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 29 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 MoPHSpVv[3Srb36gZZN{[Xl? NVux[HpzOiCq NUnUS3c{UW6qaXLpeIlwdiCxZjDoeY1idiCVR1zUNkBmgHC{ZYPz[YQhcW5iQ1jPJINmdGy|IHHzd4V{e2WmIHHzJHsyPEOfYXzwbIEudWW2aInsMWQu\2y3Y3;wfZJidm:|aXTlJJVxfGGtZTDh[pRmeiB{IHjyd{BjgSCuaYH1bYQhe2OrboTpcIxifGmxbjDjc5VvfGmwZzygTWM2OD1yLkCwNFQ6KM7:TR?= MmjoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB2M{S5NFkoRjJyNEO0PVA6RC:jPh?=
CHOK1 cells M4HPW2Z2dmO2aX;uJIF{e2G7 NELzXGw{KGh? NIHDW5JKdmirYnn0bY9vKG:oIHj1cYFvKFOJTGSyJIV5eHKnc4Pl[EBqdiCFSF;LNUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIGuxOGNeNUGPRzD1dJRic2ViYX\0[ZIhOyCqcoOgZpkhdWmlcn;i[ZRiKHOlaX70bYxt[XSrb36gZ492dnSrbnegZY5idHm|aYOsJGlEPTB;MD6wNFEh|ryP MnTBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6NEK2NVgoRjJ2OESyOlE5RC:jPh?=
HEK293.ETN cells NYXjRmdxTnWwY4Tpc44h[XO|YYm= MXSxMlUhcA>? NH\1PJlKdmirYnn0bY9vKG:oIHj1cYFvKFOJTGSyJJRz[W6|ZnXjeIVlKGmwIFjFT|I6Oy6HVF6gZ4VtdHNiYYPz[ZN{\WRiYYOgRW1IKHWydHHr[UBi\nSncjCxMlUhcHK|IHL5JJNkcW62aXzsZZRqd25iY3;1cpRqdmduIFnDOVA:OC5yME[3JO69VQ>? NXK4blN1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4PVY{PzRpPkG5PFk3Ozd2PD;hQi=>
COS-7 cells NV3XdmdvTnWwY4Tpc44h[XO|YYm= MUeyJIg> NELkR4xKdmirYnn0bY9vKG:oIHj1cYFvKFOJTGSxJJRz[W6|ZnXjeIVlKGmwIFPPV{04KGOnbHzzJIF{e2W|c3XkJIF{KEGPRzD1dJRic2ViYX\0[ZIhOiCqcoOgZpkhe2OrboTpcIxifGmxbjDjc5VvfGmwZzygTWM2OD1yLki5JO69VQ>? M2nuOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEm2N|c1Lz5zOUi5OlM4PDxxYU6=
CHO MX7GeY5kfGmxbjDhd5NigQ>? MXXJcohq[mm2aX;uJI9nKGi3bXHuJHNIVFR{IHX4dJJme3OnZDDpckBEUE9iY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBcOTSFXVHNS{Bi[2O3bYXsZZRqd25uIFXDOVAhRSByLkCwNVEh|ryPLh?= MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDJ4ME[xPEc,OTh{NkC2NVg9N2F-
CHO MoXTSpVv[3Srb36gZZN{[Xl? M3XYbmlvcGmkaYTpc44hd2ZicnH0JHNIVFR{IHX4dJJme3OnZDDpckBEUE9iY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBcOTSFXVHNS{Bi[2O3bYXsZZRqd25uIFXDOVAhRSByLkCwN{DPxE1w MmHPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh{NkC2NVgoRjF6Mk[wOlE5RC:jPh?=
CHO NWXh[Zd4TnWwY4Tpc44h[XO|YYm= MnjsTY5pcWKrdHnvckBw\iCqdX3hckBUT0yWMTDlfJBz\XO|ZXSgbY4hS0iRIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhYzF2Q23BUWch[WOldX31cIF1cW:wLDDFR|UxKD1iMT6zPUDPxE1w MkTnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh{NkC2NVgoRjF6Mk[wOlE5RC:jPh?=
