[CAS NO. 405911-17-3] GW3965 HCl

Name: GW3965 HCl
Brand: Arctom Scientific
SKU: SLK-S2630

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PRODUCTS SPECIFICATIONS [405911-17-3]

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Catalog

SLK-S2630

Brand

Selleck

CAS

405911-17-3

DESCRIPTION [405911-17-3]

Overview

MDL	MFCD08276920
Molecular Weight	618.51
Molecular Formula	C33H31ClF3NO3.HCl
SMILES	O=C(O)CC1=CC=CC(OCCCN(CC2=CC=CC(C(F)(F)F)=C2Cl)CC(C3=CC=CC=C3)C4=CC=CC=C4)=C1.[H]Cl

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.6168 mL	8.0839 mL	16.1679 mL
5 mM	0.3234 mL	1.6168 mL	3.2336 mL
10 mM	0.1617 mL	0.8084 mL	1.6168 mL
50 mM	-	-	-

Description

GW3965 HCl is a potent, selective 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. 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. In human islets, GW3965 (1 μM) reduces expression of selected pro-inflammatory cytokines including IL-8, monocyte chemotactic protein-1 and tissue factor.

References

[1] Collins JL, et al. J Med Chem. 2002, 45(10), 1963-1966.
[2] Joseph SB, et al. Proc Natl Acad Sci U S A. 2002, 99(11), 7604-7609.
[3] Leik CE, et al. Br J Pharmacol. 2007, 151(4), 450-456.
[4] Scholz H, et al. Diabetologia. 2009, 52(7), 1352-1362.
[5] Guo D, et al. Cancer Discov. 2011, 1(5), 442-456.
[6] Di Conza G, et al. Nat Immunol. 2021 Nov;22(11):1403-1415.