GW3965 HCl

Catalog No.S2630

For research use only.

GW3965 HCl is a potent, selective LXR agonist for hLXRα and hLXRβ with EC50 of 190 and 30 nM in cell-free assays, respectively.

GW3965 HCl Chemical Structure

CAS No. 405911-17-3

Selleck's GW3965 HCl has been cited by 34 publications

Purity & Quality Control

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Biological Activity

Description GW3965 HCl is a potent, selective LXR agonist for hLXRα and hLXRβ with EC50 of 190 and 30 nM in cell-free assays, respectively.
Targets
hLXRβ [1]
(Cell-free assay)
LXRα/SRC1 LiSA [1]
(Cell-free assay)
hLXRα [1]
(Cell-free assay)
30 nM(EC50) 125 nM(EC50) 190 nM(EC50)
In vitro

GW3965 recruits the steroid receptor coactivator 1 to human LXRα with EC50 of 125 nM in a cell-free ligand-sensing assay. [1] GW3965 shows a potent antagonistic activity against hLXRα and hLXRβ in cell-based assays with EC50 of 190 nM and 30 nM, respectively. Besides, GW3965 also sows excellent selectivity over other nuclear receptors. [1] In human islets, GW3965 (1 μM) reduces expression of selected pro-inflammatory cytokines including IL-8, monocyte chemotactic protein-1 and tissue factor. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 M1TyWlExKHWP MVOyNEBpenN? M3\5RmFkfGm4YYTpc44hd2ZiaIXtZY4hVFiUYXzwbIEh\XiycnXzd4VlKGmwIFjFT|I6OyClZXzsd{Bkdy2neIDy[ZN{cW6pIHj1cYFvKFK[UnHsdIhiKGG2IEGwJJVOKGGodHXyJFIxKGi{czDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[Xl? NIn0PGQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OECwOlkxQSd-MkiwNFY6ODl:L3G+
HEK293 MU[xNEB2VQ>? NV7nZ4ZsOjBiaILz NILPPYhC[3SrdnH0bY9vKG:oIILheEBNYFKkZYThJIV5eHKnc4Pl[EBqdiCKRVuyPVMh[2WubIOgZ48u\XiycnXzd4lv\yCqdX3hckBTYFKjbIDoZUBifCBzMDD1UUBi\nSncjCyNEBpenNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6 MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDByNkmwPUc,OjhyME[5NFk9N2F-
THP1 NYThWo5XTnWwY4Tpc44h[XO|YYm= MXzJcoR2[3Srb36gc4Yh[2ixbHXzeIVzd2xiZX\mcJV5KGmwIGTIVFEh[2WubIOsJGVEPTBiPTCwMlAyKM7:TT6= M1uzeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NUi3OVc{Lz5zN{W4O|U4OzxxYU6=
THP1 M3y1fWZ2dmO2aX;uJIF{e2G7 MnH0NVghcHK| M{THNGlv\HWldHnvckBw\iClaH;s[ZN1\XKxbDDl[oZtfXhiaX6gWGhROSClZXzsd{Bi\nSncjCxPEBpenNuIFXDOVAhRSByLkCxJO69VS5? NI\1OXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{SxOlUzOSd-MUe0NVY2OjF:L3G+
COS7 NFHLWndHfW6ldHnvckBie3OjeR?= NFHMXXAyPiCqcoO= NUf5bpo3SWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBNYFKkZYThJJJm[2WydH;yJJRz[W6|ZnXjeIVlKGmwIFPPV|ch[2WubIOgZYZ1\XJiMU[gbJJ{KGK7IILldI9zfGW{IITyZY5{[WO2aY\heIlwdiCjc4PhfUwhTUN3MDC9JFAvODF3IN88UU4> Mlr1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3OEe1O|MoRjF5NUi3OVc{RC:jPh?=