HEK293.ETN Mli4SpVv[3Srb36gZZN{[Xl? M1rvfGlvcGmkaYTpc44hd2ZiaIXtZY4hW0eOVEKg[ZhxemW|c3XkJIlvKEiHS{K5N{5GXE5iY3XscJMh[XO|ZYPz[YQh[XNibXX0bJltNWGucHjhMWQuY1VvMUTDYYdtfWOxcInyZY5we2mmZTD1dJRic2ViYomgd4NqdnSrbHzheIlwdiClb4XueIlv\yxiSVO1NEA:KDBwMEC2O{DPxE1w NHzEW3I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUewNFMyQCd-MUm3NFA{OTh:L3G+
COS7 M1Tpc2Z2dmO2aX;uJIF{e2G7 MYfJcohq[mm2aX;uJI9nKGi3bXHuJHNIVFRzIHX4dJJme3OnZDDpckBi\nKrY3HuJIdz\WWwIH3vcotmgSCFT2O3JINmdGy|IHHzd4V{e2WmIHHzJI1mfGi7bD3hcJBp[S2GLWvVMVE1S12pbIXjc5B6emGwb4Pp[IUhfXC2YXvlJIJ6KHOlaX70bYxt[XSrb36gZ492dnSrbnesJGlEPTBiPTCwMlg5PSEQvF2u NUS3dohQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm3NFA{OThpPkG5O|AxOzF6PD;hQi=>
HEK293 NIfhPZhHfW6ldHnvckBie3OjeR?= MlW3TY5pcWKrdHnvckBw\iCqdX3hckBUT0yWMTDlfJBz\XO|ZXSgbY4hUEWNMkmzJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiW{G0R31idHCqYT3t[ZRpgWypbIXjc5B6emGwb4Pp[IUhfXC2YXvlMEBKSzVyIE2gNE45OSEQvF2u NGrUbnE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUe4OVQ{PSd-MUm3PFU1OzV:L3G+
CHO M1XyWmZ2dmO2aX;uJIF{e2G7 NW\tPYU1OiCqcoO= M2\NWWlvcGmkaYTpc44hd2ZiaIXtZY4hW0eOVEKg[ZhxemW|c3XkJIlvKEOKTzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKHOxZHn1cU1l\XCnbnTlcpQhdWW2aInsMYFteGijLVStX3UuOTSFXXfseYNweHm{YX7vd4ll\SC3cIThb4Uh[W[2ZYKgNkBpenNuIFnDOVAhRSByLkCwNVQh|ryPLh?= NE\pNZI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEG0PVY2Oyd-MkCxOFk3PTN:L3G+
CHO MUfGeY5kfGmxbjDhd5NigQ>? MV:yJIhzew>? MknJTY5pcWKrdHnvckBw\iCqdX3hckBUT0yWMTDlfJBz\XO|ZXSgbY4hS0iRIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yhe2:maYXtMYRmeGWwZHXueEBu\XSqeXytZYxxcGFvRD3bWU0yPEOfZ3z1Z49xgXKjbn;zbYRmKHWydHHr[UBi\nSncjCyJIhzeyxiSVO1NEA:KDFwMjFOwG0v MkPkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjBzNEm2OVMoRjJyMUS5OlU{RC:jPh?=
CHO M1\WemZ2dmO2aX;uJIF{e2G7 NFfMUZBKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IGPHUHQzKGW6cILld5Nm\CCrbjDDTG8h[2WubIOgZpkhdGmzdXnkJJNkcW62aXzsZZRqd25iY3;1cpRqdmduIFnDOVAhRSByLkCwNFQ6KM7:TT6= NUXwOJZIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCxPFE1QDZpPkKwNVgyPDh4PD;hQi=>
HEK293 M4TkZWZ2dmO2aX;uJIF{e2G7 NXWxTmtFOS53IHjydy=> MWLJcohq[mm2aX;uJI9nKGi3bXHuJHNIVFR{IHX4dJJme3OnZDDpckBJTUt{OUOgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCdMUTDYYFteGijLX3leIh6dC2GLXfseYNweHm{YX7vd4ll\SC3cIThb4Uh[W[2ZYKgNU42KGi{czDifUBtcXG3aXSgd4NqdnSrbHzheIlwdiClb4XueIlv\yxiSVO1NEA:KDBwMEC2O{DPxE1w MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODV5NkW3PEc,OjB3N{[1O|g9N2F-
