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 32 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 M4O5NVExKHWP NVOwU3NWOjBiaILz MkXmRYN1cX[jdHnvckBw\iCqdX3hckBNYFKjbIDoZUBmgHC{ZYPz[YQhcW5iSFXLNlk{KGOnbHzzJINwNWW6cILld5NqdmdiaIXtZY4hWliUYXzwbIEh[XRiMUCgeW0h[W[2ZYKgNlAhcHK|IHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigQ>? MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDByNkmwPUc,OjhyME[5NFk9N2F-
HEK293 Mlr5NVAhfU1? M3TwR|IxKGi{cx?= M4TTfGFkfGm4YYTpc44hd2ZicnH0JGxZWmKndHGg[ZhxemW|c3XkJIlvKEiHS{K5N{Bk\WyuczDjc{1mgHC{ZYPzbY5oKGi3bXHuJHJZWmGucHjhJIF1KDFyIIXNJIFnfGW{IEKwJIhzeyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZk> M4nrOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MEC2PVA6Lz5{OECwOlkxQTxxYU6=
THP1 M2f1N2Z2dmO2aX;uJIF{e2G7 NF;YeG1KdmS3Y4Tpc44hd2ZiY3jvcIV{fGW{b3yg[YZndHW6IHnuJHRJWDFiY3XscJMtKEWFNUCgQUAxNjBzIN88UU4> NWnGd|ZFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe1PFc2PzNpPkG3OVg4PTd|PD;hQi=>
THP1 NWS4[Vh{TnWwY4Tpc44h[XO|YYm= MkHSNVghcHK| MXrJcoR2[3Srb36gc4Yh[2ixbHXzeIVzd2xiZX\mcJV5KGmwIGTIVFEh[2WubIOgZYZ1\XJiMUigbJJ{NCCHQ{WwJF0hOC5yMTFOwG0v M4XIVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NEG2OVIyLz5zN{SxOlUzOTxxYU6=
COS7 MoTCSpVv[3Srb36gZZN{[Xl? NV61WFdTOTZiaILz M3i3emFod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gUHhT[mW2YTDy[YNmeHSxcjD0doFve2[nY4Tl[EBqdiCFT2O3JINmdGy|IHHmeIVzKDF4IHjyd{BjgSC{ZYDvdpRmeiC2cnHud4FkfGm4YYTpc44h[XO|YYmsJGVEPTBiPTCwMlAyPSEQvF2u M{PaZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NUi3OVc{Lz5zN{W4O|U4OzxxYU6=
COS7 NHzwdHlHfW6ldHnvckBie3OjeR?= MmDVRYN1cX[jdHnvckBw\iCOWGLi[ZRiKGOxLYTyZY5{\mWldHXkJIlvKEORU{egZ4VtdHNid3n0bEBTYFKjbIDoZUBjgSC{ZYDvdpRmeiC2cnHud4FkfGm4YYTpc44h[XO|YYmsJGVEPTBiPTCwMlAyPSEQvF2u NHThNmg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{SxOlUzOSd-MUe0NVY2OjF:L3G+
THP1 NYTkSIVlSW62aXnu[oxidW2jdH;yfUBie3OjeR?= NELj[pk3KGi{cx?= M1HMS2FvfGmrbn\sZY1u[XSxcomgZYN1cX[rdImgZYdicW6|dDDoeY1idiCWSGCxJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiTGDTMZN1cW23bHH0[YQhUUx4IIDyc4R2[3Srb36gZYZ1\XJiNjDodpMh[nliRVzJV2EtKEmFNUCgQUAxNjB{IN88UU4> NXLveYdkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi4NFA4PjdpPkG4PFAxPzZ5PD;hQi=>
THP1 M4CzfGZ2dmO2aX;uJIF{e2G7 MmS3RYdwdmm|dDDhZ5Rqfmm2eTDheEBISUxvbHnub4VlKGi3bXHuJGxZWmKndHGg[ZhxemW|c3XkJIlvKFSKUEGgZ4VtdHNiYYPz[ZN{\WRiYYOgd5RqdXWuYYTpc44hd2ZiY3:tZYN1cX[jdH;yJJJm[3K3aYTt[Y51KGK7IF\SSXQh[XO|YYmsJGVEPTBiPTCwMlAzPyEQvF2u M3nON|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5Nk[1PFk4Lz5zN{[2OVg6PzxxYU6=
