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GW4064 - 10mM in DMSO, high purity , CAS No.278779-30-9(DMSO), Agonist of Farnesoid X receptor

Item Number
G407795
Grouped product items
SKUSizeAvailabilityPrice Qty
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

Basic Description

Specifications & PurityMoligand™, 10mM in DMSO
Biochemical and Physiological MechanismsGW4064 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.
Storage TempStore at -80°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeAGONIST
Mechanism of actionAgonist of Farnesoid X receptor
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.
In vitro

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 Data

cell lines:A2780 cells

Concentrations:

Incubation Time:

Powder Purity:≥99%

Associated Targets(Human)

NR1H4 Tclin Bile acid receptor (40 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

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
Molecular Weight 542.84

Certificates(CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
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Chemical and Physical Properties

SolubilitySolubility (25°C) In vitro      

Related Documents

Citations of This Product(1)

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] [10.1016/j.jhazmat.2023.131310]

References

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] [10.1016/j.jhazmat.2023.131310]

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