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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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G407795-1ml | 1ml | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $209.90 |
FXR Agonists
Specifications & Purity | 10mM in DMSO |
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Storage Temp | Store at -80°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Product Description | Information GW4064 GW4064 is an agonist of farnesoid X receptor (FXR) with EC50 of 65 nM in CV1 cell line and displays no activity at other nuclear receptors at concentrations up to 1 μM. GW4064 stimulates autophagy in MCF-7 cells. GW 4064 is a full agonist with EC50 values of 80 and 90 nM, respectively, in CV-1 cells transfected with mouse and human FXR expression vectors and an established reporter gene. There is no activity of GW 4064 on other nuclear receptors, including the retinoic acid receptor, at concentrations up to 1 μM. Thus, GW 4064 is a potent and selective nonsteroidal FXR agonist. In vivo Pharmacokinetic analysis in rats shows that GW 4064 possesses an oral bioavailability of 10% with a t1/2 = 3.5 h. Fisher rats are dosed with GW 4064 by oral gavage. After 7 days, a dose-dependent lowering of serum triglycerides is observed in the rats receiving GW 4064, with an ED50 = 20 mg/kg. cell lines:A2780 cells Concentrations: Incubation Time: Powder Purity:≥99% |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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Canonical SMILES | CC(C)C1=C(COC2=CC(=C(C=C2)/C=C/C3=CC=CC(=C3)C(O)=O)Cl)C(=NO1)C4=C(Cl)C=CC=C4Cl |
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Molecular Weight | 542.84 |
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Solubility | Solubility (25°C) In vitro |
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1. Zhiyuan Meng, Sen Yan, Wei Sun, Jin Yan, Miaomiao Teng, Ming Jia, Sinuo Tian, Zhiqiang Zhou, Wentao Zhu. (2023) Chlorothalonil induces obesity in mice by regulating host gut microbiota and bile acids metabolism via FXR pathways. JOURNAL OF HAZARDOUS MATERIALS, 452 (131310). [PMID:37003002] |
1. Zhiyuan Meng, Sen Yan, Wei Sun, Jin Yan, Miaomiao Teng, Ming Jia, Sinuo Tian, Zhiqiang Zhou, Wentao Zhu. (2023) Chlorothalonil induces obesity in mice by regulating host gut microbiota and bile acids metabolism via FXR pathways. JOURNAL OF HAZARDOUS MATERIALS, 452 (131310). [PMID:37003002] |