COS7 NGnsO4hHfW6ldHnvckBie3OjeR?= MkjLNkBpenN? M1zrU2lvcGmkaYTpc44hd2ZiaIXtZY4hW0eOVEGg[ZhxemW|c3XkJIlvKGGocnnjZY4h\3KnZX6gcY9vc2W7IFPPV|ch[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDbNVREZWGucHjhMY1mfGi7bD3EMYdtfWOxcInyZY5we2mmZTD1dJRic2ViYX\0[ZIhOiCqcoOgZpkhdGmzdXnkJJNkcW62aXzsZZRqd25iY3;1cpRqdmduIFnDOVAhRSByLki5JO69VS5? NXmzUYRKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1O|Y2PzhpPkKwOVc3PTd6PD;hQi=>
CHO NHPmSIJHfW6ldHnvckBie3OjeR?= M3jnNFIhcHK| NXPYcFFrUW6qaXLpeIlwdiCxZjDoeY1idiCVR1zUNkBmgHC{ZYPz[YQhcW5iQ1jPJINmdGy|IHHzd4V{e2WmIHHzJJNw\Gm3bT3k[ZBmdmSnboSgX|E1S11vYXzwbIEudWW2aInsMWQu\2y3Y3;wfZJidm:|aXTlJJVxfGGtZTDh[pRmeiB{IHjyd{BjgSCuaYH1bYQhe2OrboTpcIxifGmxbjDjc5VvfGmwZzygSWM2OCB;IECuNFA{KM7:TT6= MkDSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjFzMki1PVIoRjJzMUK4OVkzRC:jPh?=
CHO NX7xTm1{TnWwY4Tpc44h[XO|YYm= MmrZNkBpenN? M4XnWmlvcGmkaYTpc44hd2ZiaIXtZY4hW0eOVEGg[ZhxemW|c3XkJIlvKEOKTzDj[YxteyCjc4Pld5Nm\CCjczDzc4RqfW1vZHXw[Y5l\W62IGuxOGNeNWGucHjhMY1mfGi7bD3EMYdtfWOxcInyZY5we2mmZTD1dJRic2ViYX\0[ZIhOiCqcoOgZpkhdGmzdXnkJJNkcW62aXzsZZRqd25iY3;1cpRqdmduIFXDOVAhRSByLkSyPFUh|ryPLh?= M3XiVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMUK4OVkzLz5{MUGyPFU6OjxxYU6=
CHO NX61c2dXTnWwY4Tpc44h[XO|YYm= Mn3aNkBpenN? NVXE[opMUW6qaXLpeIlwdiCxZjDoeY1idiCVR1zUNkBmgHC{ZYPz[YQhcW5iQ1jPJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiW{G0R31idHCqYT3t[ZRpgWxvRD3ncJVkd3C7cnHuc5Nq\GVidYD0ZYtmKGGodHXyJFIhcHK|IHL5JIxqeXWrZDDzZ4lvfGmubHH0bY9vKGOxdX70bY5oNCCLQ{WwJF0hOC5yMEC0PUDPxE1w NEG2Xnk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUG5N|MxQCd-MkGxPVM{ODh:L3G+
CHO M1zXVmZ2dmO2aX;uJIF{e2G7 M33keFYxKG2rboO= MlH5TY5pcWKrdHnvckBw\iCqdX3hckBUT0yWMjDlfJBz\XO|ZXSgbY4hS0iRIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhYzF2Q22tZYxxcGFvbXX0bJltNURvZ3z1Z49xgXKjbn;zbYRmKHS{YX7zdI9zfCCjZoTldkA3OCCvaX7zJIJ6KHOlaX70bYxt[XSrb36gZ492dnSrbnesJGlEPTBiPTCwMlAxPCEQvF2u NIW4W|Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO5PFEzPCd-MkGzPVgyOjR:L3G+
CHO NF;oPXdHfW6ldHnvckBie3OjeR?= NF;FZWI3OCCvaX7z NHe4ZZlKdmirYnn0bY9vKG:oIHj1cYFvKFOJTGSyJIV5eHKnc4Pl[EBqdiCFSF:gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCdMUTDYU1idHCqYT3t[ZRpgWxvRD3ncJVkd3C7cnHuc5Nq\GVidILhcpNxd3K2IHHmeIVzKDZyIH3pcpMh[nlic3PpcpRqdGyjdHnvckBkd3WwdHnu[{BqdiCycnXz[Y5k\SCxZjCxNFAmKHCuYYPtZUwhUUN3MDC9JFAvODJ{IN88UU4> NUHrbJBmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzPVgyOjRpPkKxN|k5OTJ2PD;hQi=>