COS7 NXW2NHIyTnWwY4Tpc44h[XO|YYm= MXXBZ5RqfmG2aX;uJI9nKEy[UnLleIEh[29vdILhcpNn\WO2ZXSgbY4hS0:VNzDj[YxteyC5aYToJHJZWmGucHjhJIJ6KHKncH;yeIVzKHS{YX7zZYN1cX[jdHnvckBie3OjeTygSWM2OCB;IECuNFE2KM7:TT6= M1i0UlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NEG2OVIyLz5zN{SxOlUzOTxxYU6=
THP1 MnLYRY51cWmwZnzhcY1ifG:{eTDhd5NigQ>? MWS2JIhzew>? NIfCZ4RCdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVFjQNUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFzQV{1{fGmvdXzheIVlKEmONjDwdo9lfWO2aX;uJIFnfGW{IE[gbJJ{KGK7IFXMTXNCNCCLQ{WwJF0hOC5yMjFOwG0v MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDhyMEe2O{c,OTh6MEC3Olc9N2F-
THP1 NIDPempHfW6ldHnvckBie3OjeR?= NVTU[ZFPSWexbnnzeEBi[3Srdnn0fUBifCCJQVytcIlvc2WmIHj1cYFvKEy[UnLleIEh\XiycnXzd4VlKGmwIGTIVFEh[2WubIOgZZN{\XO|ZXSgZZMhe3SrbYXsZZRqd25ib3[gZ48u[WO2aY\heI9zKHKnY4L1bZRu\W62IHL5JGZTTVRiYYPzZZktKEWFNUCgQUAxNjB{NzFOwG0v MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzZ4NUi5O{c,OTd4NkW4PVc9N2F-
RAW264.7 NGLmOppHfW6ldHnvckBie3OjeR?= M3;oc|I1KGi{cx?= M3\OWmlv\HWldHnvckBw\iCdM1jdZ4hwdGW|dHXyc4wh\W[obIX4JIlvKG2xdYPlJHJCXzJ4ND63JINmdGy|IHzvZYRm\CC5aYToJIFk\XS7bHH0[YQuVESOIHHmeIVzKDJ2IHjyd{whTUN3MDC9JFAvODJ7IN88UU4> NHrVflc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUexO|MxPCd-MUm3NVc{ODR:L3G+
THP1 NVnv[Hd1TnWwY4Tpc44h[XO|YYm= NUi5bIFxW3SrbYXsZZRqd25ib3[gX|NJZWOqb3zld5Rmem:uIHXm[ox2gCCrbjDoeY1idiCWSGCxJIZw[W1iY3XscJMhdG:jZHXkJJdqfGhiYXOtUGRNNCCHQ{WwJF0hOC5yM{Gg{txONg>? NILTSJU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEm3N|I5QCd-MUi5O|MzQDh:L3G+
CV1 M1OwXmZ2dmO2aX;uJIF{e2G7 NEjwdZNCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IFzYVoJmfGFibHnnZY5lKGKrbnTpcoch\G:vYXnuJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gWFE{OTdvaX7keYNm\CC2cnHud4NzcXC2aX;uZYwh[WO2aY\peJkhcW5iYX\ybYNidiCpcnXlckBud26tZYmgR3YyKGOnbHzzJINwNXS{YX7z[oVkfGWmIIfpeIghT2GuND3TVmMyKGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKgZZN{[XluIFnDOVAhRSByLkCzPVgyKM7:TT6= MmnIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB|NEWxNFIoRjJyM{S1NVAzRC:jPh?=
THP1 MkfpSpVv[3Srb36gZZN{[Xl? MkDnRYdwdmm|dDDhZ5Rqfmm2eTDheEBISUxvbHnub4VlKGi3bXHuJGxZWmGucHjhJIV5eHKnc4Pl[EBqdiCWSGCxJINmdGy|IHHzd4V{e2WmIHHzJJN1cW23bHH0bY9vKG:oIHPvZYN1cX[jdH;yJJJm[3K3aYTt[Y51KGK7IF\SSXQh[XO|YYmsJGVEPTBiPTCwMlA6PyEQvF2u MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzZ4NUi5O{c,OTd4NkW4PVc9N2F-
