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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C33H31ClF3NO3.HCl |
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分子量 | 618.51 | CAS No. | 405911-17-3 | |
Solubility (25°C)* | 体外 | DMSO | 124 mg/mL warmed with 50ºC water bath (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. |
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. |
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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] |
細胞アッセイ | 細胞株 | BMDMs |
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濃度 | 3 μM | |
反応時間 | ||
実験の流れ | Cells were treated with various concentrations of GW3965. |
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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. |
, , 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]
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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。