CHO MVHGeY5kfGmxbjDhd5NigQ>? MVG2NEBucW6| NILmNphKdmirYnn0bY9vKG:oIHj1cYFvKFOJTGSxJIV5eHKnc4Pl[EBqdiCFSF:gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCdMUTDYU1idHCqYT3t[ZRpgWxvRD3ncJVkd3C7cnHuc5Nq\GVidILhcpNxd3K2IHHmeIVzKDZyIH3pcpMh[nlic3PpcpRqdGyjdHnvckBkd3WwdHnu[{whUUN3MDC9JFAvOzdizszNMi=> NILZU5Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO5PFEzPCd-MkGzPVgyOjR:L3G+
CHO M2XWdWZ2dmO2aX;uJIF{e2G7 NWPZdlFCPjBibXnudy=> M13hXGlvcGmkaYTpc44hd2ZiU1fMWFYh\XiycnXzd4VlKGmwIFPIU{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIGuxOGNeNWGucHjhMY1mfGi7bD3EMYdtfWOxcInyZY5we2mmZTD0doFve3CxcoSgZYZ1\XJiNkCgcYlveyCkeTDzZ4lvfGmubHH0bY9vKGOxdX70bY5oNCCLQ{WwJF0hOC5|ODFOwG0v NXnDdJFLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzPVgyOjRpPkKxN|k5OTJ2PD;hQi=>
CHO MVzGeY5kfGmxbjDhd5NigQ>? MXOyJIhzew>? MWHJcohq[mm2aX;uJI9nKGi3bXHuJHNIVFR{IHX4dJJme3OnZDDpckBEUE9iY3XscJMh[XO|ZYPz[YQh[XNiW{G0R30u[WyyaHGtcYV1cHmuLVSt[4x2[2:yeYLhco9{cWSnIIXweIFs\SCjZoTldkAzKGi{czDifUBtcXG3aXSgd4NqdnSrbHzheIlwdiClb4XueIVzNCCLQ{WwJF0hOC5yMEC0PUDPxE1w NXruS5hCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1NVQxOTRpPkKxOVE1ODF2PD;hQi=>
CHO NH\YZYZHfW6ldHnvckBie3OjeR?= MnK0OlAhdWmwcx?= MoXITY5pcWKrdHnvckBw\iCqdX3hckBUT0yWMjDlfJBz\XO|ZXSgbY4hS0iRIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhYzF2Q22tS4x2[2:|ZTD1dJRic2VidYPpcochYzF2Q22tcYV1cHmuIHfseYNweHm{YX7vd4ll\SCjZoTldkA3OCCvaX7zJIJ6KG2rY4LvZoV1[SCybHH0[UBkd3WwdHnu[{whUUN3MDC9JFAvODB|IN88UU4> NWDmXlBrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG1OlU1QTdpPkKxOVY2PDl5PD;hQi=>
CHO NVi0TZo{TnWwY4Tpc44h[XO|YYm= NUHyOmwxUW6qaXLpeIlwdiCxZjDoeY1idiCVR1zUNkBmgHC{ZYPz[YQhcW5iQ1jPJINmdGy|IIXzbY5oKG2ndHj5cE1idHCqYT3EMYdtfWOxcInyZY5we2mmZTDifUBtcXG3aXSgd4NqdnSrbHzheIlwdiClb4XueIlv\yxiSVO1NEA:KDBwMECxN|Uh|ryPLh?= MkjhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3OUK3PVQoRjJzNUmyO|k1RC:jPh?=
COS7 NHW1PGFHfW6ldHnvckBie3OjeR?= NEDReokzKGi{cx?= MnX1TY5pcWKrdHnvckBw\iCqdX3hckBUT0yWMjDlfJBz\XO|ZXSgbY4h[W[{aXPhckBoemWnbjDtc45s\XliQ1;TO{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIGuxOGNeNW2ndHj5cE1idHCqYT3EMYdtfWOxcInyZY5we2mmZTD1dJRic2ViYX\0[ZIhOiCqcoOgZpkhe2OrboTpcIxifGmxbjDjc5VvfGmwZzDpckBxemW|ZX7j[UBw\iB{NTClJIh2dWGwIIDsZZNu[SxiSVO1NEA:KDBwMECzNkDPxE1w MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTd|N{K2Okc,OjF5M{eyOlY9N2F-