CV1 MYHGeY5kfGmxbjDhd5NigQ>? NECzNI9CdnSjZ3;ubZN1KGGldHn2bZR6KGG2IFzYVoFteGijIHzp[4Fv\CCkaX7kbY5oKGSxbXHpckBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJHQyOzF5LXnu[JVk\WRidILhcpNkemmydHnvcoFtKGGldHn2bZR6KGmwIHHmdolk[W5iZ4Ll[Y4hdW:wa3X5JGNXOSClZXzsd{Bkdy22cnHud4Zm[3SnZDD3bZRpKEejbEStV3JEOSCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIF{e2G7LDDJR|UxKD1iMD6xJO69VS5? NXXTTGJYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCzOFUyODJpPkKwN|Q2OTB{PD;hQi=>
SH-SY5Y NXjKV3JUTnWwY4Tpc44h[XO|YYm= M{H4OVI1KGi{cx?= NGPhTYxC\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJGxZWmKndHGg[ZhxemW|c3XkJIlvKGi3bXHuJHNJNVO\NWmgZ4VtdHNiY3:teJJidnOoZXP0[YQhf2m2aDDHZYw1NUyERDDh[pRmeiB{NDDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBGSzVyIE2gNE4yOyEQvF2u MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTJ4NES4NUc,OTl{NkS0PFE9N2F-
HepG2 MkTGSpVv[3Srb36gZZN{[Xl? NFr6dGFG\m[nY4Sgc44hW1KHQmCxZ{Bo\W6nIHX4dJJme3Orb36gbY4hcHWvYX6gTIVxTzJiY3XscJMtKEWFNUCgQUAxNjJzIN88UU4> NGnoVpE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEm3N|I5QCd-MUi5O|MzQDh:L3G+
HuH7 NFi5bHBHfW6ldHnvckBie3OjeR?= NVT4eGdLSWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBz\WOxbXLpcoFvfCCOWGLi[ZRiKGyrZ3Hu[EBjcW6maX7nJIRwdWGrbjDpckBpfW2jbjDIeWg4KGOnbHzzJINwNXS{YX7z[oVkfGWmIIfpeIgh\nW|ZXSgS4FtPC2GQlSgZpkhfHKjboPhZ5RqfmG2aX;uJIF{e2G7LDDFR|UxKD1iMD6zNUDPxE1w M4nWO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OUezNlg5Lz5zOEm3N|I5QDxxYU6=
SH-SY5Y MkPWSpVv[3Srb36gZZN{[Xl? NXnRZWp2OjRiaILz M3HWfmFod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gUHhT[WyyaHGg[ZhxemW|c3XkJIlvKGi3bXHuJHNJNVO\NWmgZ4VtdHNiY3:teJJidnOoZXP0[YQhf2m2aDDHZYw1NUyERDDh[pRmeiB{NDDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBGSzVyIE2gNE4{OSEQvF2u NGDFWZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUK2OFQ5OSd-MUmyOlQ1QDF:L3G+
CHO MlnLSpVv[3Srb36gZZN{[Xl? MX3B[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIFzYVkBj\XSjIILlZ4VxfG:{IHX4dJJme3OnZDDpckBEUE9iY3XscJMh[nlicnXwc5J1\XJiYYPzZZktKEWFNUCgQUAxNjRzIN88UU4> MmTTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTdyM{SxNVkoRjF5MEO0NVE6RC:jPh?=
CHOK1 MWDGeY5kfGmxbjDhd5NigQ>? MlzMNlQhcHK| MmLVRYdwdmm|dDDhZ5Rqfmm2eTDheEBI[Wx2LYTh[4dm\CCOWGLi[ZRiKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIFPIU2syKGOnbHzzJIFnfGW{IEK0JIhzeyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEWFNUCgQUAxNjR{IN88UU4> MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ5N{[2OEc,OjV4N{e2OlQ9N2F-
THP1 M1ezcWZ2dmO2aX;uJIF{e2G7 NVjQ[nYzTW[oZXP0JI9vKEGEQ1GxJIdmdmViZYjwdoV{e2mxbjDpckBpfW2jbjDkbYZn\XKnboTpZZRm\CCWSGCxJINmdGy|LDDFR|UxKD1iMD60N|Qh|ryPLh?= NWfaXnZvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi5O|MzQDhpPkG4PVc{Ojh6PD;hQi=>