RAW264.7 MlXlSpVv[3Srb36gZZN{[Xl? NV:yNJpvOjRiaILz Mm\kTY5lfWO2aX;uJI9nKFt|SG3jbI9t\XO2ZYLvcEBm\m[udYigbY4hdW:3c3WgVmFYOjZ2LkegZ4VtdHNibH;h[IVlKHerdHigZYNmfHmuYYTl[E1NTExiYX\0[ZIhOjRiaILzMEBGSzVyIE2gNE4xOjlizszNMi=> M1:wfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7N{G3N|A1Lz5zOUexO|MxPDxxYU6=
THP1 Mk\jSpVv[3Srb36gZZN{[Xl? Mo\HV5RqdXWuYYTpc44hd2ZiW{PIYYNpd2ync4Tldo9tKGWoZnz1fEBqdiCqdX3hckBVUFBzIH\vZY0h[2WubIOgcI9i\GWmIIfpeIgh[WNvTFTMMEBGSzVyIE2gNE4xOzFizszNMi=> MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDl5M{K4PEc,OTh7N{OyPFg9N2F-
CV1 Mn64SpVv[3Srb36gZZN{[Xl? M{fFSmFvfGGpb37pd5Qh[WO2aY\peJkh[XRiTGjSZoV1[SCuaXfhcoQh[mmwZHnu[{Bld22jaX6gZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDUNVMyPy2rbnT1Z4VlKHS{YX7zZ5JqeHSrb37hcEBi[3Srdnn0fUBqdiCjZoLpZ4FvKGe{ZXXuJI1wdmuneTDDWlEh[2WubIOgZ48ufHKjboPm[YN1\WRid3n0bEBI[Wx2LWPSR|Eh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDhd5NigSxiSVO1NEA:KDBwMEO5PFEh|ryPLh?= M1yzUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyM{S1NVAzLz5{MEO0OVExOjxxYU6=
THP1 NHT2fGdHfW6ldHnvckBie3OjeR?= NGjDNFRC\2:waYP0JIFkfGm4aYT5JIF1KEeDTD3sbY5s\WRiaIXtZY4hVFiUYXzwbIEh\XiycnXzd4VlKGmwIGTIVFEh[2WubIOgZZN{\XO|ZXSgZZMhe3SrbYXsZZRqd25ib3[gZ49i[3SrdnH0c5IhemWlcoXpeI1mdnRiYomgSnJGXCCjc4PhfUwhTUN3MDC9JFAvODl5IN88UU4> MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzZ4NUi5O{c,OTd4NkW4PVc9N2F-
CV1 NILLVFRHfW6ldHnvckBie3OjeR?= NVvqfpl1SW62YXfvcol{fCCjY4Tpeol1gSCjdDDMXHJidHCqYTDsbYdidmRiYnnu[Ilv\yCmb33hbY4h[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBVOTNzNz3pcoR2[2WmIITyZY5{[3KrcITpc45idCCjY4Tpeol1gSCrbjDh[pJq[2GwIHfy[YVvKG2xbnvlfUBEXjFiY3XscJMh[29vdILhcpNn\WO2ZXSge4l1cCCJYXy0MXNTSzFiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBie3OjeTygTWM2OCB;IECuNUDPxE1w NXXo[4RoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCzOFUyODJpPkKwN|Q2OTB{PD;hQi=>
SH-SY5Y Mn;xSpVv[3Srb36gZZN{[Xl? NGjXTlYzPCCqcoO= MkX3RYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDMXHJj\XSjIHX4dJJme3OnZDDpckBpfW2jbjDTTE1UYTW\IHPlcIx{KGOxLYTyZY5{\mWldHXkJJdqfGhiR3HsOE1NSkRiYX\0[ZIhOjRiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygSWM2OCB;IECuNVMh|ryPLh?= MlSzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl{NkS0PFEoRjF7Mk[0OFgyRC:jPh?=
HepG2 NYnVS2xbTnWwY4Tpc44h[XO|YYm= Mnv4SYZn\WO2IH;uJHNTTUKSMXOg[4Vv\SCneIDy[ZN{cW:wIHnuJIh2dWGwIFjldGczKGOnbHzzMEBGSzVyIE2gNE4zOSEQvF2u MlrIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh7N{OyPFgoRjF6OUezNlg5RC:jPh?=
HuH7 MnvnSpVv[3Srb36gZZN{[Xl? NYXNcIlqSWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBz\WOxbXLpcoFvfCCOWGLi[ZRiKGyrZ3Hu[EBjcW6maX7nJIRwdWGrbjDpckBpfW2jbjDIeWg4KGOnbHzzJINwNXS{YX7z[oVkfGWmIIfpeIgh\nW|ZXSgS4FtPC2GQlSgZpkhfHKjboPhZ5RqfmG2aX;uJIF{e2G7LDDFR|UxKD1iMD6zNUDPxE1w MojsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh7N{OyPFgoRjF6OUezNlg5RC:jPh?=
SH-SY5Y MUXGeY5kfGmxbjDhd5NigQ>? NXfRUYlJOjRiaILz MkfERYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDMXHJidHCqYTDlfJBz\XO|ZXSgbY4hcHWvYX6gV2guW1l3WTDj[YxteyClbz30doFve2[nY4Tl[EB4cXSqIFfhcFQuVEKGIHHmeIVzKDJ2IHjyd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGVEPTBiPTCwMlMyKM7:TT6= NYXQZ292RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmyOlQ1QDFpPkG5NlY1PDhzPD;hQi=>
CHO M1Wxe2Z2dmO2aX;uJIF{e2G7 MkfmRYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDMXHIh[mW2YTDy[YNmeHSxcjDlfJBz\XO|ZXSgbY4hS0iRIHPlcIx{KGK7IILldI9zfGW{IHHzd4F6NCCHQ{WwJF0hOC52MTFOwG0v NF7vOWM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{CzOFEyQSd-MUewN|QyOTl:L3G+
CHOK1 NEG5dIVHfW6ldHnvckBie3OjeR?= NEfadGUzPCCqcoO= NUPCVXN3SWexbnnzeEBi[3Srdnn0fUBifCCJYXy0MZRi\2enZDDMXHJj\XSjIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJGNJV0tzIHPlcIx{KGGodHXyJFI1KGi{czDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFXDOVAhRSByLkSyJO69VS5? MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ5N{[2OEc,OjV4N{e2OlQ9N2F-
THP1 NYP0O5dSTnWwY4Tpc44h[XO|YYm= M2jn[mVn\mWldDDvckBCSkODMTDn[Y5mKGW6cILld5Nqd25iaX6gbJVu[W5iZHnm[oVz\W62aXH0[YQhXEiSMTDj[YxteyxiRVO1NEA:KDBwNEO0JO69VS5? NEDaVoU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEm3N|I5QCd-MUi5O|MzQDh:L3G+
CV1 M{P2TWZ2dmO2aX;uJIF{e2G7 NYf6d5dySWexbnnzeEBi[3Srdnn0fUBifCCOWGLi[ZRiKGyrZ3Hu[EBjcW6maX7nJIRwdWGrbj3t[YRq[XSnZDD0doFve2O{aYD0bY9v[WxiYXP0bZZqfHliaX6gZYZzcWOjbjDndoVmdiCvb37r[ZkhS1ZzIHPlcIx{KGOxLYTyZY5{\mWldHXkJJdqfGhiR3HsOE1UWkNzIHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh[XO|YYmsJGVEPTBiPTCwMlUxOTF7IN88UU4> NE\OcVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEO0OVExOid-MkCzOFUyODJ:L3G+
HuH7 NHS3VIRHfW6ldHnvckBie3OjeR?= NGnxbGRC\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJJJm[2:vYnnuZY51KEy[UnHsdIhiKGyrZ3Hu[EBjcW6maX7nJIRwdWGrbjDpckBpfW2jbjDIeWg4KGOnbHzzJINwNXS{YX7z[oVkfGWmIIfpeIgh\nW|ZXSgS4FtPC2GQlSgZpkhfHKjboPhZ5RqfmG2aX;uJIF{e2G7LDDFR|UxKD1iMD62OkDPxE1w NE\UfW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEm3N|I5QCd-MUi5O|MzQDh:L3G+
CV1 M3rST2Z2dmO2aX;uJIF{e2G7 MlT1RYdwdmm|dDDhZ5Rqfmm2eTDheEBNYFKjbIDoZUBtcWejbnSgZolv\GmwZzDkc41icW5vbXXkbYF1\WRidILhcpNkemmydHnvcoFtKGGldHn2bZR6KGmwIHHmdolk[W5iZ4Ll[Y4hdW:wa3X5JGNXOSClZXzsd{Bkdy22cnHud4Zm[3SnZDD3bZRpKEejbEStV3JEOSCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIF{e2G7LDDFR|UxKD1iMD63PVQ{OyEQvF2u NYHIcpFGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCzOFUyODJpPkKwN|Q2OTB{PD;hQi=>
CHOK1 NGnweXpHfW6ldHnvckBie3OjeR?= NIHk[4szPCCqcoO= MnfCRYdwdmm|dDDhZ5Rqfmm2eTDheEBI[Wx2LYTh[4dm\CCOWGLhcJBp[SBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDDTG9MOSClZXzsd{Bi\nSncjCyOEBpenNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwJF0hOS5|IN88UU4> NUHwXHZyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2O|c3PjRpPkK1Olc4PjZ2PD;hQi=>
HepG2 M1TyNGZ2dmO2aX;uJIF{e2G7 NGXESVlG\m[nY4Sgc44hfHKrZ3z5Z4VzcWSnIHHjZ5VufWyjdHnvckBqdiCqdX3hckBJ\XCJMjDj[YxteyxiRVO1NEA:KDJwMECyJO69VS5? MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDl5M{K4PEc,OTh7N{OyPFg9N2F-
HepG2 MoLYSpVv[3Srb36gZZN{[Xl? NFzXdXg2ODBibl2= NWDWd|lTUW6qaXLpeIlwdiCxZjCyMUg{NSh|LTioNk1kcGyxcn:tN{0pfHKrZnz1c5JwdWW2aInsLYJmdnq7bDmoNkwzNWSrcHjlcplt\XSqeXypZY1qdm9rcILvdI95gSmyaHXufYwq[WOndHnjJIFkcWRvaX7keYNm\CC|cnXidFFkKG2UTlGg[ZhxemW|c3nvckBqdiCqdX3hckBJ\XCJMjDj[YxteyCjdDC1NFAhdk1? NFTkSnk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEiwNFc3Pyd-MUi4NFA4Pjd:L3G+
HepG2 NHHjUJpHfW6ldHnvckBie3OjeR?= MWq1NFAhdk1? M1LXbWlvcGmkaYTpc44hd2ZiMj2oN{0pOy1qKEKtZ4htd3KxLUOtLJRzcW[udX;yc41mfGi7bDni[Y57gWxrKEKsNk1lcXCqZX75cIV1cHmuKXHtbY5wMXC{b4DvfJkqeGinbonsLYFk\XSrYzDhZ4llNWmwZIXj[YQh\mG|IH3SUmEh\XiycnXzd4lwdiCrbjDoeY1idiCKZYDHNkBk\WyuczDheEA2ODBibl2= NX\yfIRJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi4NFA4PjdpPkG4PFAxPzZ5PD;hQi=>
RAW264.7 NXrLVmQ4TnWwY4Tpc44h[XO|YYm= MnvTNUB2VQ>? MnzqVoVlfWO2aX;uJI9nKEySUz3zeIlufWyjdHXkJIlPV1NiZ3Xu[UBmgHC{ZYPzbY9vKGmwIH3veZNmKFKDV{K2OE44KGOnbHzzJIV5eHKnc4PpcochVFiUYXzwbIEh[XRiMTD1UUBjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYm= MlvYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh6MEC3OlcoRjF6OECwO|Y4RC:jPh?=
RAW264.7 NV7wOlE5TnWwY4Tpc44h[XO|YYm= MVyxJJVO MlPxTY5pcWKrdHnvckBw\iCOUGOtd5RqdXWuYYTl[EBvfWOuZXHyJINwNXKncILld5NweiC{ZXzlZZNmKG[{b32gbW5QWyCycn;tc5RmeiCrbjDtc5V{\SCUQWeyOlQvPyClZXzsd{BifCBzIIXNJIJ6KFKWLWDDVi=> MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDhyMEe2O{c,OTh6MEC3Olc9N2F-
HeLa NUjoV4FJTnWwY4Tpc44h[XO|YYm= M2\CUFEhfU1? NI[4dFVKdmS3Y4Tpc44hd2ZiTGjSZoV1[SCVVV3PfYxifGmxbjDifUBUXU2RMjDpckBpfW2jbjDI[WxiKGOnbHzzJIF1KDFidV2gZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| NFX6dGg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEiwNFc3Pyd-MUi4NFA4Pjd:L3G+
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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.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 16 mg/mL warmed
(25.86 mM)
Water Insoluble
Ethanol Insoluble

* 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 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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