293 M2PGUGZ2dmO2aX;uJIF{e2G7 NF3r[JcyNjViaILz M{fReGlvcGmkaYTpc44hd2ZiaIXtZY4hW0eOVEGg[ZhxemW|c3XkJIlvKGi3bXHuJFI6OyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJHsyPEOfLX3leIh6dC2jbIDoZU1FNWeudXPvdJlz[W6xc3nk[UB2eHSja3WgZYZ1\XJiMT61JIhzeyCkeTDzZ4lvfGmubHH0bY9vKGOxdX70bY5oKGmwIIDy[ZNmdmOnIH;mJFI2KCViaIXtZY4heGyjc33hMEBKSzVyIE2gN{4yKM7:TT6= NGjXe3I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUezO|I3Pid-MkG3N|czPjZ:L3G+
CHO NXW2fIxVTnWwY4Tpc44h[XO|YYm= NV7hcpA5OiCqcoO= NHPxZ|FKdmirYnn0bY9vKG:oIHj1cYFvKFOJTGSyJIV5eHKnc4Pl[EBqdiCFSF:gZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKFtzNFPdMYxi[mWuZXSgRW1IKGGodHXyJFIhcHK|IHL5JIxqeXWrZDDzZ4lvfGmubHH0bY9vKGOxdX70bY5oNCCLQ{WwJF0hOC5yMEGzOUDPxE1w NFnjbnA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUi2PFI{QSd-MkG4OlgzOzl:L3G+
CHO MmPQSpVv[3Srb36gZZN{[Xl? MWWyJIhzew>? M{nObWlvcGmkaYTpc44hd2ZiaIXtZY4hW0eOVEKg[ZhxemW|c3XkJIlvKEOKTzDj[YxteyCjc4Pld5Nm\CCjczDbNVREZS2jbIDoZU1u\XSqeXytSE1odHWlb4D5doFvd3OrZHWgeZB1[WunIHHmeIVzKDJiaILzJIJ6KGyrcYXp[EB{[2mwdHnscIF1cW:wIHPveY51cW6pLDDJR|UxKD1iMD6wNFA1QSEQvF2u MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTlyNkm1N{c,OjF7ME[5OVM9N2F-
CHO-K1 NHPVbY1HfW6ldHnvckBie3OjeR?= M1;sO2lvcGmkaYTpc44hd2ZiaIXtZY4hW0eOVEKg[ZhxemW|c3XkJIlvKEOKTz3LNUBk\WyuczDifUBcOTSFXVHNS{B2eHSja3WgZZN{[XluIFnDOVAhRSByLkCwNVMh|ryPLh?= M{XTTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWyNlU2Lz5{Mk[1NlI2PTxxYU6=
CHO-K1 M3\HN2Z2dmO2aX;uJIF{e2G7 MoDnTY5pcWKrdHnvckBw\iCqdX3hckBUT0yWMTDlfJBz\XO|ZXSgbY4hS0iRLVuxJINmdGy|IHL5JHsyPEOfQV3HJJVxfGGtZTDhd5NigSxiSVO1NEA:KDBwODFOwG0v M4TY[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NkWyNlU2Lz5{Mk[1NlI2PTxxYU6=
CHO-K1 M4HzT2Z2dmO2aX;uJIF{e2G7 MkLENVIxKG2rboO= MmjvTY5pcWKrdHnvckBw\iCqdX3hckBUT0yWMjDlfJBz\XO|ZXSgbY4hS0iRLVuxJINmdGy|IHnuZ5Vj[XSnZDDmc5IhOTJyIH3pcpMh[XRiM{eg[IVoSyCkeTDbNVREZS2DTVegeZB1[WunIHHzd4F6NCCHQ{WwJF0hOC5yMEK0JO69VS5? MlzhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ6MUiwOFAoRjJ{OEG4NFQxRC:jPh?=
CHO-K1 NFLYc4lHfW6ldHnvckBie3OjeR?= NFXFNoUyOjBibXnudy=> MWPJcohq[mm2aX;uJI9nKGi3bXHuJHNIVFRzIHX4dJJme3OnZDDpckBEUE9vS{GgZ4VtdHNiaX7jeYJifGWmIH\vdkAyOjBibXnud{BifCB|NzDk[YdEKGK7IGuxOGNeNUGPRzD1dJRic2ViYYPzZZktKEWFNUCgQUAxNjV7MzFOwG0v NWfUZW1SRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK4NVgxPDBpPkKyPFE5ODRyPD;hQi=>