CV1 M2XucmZ2dmO2aX;uJIF{e2G7 MWrB[49vcXO2IHHjeIl3cXS7IHH0JGxZWmKndHGgcIlo[W6mIHLpcoRqdmdiZH;tZYlvNW2nZHnheIVlKHS{YX7zZ5JqeHSrb37hcEBi[3Srdnn0fUBqdiCjZoLpZ4FvKGe{ZXXuJI1wdmuneTDDWlEh[2WubIOgZ48ufHKjboPm[YN1\WRid3n0bEBI[Wx2LWPSR|Eh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDhd5NigSxiRVO1NEA:KDBwNUCxNVkh|ryPLh?= M2PBfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyM{S1NVAzLz5{MEO0OVExOjxxYU6=
HuH7 NVv4TFdnTnWwY4Tpc44h[XO|YYm= MYHB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIILlZ49u[mmwYX70JGxZWmGucHjhJIxq\2GwZDDibY5lcW6pIHTvcYFqdiCrbjDoeY1idiCKdVi3JINmdGy|IHPvMZRz[W6|ZnXjeIVlKHerdHig[pV{\WRiR3HsOE1FSkRiYomgeJJidnOjY4TpeoF1cW:wIHHzd4F6NCCHQ{WwJF0hOC54NjFOwG0v MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDl5M{K4PEc,OTh7N{OyPFg9N2F-
CV1 NF\GfW1HfW6ldHnvckBie3OjeR?= MVHB[49vcXO2IHHjeIl3cXS7IHH0JGxZWmGucHjhJIxq\2GwZDDibY5lcW6pIHTvcYFqdi2vZXTpZZRm\CC2cnHud4NzcXC2aX;uZYwh[WO2aY\peJkhcW5iYX\ybYNidiCpcnXlckBud26tZYmgR3YyKGOnbHzzJINwNXS{YX7z[oVkfGWmIIfpeIghT2GuND3TVmMyKGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKgZZN{[XluIFXDOVAhRSByLke5OFM{KM7:TT6= NGLubXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEO0OVExOid-MkCzOFUyODJ:L3G+
CHOK1 M4\ESWZ2dmO2aX;uJIF{e2G7 MXuyOEBpenN? Moq5RYdwdmm|dDDhZ5Rqfmm2eTDheEBI[Wx2LYTh[4dm\CCOWGLhcJBp[SBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDDTG9MOSClZXzsd{Bi\nSncjCyOEBpenNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwJF0hOS5|IN88UU4> MkjYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4N{e2OlQoRjJ3Nke3OlY1RC:jPh?=
HepG2 MlXJSpVv[3Srb36gZZN{[Xl? M17od2Vn\mWldDDvckB1emmpbInj[ZJq\GViYXPjeY12dGG2aX;uJIlvKGi3bXHuJGhmeEd{IHPlcIx{NCCHQ{WwJF0hOi5yMEKg{txONg>? NXjoO4hlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi5O|MzQDhpPkG4PVc{Ojh6PD;hQi=>
HepG2 MojLSpVv[3Srb36gZZN{[Xl? MYK1NFAhdk1? NIPEbG1KdmirYnn0bY9vKG:oIEKtLFMuMDNvKDiyMYNpdG:{bz2zMUh1emmobIXvdo9u\XSqeXypZoVvgnmuKTiyMFIu\GmyaHXufYxmfGi7bDnhcYlvdymycn;wc5h6MXCqZX75cEli[2W2aXOgZYNq\C2rbnT1Z4VlKHO{ZXLwNYMhdVKQQTDlfJBz\XO|aX;uJIlvKGi3bXHuJGhmeEd{IHPlcIx{KGG2IEWwNEBvVQ>? Mon3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh6MEC3OlcoRjF6OECwO|Y4RC:jPh?=
HepG2 MYfGeY5kfGmxbjDhd5NigQ>? MnvUOVAxKG6P MWnJcohq[mm2aX;uJI9nKDJvKEOtLFMuMCh{LXPocI9zdy1|LTj0dolndHWxcn;t[ZRpgWxrYnXufpltMSh{LEKt[IlxcGWweXzleIh6dCmjbXnuc{lxem:yb4j5LZBp\W67bDnhZ4V1cWNiYXPp[E1qdmS3Y3XkJIZieyCvUl7BJIV5eHKnc4Ppc44hcW5iaIXtZY4hUGWyR{KgZ4VtdHNiYYSgOVAxKG6P MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDhyMEe2O{c,OTh6MEC3Olc9N2F-
RAW264.7 MojBSpVv[3Srb36gZZN{[Xl? NUnUflJCOSC3TR?= Mo\UVoVlfWO2aX;uJI9nKEySUz3zeIlufWyjdHXkJIlPV1NiZ3Xu[UBmgHC{ZYPzbY9vKGmwIH3veZNmKFKDV{K2OE44KGOnbHzzJIV5eHKnc4PpcochVFiUYXzwbIEh[XRiMTD1UUBjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYm= NHXwfGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEiwNFc3Pyd-MUi4NFA4Pjd:L3G+
