GW3965 HCl

製品コードS2630 バッチS263005

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	50 mg/mL warmed with 50ºC water bath (80.83 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 is a potent, selective LXR agonist for hLXRα and hLXRβ with EC50 of 190 and 30 nM in cell-free assays, respectively.
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 C_max of 12.7 μg/mL and t_1/2 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]

製品説明

GW3965 HCl is a potent, selective LXR agonist for hLXRα and hLXRβ with EC50 of 190 and 30 nM in cell-free assays, respectively.

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 C_max of 12.7 μg/mL and t_1/2 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)

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

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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：

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
Activation of LXRs Reduces Oxysterol Lipotoxicity in RPE Cells by Promoting Mitochondrial Function [ Nutrients, 2022, 14(12)2473]	PubMed: 35745203
Activation of liver X receptors protects oligodendrocytes in CA3 of stress-induced mice [ Front Pharmacol, 2022, 13:936045]	PubMed: 35959443
Deficiency of proline/serine-rich coiled-coil protein 1 (PSRC1) accelerates trimethylamine N-oxide-induced atherosclerosis in ApoE-/- mice [ J Mol Cell Cardiol, 2022, 170:60-74]	PubMed: 35690006

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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