An orally-active agonist of LXRα and LXRβ
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GW 3965 (hydrochloride)

Item No. 10054

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[3-[[[2-chloro-3-(trifluoromethyl)phenyl]methyl](2,2-diphenylethyl)amino]propoxy]-benzeneacetic acid, monohydrochloride
CAS Number
405911-17-3
Molecular Formula
C33H31ClF3NO3 • HCl
Formula Weight
618.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS(pH 7.2) (1:4): 0.2 mg/mlEthanol: 2 mg/ml
λmax
204, 272 nm
SMILES
OC(CC1=CC(OCCCN(CC2=C(Cl)C(C(F)(F)F)=CC=C2)CC(C3=CC=CC=C3)C4=CC=CC=C4)=CC=C1)=O.Cl
InChi Code
InChI=1S/C33H31ClF3NO3.ClH/c34-32-27(15-8-17-30(32)33(35,36)37)22-38(18-9-19-41-28-16-7-10-24(20-28)21-31(39)40)23-29(25-11-3-1-4-12-25)26-13-5-2-6-14-26;/h1-8,10-17,20,29H,9,18-19,21-23H2,(H,39,40);1H
InChi Key
NMPUWJFHNOUNQU-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $28

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    5 mg

    $76

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    10 mg

    $125

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    50 mg

    $275

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    Product Description

    GW 3965 is an orally-active agonist of LXRα and LXRβ, activating the human isoforms with EC50 values of 190 and 30 nM, respectively.1 It alters LXR-regulated gene expression in mice and rats, affecting pathways related to glucose and lipid metabolism.1,2,3 GW 3965 also affects inflammation and pressor responses through LXRα and LXRβ.4,5,6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Collins, J.L., Fivush, A.M., Watson, M.A., et al. Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines. J. Med. Chem. 45, 1963-1966 (2002).

    2. Joseph, S.B., McKilligin, E., Pei, L., et al. Synthetic LXR ligand inhibits the development of atherosclerosis in mice. Proc. Natl. Acad. Sci. USA 99(11), 7604-7609 (2002).

    3. Hazra, S., Rasheed, A., Bhatwadekar, A., et al. Liver X receptor modulates diabetic retinopathy outcome in a mouse model of streptozotocin-induced diabetes. Diabetes 61(12), 3270-3279 (2012).

    4. Joseph, S.B., Castrillo, A., Lafitte, B.A., et al. Reciprocal regulation of inflammation and lipid metabolism by liver X receptors. Nat. Med. 9(2), 213-219 (2003).

    5. Leik, C.E., Carson, N.L., Hennan, J.K., et al. GW3965, a synthetic liver X receptor (LXR) agonist, reduces angiotensin II-mediated pressor responses in Sprague-Dawley rats. Br. J. Pharmacol. 151(4), 450-456 (2007).

    6. Archer, A., Stolarczyk, É., Doria, M.L., et al. LXR activation by GW3965 alters fat tissue distribution and adipose tissue inflammation in ob/ob female mice. J. Lipid Res. 54(5), 1300-1311 (2013).