GW3965 Hydrochloride

製品コードS2630 バッチS263002

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₃₃H₃₁ClF₃NO₃.HCl
	分子量	618.51	CAS No.	405911-17-3
Solubility (25°C)*	体外	DMSO	124 mg/mL (200.48 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	GW3965 HClは、hLXRαおよびhLXRβに対する強力で選択的なLXRアゴニストであり、それぞれセルフリーアッセイにおいてEC50が190 nMおよび30 nMです。
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.
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 C_max of 12.7 μg/mL and t_1/2 of 2 hours. GW3965 (10mg/kg) induces expression of ABCA1 and ABCG1 and shows potent antiatherogenic activity in both LDLR−/− and apoE−/− mice. In male sprague-dawley rats, GW3965 reduces Ang II-mediated increases in blood pressure and decreases vascular Ang II receptor gene expression. 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.

製品説明

GW3965 HClは、hLXRαおよびhLXRβに対する強力で選択的なLXRアゴニストであり、それぞれセルフリーアッセイにおいてEC50が190 nMおよび30 nMです。

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.

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 C_max of 12.7 μg/mL and t_1/2 of 2 hours.

GW3965 (10mg/kg) induces expression of ABCA1 and ABCG1 and shows potent antiatherogenic activity in both LDLR−/− and apoE−/− mice.

In male sprague-dawley rats, GW3965 reduces Ang II-mediated increases in blood pressure and decreases vascular Ang II receptor gene expression.

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.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	BMDMs
	濃度	3 μM
	反応時間
	実験の流れ	Cells were treated with various concentrations of GW3965.
動物実験	動物モデル	C57BL/6 mice
	投薬量	≤10 mg/kg
	投与方法	Administered via p.o.

参考

https://pubmed.ncbi.nlm.nih.gov/11985463/
https://pubmed.ncbi.nlm.nih.gov/12032330/
https://pubmed.ncbi.nlm.nih.gov/17420776/

https://pubmed.ncbi.nlm.nih.gov/19415233/
https://pubmed.ncbi.nlm.nih.gov/22059152/
https://pubmed.ncbi.nlm.nih.gov/34686867/

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カスタマーフィードバック

: , , FEBS Lett, 2015, 589(1):52-8.

: Data from [Data independently produced by , , Arch Toxicol, 2017, 91(1):271-287]

: Data from [Data independently produced by , , Exp Neurol, 2018, 304:21-29]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

HDL Nanodiscs Loaded with Liver X Receptor Agonist Decreases Tumor Burden and Mediates Long-term Survival in Mouse Glioma Model [ Small, 2025, 21(20):e2307097]	PubMed: 40249282
Cholesterol Accumulation Enhances Cigarette Smoke-Induced Airway Epithelial Inflammation [ Int J Chron Obstruct Pulmon Dis, 2025, 20:411-423]	PubMed: 40008109
A multiparametric screen uncovers FDA-approved small molecules that potentiate the nuclear mechano-dysfunctions in ATR-defective cells [ Sci Rep, 2024, 14(1):30786]	PubMed: 39730498
Host-to-graft propagation of inoculated α-synuclein into transplanted human induced pluripotent stem cell-derived midbrain dopaminergic neurons [ Regen Ther, 2024, 25:229-237]	PubMed: 38283940
Restoration of lipid homeostasis between TG and PE by the LXRα-ATGL/EPT1 axis ameliorates hepatosteatosis [ Cell Death Dis, 2023, 14(2):85]	PubMed: 36746922
Activation of liver X receptors suppresses the abundance and osteoclastogenic potential of osteoclast precursors and periodontal bone loss [ Mol Oral Microbiol, 2023, 10.1111/omi.12447]	PubMed: 38108557
Expression and role of nicotinic acetylcholine receptors during midbrain dopaminergic neuron differentiation from human induced pluripotent stem cells [ Neuropsychopharmacol Rep, 2023, 10.1002/npr2.12361]	PubMed: 37366076
Oridonin alleviates hyperbilirubinemia through activating LXRα-UGT1A1 axis [ Pharmacol Res, 2022, 178:106188]	PubMed: 35338002
Integrated Analysis Highlights the Immunosuppressive Role of TREM2+ Macrophages in Hepatocellular Carcinoma [ Front Immunol, 2022, 13:848367]	PubMed: 35359989
Liver X receptor-agonist treatment rescues degeneration in a Drosophila model of hereditary spastic paraplegia [ Acta Neuropathol Commun, 2022, 10(1):40]	PubMed: 35346366

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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