CHO MYnGeY5kfGmxbjDhd5NigQ>? M{jYPFQ2KG2rboO= NUHtcXpEUW6qaXLpeIlwdiCxZjDoeY1idiCVR1zUNkBmgHC{ZYPz[YQhcW5iQ1jPJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2Zic3;kbZVuNWSncHXu[IVvfCCdMUTDYY1mfGi7bD3hcJBp[S2GLXfseYNweHm{YX7vd4ll\SC3cIThb4Uh[W[2ZYKgOFUhdWmwczygTWM2OCB;IECuNFAyOyEQvF2u NHnTZ5Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Mki4PVM2OSd-MkK4PFk{PTF:L3G+
CHO MknUSpVv[3Srb36gZZN{[Xl? MUm0OUBucW6| NGjhcJVKdmirYnn0bY9vKG:oIHj1cYFvKFOJTGSxJIV5eHKnc4Pl[EBqdiCFSF:gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iC|b3TpeY0u\GWyZX7k[Y51KFtzNFPdcYV1cHmuLXHsdIhiNURvZ3z1Z49xgXKjbn;zbYRmKHWydHHr[UBi\nSncjC0OUBucW6|LDDJR|UxKD1iMD64JO69VS5? NUizcI54RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK4PFk{PTFpPkKyPFg6OzVzPD;hQi=>
CHOK1 M3rzV2Z2dmO2aX;uJIF{e2G7 MVezJIhzew>? NVTlXYlJUW6qaXLpeIlwdiCxZjDoeY1idiCVR1zUNUBmgHC{ZYPz[YQhcW5iQ1jPT|Eh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDbNVREZS2DTVegeZB1[WunIHHmeIVzKDNiaILzJIJ6KG2rY4LvZoV1[SC|Y3nueIltdGG2aX;uJINwfW62aX7nJIFv[Wy7c3nzMEBKSzVyIE2gNE45QTFizszNMi=> MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh2Mk[xPEc,OjR6NEK2NVg9N2F-
CHO MUXGeY5kfGmxbjDhd5NigQ>? M3jVO|IhcHK| MoPGTY5pcWKrdHnvckBw\iCqdX3hckBUT0yWMjDlfJBz\XO|ZXSgbY4hS0iRIHPlcIx{KGG|c3Xzd4VlKGG|IGuxOGNeNWGucHjhMY1mfGi7bD3EMYdtfWOxcInyZY5we2mmZTD1dJRic2ViYX\0[ZIhOiCqcoOgZpkhdGmzdXnkJJNkcW62aXzsZZRqd25iY3;1cpRqdmduIFnDOVAhRSByLkCwNFQ6KM7:TT6= MlH4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MECyPVcoRjJ2OUCwNlk4RC:jPh?=
CHO NHTVNYRHfW6ldHnvckBie3OjeR?= NWTCTIxtOiCqcoO= MUfDc41x\XSrdHn2[UBqdmirYnn0bY9vKG:oIH\1cIwudGWwZ4ToJIh2dWGwIGPHUHQzKGW6cILld5Nm\CCrbjDDTG8h[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDzc4RqfW1vZHXw[Y5l\W62IGuxOGNeNWGucHjhMY1mfGi7bD3EMYdtfWOxcInyZY5we2mmZTD1dJRic2ViYX\0[ZIhOiCqcoOgZpkhe2OrboTpcIxifGmxbjDjc5VvfGmwZzygTWM2OCB;IECuNFA2KM7:TT6= MkSwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4NUCyOVQoRjJ3NkWwNlU1RC:jPh?=
CHO M13NV2Z2dmO2aX;uJIF{e2G7 M37q[VEzOCCvaX7z M{DlbWlvcGmkaYTpc44hd2ZiaIXtZY4hW0eOVEKg[ZhxemW|c3XkJIlvKEOKTzDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckB2eHSja3Wgc4YhYzF2Q23BUWch[W[2ZYKgNVIxKG2rboOgZpkhXG:yQ3;1cpQhdWW2aH;kMEBKSzVyIE2gNE4xODF3IN88UU4> MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR2N{e5NUc,Ojh2NEe3PVE9N2F-
