| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
GW4064 (GW-4064) is a novel, potent and selective agonist of farnesoid X receptor (FXR) (EC50 of 65 nM in CV1 cell line) with potential usefulness in the treatment of cholestatic liver disease. It displays no activity at other nuclear receptors, including the retinoic acid receptor, at concentrations up to 1 μM. GW-4064 upregulates adipokine expression in preadipocytes and HepG2 cells. GW4064 could reduce induction of proinflammatory cytokines by LPS in vitro. GW4064 shows beneficial effects on cholesterol and TG (triglycerides) in various animal species. GW4064 is found to lower serum TG levels in both the KK-Ay and ob/ob mice potently. In KK-Ay mice, a 1-week administration of GW4064 also significantly lowers VLDL secretion. GW4064 can also lower serum TGs in the SHP+/+ mice.
| ln Vitro |
GW4064 treatment (1, 2.5, 5, 10 μM) decreased cell lipid accumulation. In a dose-dependent way, GW4064 therapy dramatically reduced the levels of CD36 protein generated by oleic acid. When combined, these findings imply that long-term GW4064 therapy can prevent hepatic fat buildup by blocking Cd36 expression [2].
|
||
|---|---|---|---|
| ln Vivo |
In C57BL/6 mice, GW4064 prevents body weight increase brought on by high-fat (HFD) or high-fat, high-cholesterol diets. Reduced liver triglyceride and free fatty acid levels showed that GW4064 treatment dramatically prevented diet-induced hepatic steatosis in HFD mice. Without changing the expression of genes directly related to adipogenesis, GW4064 dramatically lowers the expression of the lipid transporter CD36. Treatment with GW4064 decreases inflammation in the liver while having no effect on white adipose tissue [2]. In rats treated with ANIT, therapy with GW4064 (30 mg/kg) led to a statistically significant reduction in serum ALT, AST, LDH, and ALP activity. The use of GW4064 also markedly lowered serum bile acid levels. Rats given GW4064 had lower bilirubin levels, although the difference was not statistically significant. Notably, TUDCA merely decreased LDH levels; GW4064 was more successful in lowering these liver damage markers [3].
|
||
| Animal Protocol |
|
||
| References |
[1]. Akwabi-Ameyaw A, et al.Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064. Bioorg Med Chem Lett, 2008, 18(15), 4339-4343.
[2]. Ma Y, et al. Synthetic FXR agonist GW4064 prevents diet-induced hepatic steatosis and resistance. Pharm Res. 2013 May;30(5):1447-57. [3]. Liu Y, et al. Hepatoprotection by the farnesoid X receptor agonist GW4064 in rat models of intra- and extrahepatic cholestasis. J Clin Invest. 2003 Dec;112(11):1678-87 |
| Molecular Formula |
C28H22CL3NO4
|
|
|---|---|---|
| Molecular Weight |
542.84
|
|
| CAS # |
278779-30-9
|
|
| Related CAS # |
278779-30-9;
|
|
| SMILES |
ClC1C([H])=C([H])C([H])=C(C=1C1C(C([H])([H])OC2C([H])=C([H])C(/C(/[H])=C(\[H])/C3C([H])=C([H])C([H])=C(C(=O)O[H])C=3[H])=C(C=2[H])Cl)=C(C([H])(C([H])([H])[H])C([H])([H])[H])ON=1)Cl
|
|
| Synonyms |
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
|
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8422 mL | 9.2108 mL | 18.4216 mL | |
| 5 mM | 0.3684 mL | 1.8422 mL | 3.6843 mL | |
| 10 mM | 0.1842 mL | 0.9211 mL | 1.8422 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA