GW3965 HCl

GW3965 HClは強力で、選択的で、経口で有効なLXR作用薬です。そして、それはLXRα/SRC1 LiSAとLXRα-GAL4でその力を示します。 EC50 がそれぞれ 125 nM と 190 nMです。

価格 在庫  
USD 122 あり
USD 189 あり
USD 302 あり
USD 718 あり

GW3965 HCl 化学構造
分子量: 618.51





  • Compare Liver X Receptor Inhibitors
    Liver X Receptor製品生物活性の比較
  • GW3965 HClのメカニズム



製品説明 GW3965 HClは強力で、選択的で、経口で有効なLXR作用薬です。そして、それはLXRα/SRC1 LiSAとLXRα-GAL4でその力を示します。 EC50 がそれぞれ 125 nM と 190 nMです。
IC50 125 nM [1] 190 nM [1] 30 nM [1]
In vitro試験 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
THP1 cells MUjGeY5kfGmxbjDhd5NigQ>? NYj4T3RCOThiaB?= M2nNUmlv\HWldHnvckBw\iClaH;s[ZN1\XKxbDDl[oZtfXhiaX6gWGhROSClZXzsd{Bi\nSncjCxPEBpenNuIFXDOVA:OC5yMTFOwG0> MoPhNVc1OTZ3MkG=
COS7 cells MVvGeY5kfGmxbjDhd5NigQ>? M2LBR2FkfGm4YYTpc44hd2ZiTGjSZoV1[SClbz30doFve2[nY4Tl[EBqdiCFT2O3JINmdGy|IIfpeIghWliUYXzwbIEh[nlicnXwc5J1\XJidILhcpNi[3SrdnH0bY9vKGG|c3H5MEBGSzVyPUCuNFE2KM7:TR?= MYmxO|QyPjV{MR?=
human THP1 cells NIiyUZpHfW6ldHnvckBie3OjeR?= M4HiNVYhcA>? NFj3UmZCdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVFjQNUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFzQV{1{fGmvdXzheIVlKEmONjDwdo9lfWO2aX;uJIFnfGW{IE[gbJJ{KGK7IFXMTXNCNCCLQ{WwQVAvODJizszN MYGxPFgxODd4Nx?=
mouse RAW264.7 cells NIn2dmJHfW6ldHnvckBie3OjeR?= NVnVbHhFOjRiaB?= MV;JcoR2[3Srb36gc4YhYzOKXXPoc4xme3Sncn;sJIVn\my3eDDpckBud3W|ZTDSRXczPjRwNzDj[YxteyCub3Hk[YQhf2m2aDDhZ4V1gWyjdHXkMWxFVCCjZoTldkAzPCCqcoOsJGVEPTB;MD6wNlkh|ryP NEPjNGgyQTdzN{OwOC=>
human SH-SY5Y cells NYTTZVRxTnWwY4Tpc44h[XO|YYm= M{jlTVI1KGh? MXHB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIFzYVoJmfGFiZYjwdoV{e2WmIHnuJIh2dWGwIGPIMXN[PVliY3XscJMh[29vdILhcpNn\WO2ZXSge4l1cCCJYXy0MWxDTCCjZoTldkAzPCCqcoOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxRTBwMUOg{txO NILRWIkyQTJ4NES4NS=>
human HepG2 cells Ml\USpVv[3Srb36gZZN{[Xl? M3;McGVn\mWldDDvckBUWkWEUEHjJIdmdmViZYjwdoV{e2mxbjDpckBpfW2jbjDI[ZBIOiClZXzsd{whTUN3ME2wMlIyKM7:TR?= M3\CclE5QTd|Mki4
human HuH7 cells M3jyUmZ2dmO2aX;uJIF{e2G7 MV\B[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIILlZ49u[mmwYX70JGxZWmKndHGgcIlo[W6mIHLpcoRqdmdiZH;tZYlvKGmwIHj1cYFvKEi3SEegZ4VtdHNiY3:teJJidnOoZXP0[YQhf2m2aDDmeZNm\CCJYXy0MWRDTCCkeTD0doFve2GldHn2ZZRqd25iYYPzZZktKEWFNUC9NE4{OSEQvF2= NIrOZ2IyQDl5M{K4PC=>
CHO cells MnPrSpVv[3Srb36gZZN{[Xl? M4XmVGFod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gUHhTKGKndHGgdoVk\XC2b4Kg[ZhxemW|c3XkJIlvKEOKTzDj[YxteyCkeTDy[ZBwenSncjDhd5NigSxiRVO1NF0xNjRzIN88US=> NEnoPGcyPzB|NEGxPS=>
CHOK1 cells MWTGeY5kfGmxbjDhd5NigQ>? MUOyOEBp NUPibHkxSWexbnnzeEBi[3Srdnn0fUBifCCJYXy0MZRi\2enZDDMXHJj\XSjIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJGNJV0tzIHPlcIx{KGGodHXyJFI1KGi{czDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFXDOVA:OC52MjFOwG0> Ml;wNlU3Pzd4NkS=
human primary hepatocytes M2C4NGZ2dmO2aX;uJIF{e2G7 MWSxJO69VQ>? NUWwXWJsUW6mdXP0bY9vKG:wIF\BV{Bo\W6nIHX4dJJme3Orb36gbY4hcHWvYX6gdJJqdWG{eTDo[ZBifG:leYTld{BifCBzIIXN NH;kZ2cyPzZ4NUi5Oy=>
human HeLa cells MljSSpVv[3Srb36gZZN{[Xl? MmfVNUDPxE1? M4\pNmlv\HWldHnvckBw\iCOWGLi[ZRiKFOXTV;5cIF1cW:wIHL5JHNWVU9{IHnuJIh2dWGwIFjlUIEh[2WubIOgZZQhOSC3TTDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? M{K3b|E5QDByN{[3