CHO MljMSpVv[3Srb36gZZN{[Xl? Mlr4NVIxKG2rboO= NXO3TnF[UW6qaXLpeIlwdiCxZjDoeY1idiCVR1zUNUBmgHC{ZYPz[YQhcW5iQ1jPJINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKHWydHHr[UBw\iCdMUTDYWFOTyCjZoTldkAyOjBibXnud{BjgSCWb4DDc5VvfCCvZYToc4QtKEmFNUCgQUAxNjZ{OTFOwG0v NVLKUlE4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0OFc4QTFpPkK4OFQ4PzlzPD;hQi=>
CHO M{XnZ2Z2dmO2aX;uJIF{e2G7 MYKxJIhz NWPxOGFvUW6qaXLpeIlwdiCxZjDoeY1idiCVR1zUNkBmgHC{ZYPz[YQhcW5iQ1jPJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiCdMUTDYWFOTyC3cIThb4Uh[W[2ZYKgNUBpeiCkeTDtbYNzd2KndHGgZ492dnSrbnegcYV1cG:mLDDFR|UxKD1iMD6wNFIh|ryPLh?= NHOxO4Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUKxOlU3OCd-MkmyNVY2PjB:L3G+
CHO NEXGXFNHfW6ldHnvckBie3OjeR?= NF7kUFMyKGi{ NUOxZVZlUW6qaXLpeIlwdiCxZjDoeY1idiCVR1zUNUBmgHC{ZYPz[YQhcW5iQ1jPJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiCdMUTDYWFOTyC3cIThb4Uh[W[2ZYKgNUBpeiCkeTDtbYNzd2KndHGgZ492dnSrbnegcYV1cG:mLDDFR|UxKD1iMD64OkDPxE1w Ml;lQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{MU[1OlAoRjJ7MkG2OVYxRC:jPh?=
CHO MkT0SpVv[3Srb36gZZN{[Xl? MVSxJIhz M{\SU2lvcGmkaYTpc44hd2ZiZoXscE1t\W6pdHigbJVu[W5iU1fMWFIh\XiycnXzd4VlKGmwIFPIU{Bk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCdMUTDYU1u\XSqeXygZYxxcGFvRD3ncJVkd3C7cnHuc5Nq\GVidYD0ZYtmKGGodHXyJFEhcHJiYomgcIlyfWmmIIPjbY51cWyuYYTpc44h[2:3boTpcochdWW2aH;kMEBKSzVyIE2gNE4xODFyNTFOwG0v M{\WclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7N{[0O|QzLz5{OUe2OFc1OjxxYU6=
HEK293 NILheYJHfW6ldHnvckBie3OjeR?= NXzTXo8yOTBibXnudy=> NETsW2xKdmirYnn0bY9vKG: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=> NI[0NXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUm1OFY5Oid-Mkm5OVQ3QDJ:L3G+
HEK293 NEHLdHlHfW6ldHnvckBie3OjeR?= MnXtNVAhdWmwcx?= MnzqTY5pcWKrdHnvckBw\iCqdX3hckBUT0yWMTDlfJBz\XO|ZXSgbY4hUEWNMkmzJINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKFtzNFPdMWFOTyC3cIThb4UheHKnaX7jeYJifGWmIH\vdkAyOCCvaX7zJIZwdGyxd3XkJIJ6KFtzNFPdMWFOTyCjZHTpeIlwdiCjbnSgcYVie3W{ZXSgZYZ1\XJiMjDodpMh[nlibHnxeYllKHOlaX70bYxt[XSrb36gZ492dnSrbnegcYV1cG:mLDDJR|UxKD1iMT64N{DPxE1w MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTl3NE[4Nkc,Ojl7NUS2PFI9N2F-
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

Solubility (25°C)

In vitro

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

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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