RAW264.7 MWTGeY5kfGmxbjDhd5NigQ>? MWWxJJVO MVzJcohq[mm2aX;uJI9nKEySUz3zeIlufWyjdHXkJI52[2ynYYKgZ48uemWycnXzd49zKHKnbHXhd4Uh\nKxbTDpUm9UKHC{b33veIVzKGmwIH3veZNmKFKDV{K2OE44KGOnbHzzJIF1KDFidV2gZpkhWlRvUFPS MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDhyMEe2O{c,OTh6MEC3Olc9N2F-
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SK-N-SH MVLxTHRUKGG|c3H5 MVXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3TTEBk\Wyucx?= MkLpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
BT-12 NWTCOI45eUiWUzDhd5NigQ>? NH;uV|dyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStNVIh[2WubIO= MmT2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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Assay
Methods Test Index PMID
Western blot Skp2 / pEGFR / EGFR / pERK / ERK ; LXRα / LXRβ / ABCA1 / ABCG1 25184494 11604492
Immunofluorescence LAMP-1 / LDLR ; pRelA 23382078 26635040
Growth inhibition assay Cell viability 25184494
In vivo In mice, GW3965 at a dose of 10 mg/kg upregulates ABCA1 expression 8-fold and raises circulating levels of HDL by 30% with Cmax of 12.7 μg/mL and t1/2 of 2 hours. [1] GW3965 (10mg/kg) induces expression of ABCA1 and ABCG1 and shows potent antiatherogenic activity in both LDLR−/− and apoE−/− mice. [2] In male sprague-dawley rats, GW3965 reduces Ang II-mediated increases in blood pressure and decreases vascular Ang II receptor gene expression. [3] In Glioblastoma mouse model, GW3965 results in inducible degrader of LDLR-mediated LDLR degradation, increased expression of the ABCA1 cholesterol efflux transporter, and thus potently promotes tumor cell death. [5]

Protocol (from reference)

Animal Research:[1]
  • Animal Models: C57BL/6 mice
  • Dosages: ≤10 mg/kg
  • Administration: Administered via p.o.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 618.51
Formula

C33H31ClF3NO3.HCl

CAS No. 405911-17-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C(C=C1)C(CN(CCCOC2=CC=CC(=C2)CC(=O)O)CC3=C(C(=CC=C3)C(F)(F)F)Cl)C4=CC=CC=C4.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

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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Frequently Asked Questions

Question 1:
How to formulate the compound for mouse in vivo experiment?

Answer:
S2630 GW3965 HCl can be dissolved in 2% DMSO/30% PEG 300/dd H2O at 10 mg/mL as a homogeneous suspension. This vehicle is suitable for oral gavage to mice.

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