... Click to View More Cell Line Experimental Data

In vivo試験 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]

プロトコル (参考用のみ)

動物実験: [1]

動物モデル C57BL/6 mice
製剤 GW3965 is dissolved in 0.5% Methyl Cellulose.
投薬量 ≤10 mg/kg
投与方法 Administered via p.o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)



Download GW3965 HCl SDF
分子量 618.51


CAS No. 405911-17-3
保管 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 16 mg/mL warming (25.86 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo
* <1 mg/ml means slightly soluble or 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.
化学名 2-(3-(3-((2-chloro-3-(trifluoromethyl)benzyl)(2,2-diphenylethyl)amino)propoxy)phenyl)acetic acid hydrochloride

文献中の引用 (2)

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.



電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)


* 必須

Related 肝臓Xレセプター モジュレータ

  • SR9243

    SR9243 is a potent and selective LXR inverse agonist.

  • CB-839

    CB-839 is a potent, selective, and orally bioavailable glutaminase inhibitor with IC50 of 24 nM for recombinant human GAC. Phase 1.

  • GKT137831

    GKT137831 is a potent, dual NADPH oxidase NOX1/NOX4 inhibitor with Ki of 110 nM and 140 nM, respectively. Phase 2.

  • Obeticholic Acid

    Obeticholic Acid is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. Phase 3.

  • T0901317

    T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of about 50 nM and 5 μM, respectively.

  • H 89 2HCl

    H 89 2HClは一種の有効なPKA阻害剤で、無細胞試験でKi値が48 nMになって、PKAに作用する選択性がPKGに作用する選択性より10倍高くなって、PKC、MLCK、カルモジュリンキナーゼ (calmodulin kinase II)とカゼインキナーゼ(casein kinase I/II)に作用する選択性より500倍高くなります。

  • Puromycin 2HCl

  • Cyclosporin A

    Cyclosporin A is an antilymphocytic agent, competitively binds to and inhibits calcineurin.

  • Dexamethasone (DHAP)

    Dexamethasone (DHAP)は一種の有効な半合成の糖質コルチコイド(glucocorticoid)類ステロイド(steroid)薬で、一種のインターロイキン(interleukin )受容体調節剤ですし、抗炎と免疫抑制作用をしています。


Tags: GW3965 HClを買う | GW3965 HCl供給者 | GW3965 HClを購入する | GW3965 HCl費用 | GW3965 HCl生産者 | オーダーGW3965 HCl | GW3965 HCl代理店
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID