GW3965 HCl 405911-17-3

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Molecular Weight: 618.51 GW3965 HCl is a potent, selective LXR agonist for hLXRα and hLXRβ with EC50 of 190 and 30 nM, respectively.


Biological Activity

Description	GW3965 HCl is a potent, selective LXR agonist for hLXRα and hLXRβ with EC50 of 190 and 30 nM, respectively.
Targets	hLXRβ [1]	LXRα/SRC1 LiSA [1]	hLXRα [1]
IC50	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]
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]
Features

Protocol(Only for Reference)


Animal Study: [1]

Animal Models	C57BL/6 mice
Formulation	GW3965 is dissolved in 0.5% Methyl Cellulose.
Dosages	≤10 mg/kg
Administration	Administered via p.o.

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

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

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)

1

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.





Chemical Information

Molecular Weight (MW)	618.51
Formula	C33H31ClF3NO3.HCl
CAS No.	405911-17-3

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms

Solubility (25°C) *	In vitro	DMSO	124 mg/mL (200.48 mM)
		Water	<1 mg/mL (
		Ethanol	<1 mg/mL (

Chemical Name	2-(3-(3-((2-chloro-3-(trifluoromethyl)benzyl)(2,2-diphenylethyl)amino)propoxy)phenyl)acetic acid hydrochloride

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Stock Solution (1ml DMSO)	1mM	10mM	20mM	30mM
Mass(mg)	0.61851	6.1851	12.3702	18.5553

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