJme3OnZDDpckBEUE9iY3XscJMh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6geZB1[WunIH;mJHsyPEOfQV3HJIFnfGW{IEGyNEBucW6|IHL5JHRweEOxdX70JI1mfGixZDygTWM2OCB;IECuOlI6KM7:TT6= M4i3T|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NES3O|kyLz5{OES0O|c6OTxxYU6=
CHO MmPjSpVv[3Srb36gZZN{[Xl? M{[5dlEhcHJ? NHrXS5RKdmirYnn0bY9vKG:oIHj1cYFvKFOJTGSyJIV5eHKnc4Pl[EBqdiCFSF:gZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKFtzNFPdRW1IKHWydHHr[UBi\nSncjCxJIhzKGK7IH3pZ5Jw[mW2YTDjc5VvfGmwZzDt[ZRpd2RuIFXDOVAhRSByLkCwNkDPxE1w MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTJzNkW2NEc,Ojl{MU[1OlA9N2F-
CHO NHfTTI9HfW6ldHnvckBie3OjeR?= NHvtNXIyKGi{ MX7Jcohq[mm2aX;uJI9nKGi3bXHuJHNIVFRzIHX4dJJme3OnZDDpckBEUE9iY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJHsyPEOfQV3HJJVxfGGtZTDh[pRmeiBzIHjyJIJ6KG2rY4LvZoV1[SClb4XueIlv\yCvZYToc4QtKEWFNUCgQUAxNjh4IN88UU4> NYXqZ21URGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmyNVY2PjBpPkK5NlE3PTZyPD;hQi=>
CHO NHTqTnVHfW6ldHnvckBie3OjeR?= NIezb5AyKGi{ NF61Wm5KdmirYnn0bY9vKG:oIH\1cIwudGWwZ4ToJIh2dWGwIGPHUHQzKGW6cILld5Nm\CCrbjDDTG8h[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iW{G0R30udWW2aInsJIFteGijLVSt[4x2[2:yeYLhco9{cWSnIIXweIFs\SCjZoTldkAyKGi{IHL5JIxqeXWrZDDzZ4lvfGmubHH0bY9vKGOxdX70bY5oKG2ndHjv[EwhUUN3MDC9JFAvODBzMEWg{txONg>? MlSyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl5NkS3OFIoRjJ7N{[0O|QzRC:jPh?=
HEK293 NF7p[GpHfW6ldHnvckBie3OjeR?= M1\CWFExKG2rboO= NGnRb2VKdmirYnn0bY9vKG:oIHj1cYFvKFOJTGSyJIV5eHKnc4Pl[EBqdiCKRVuyPVMh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iW{G0R30uSU2JIIXweIFs\SCycnXpcoN2[mG2ZXSg[o9zKDFyIH3pcpMh\m:ubH;3[YQh[nliW{G0R30uSU2JIHHk[Il1cW:wIHHu[EBu\WG|dYLl[EBi\nSncjCyJIhzeyCkeTDsbZF2cWRic3PpcpRqdGyjdHnvckBkd3WwdHnu[{Bu\XSqb3SsJGlEPTBiPTCwMlAxOTRizszNMi=> MnXXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl7NUS2PFIoRjJ7OUW0OlgzRC:jPh?=
HEK293 M2rteWZ2dmO2aX;uJIF{e2G7 NI\wUJYyOCCvaX7z MXLJcohq[mm2aX;uJI9nKGi3bXHuJHNIVFRzIHX4dJJme3OnZDDpckBJTUt{OUOgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4hYzF2Q22tRW1IKHWydHHr[UBxemWrbnP1ZoF1\WRiZn;yJFExKG2rboOg[o9tdG:5ZXSgZpkhYzF2Q22tRW1IKGGmZHn0bY9vKGGwZDDt[YF{fXKnZDDh[pRmeiB{IHjyd{BjgSCuaYH1bYQhe2OrboTpcIxifGmxbjDjc5VvfGmwZzDt[ZRpd2RuIFnDOVAhRSBzLkizJO69VS5? Ml7HQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl7NUS2PFIoRjJ7OUW0OlgzRC:jPh?=
Assay
Methods Test Index PMID
Western blot HIF-1α / p-AMPK / AMPK / p-ERK / ERK / β-actin ; DDR1 ; HIF-1α / PHD2 / tubulin ; p-elf2α / t-elf2α / tubulin-α ; Bax / Bcl2 / PARP / β-actin 27391020 31979355 32444604 31285506
Growth inhibition assay Tumor volume 28763435
IHC TUNEL-positive cells ; HIF1 ; TUNEL-positive cells ; mice kidney sections ; HE staining / SGLT2 27391020 32444604 28763435
Immunofluorescence Metabolic switch in diabetic kidneys ; F-actin ; EdU ; PECAM-1 / α-SMA ; podocytes 32444604 32848736 30089717
In vivo Dapagliflozin reduces blood glucose levels by 55% after 0.1 mg/kg oral dose in hyperglycemic streptozotocin (STZ) rats, which is in part to the metabolic stability conferred by the C-glucoside linkage. Dapagliflozin displays a favorable absorption, distribution, metabolism, and excretion (ADME) profile and is orally bioavailable. [1] Dapagliflozin (1 mg/kg) causes significant dose-dependent glucosuria and increase in urine volume in normal rats over 24 hours post-dose. Dapagliflozin induces increase in urine glucose and urine volume excretion at 6 hours post-dose in Zucker diabetic fatty (ZDF) rats. Dapagliflozin lowers fasting and fed glucose levels in ZDF rats even by 2 weeks of treatment, without any marker of renal or liver toxicity. [2] Dapagliflozin significantly reduces the development of hyperglycaemia, with lowered blood glucose. Dapagliflozin could improve the insulin sensitivity, reduce β-cell mass and the development of impaired pancreatic function. [4]

Protocol (from reference)

Animal Research:[1]
  • Animal Models: Normal Sprague Dawley rats or streptozotocin induced male Sprague Dawley rats
  • Dosages: 0.01-10 mg/kg (1 mL/kg) followed by a 50% glucose solution (2 g/kg)
  • Administration: Dosed orally
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 82 mg/mL
(200.55 mM)
Water Insoluble
Ethanol ''17 mg/mL

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+40%PEG300+5% tween80+50% H2O
For best results, use promptly after mixing.

4.1 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 408.87
Formula

C21H25ClO6

CAS No. 461432-26-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCOC1=CC=C(C=C1)CC2=C(C=CC(=C2)C3C(C(C(C(O3)CO)O)O)O)Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04887935 Not yet recruiting Drug: Dapagliflozin|Device: BIOSENSE Meter Prostate Cancer|Cancer of Prostate Washington University School of Medicine September 30 2022 Phase 1
NCT05174052 Not yet recruiting Drug: Dapagliflozin 10Mg Tab|Drug: Placebo Diabete Mellitus|Atrial Fibrillation University of Oklahoma February 2022 Phase 3
NCT05141552 Not yet recruiting Drug: Dapagliflozin 10Mg Tab Hemodialysis Complication RenJi Hospital December 1 2021 Not Applicable
NCT05188144 Recruiting -- Heart Failure AstraZeneca November 29 2021 --
NCT04923295 Recruiting Drug: Dapagliflozin 10Mg Tab Peritoneal Dialysis Complication|Ultrafiltration Failure An-Najah National University June 2 2021 Not Applicable

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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