INT-767
- Product Name
- INT-767
- CAS No.
- 1000403-03-1
- Chemical Name
- INT-767
- Synonyms
- INT-767;INT-767 (INT767);Sodium (R)-3-[(3R,5S,6R,7R,8S,9S,10S,13R,14S,17R)-6-Ethyl-3,7-dihydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl]butyl Sulfate
- CBNumber
- CB33048660
- Molecular Formula
- C25H45NaO6S
- Formula Weight
- 496.68
- MOL File
- 1000403-03-1.mol
INT-767 Property
- storage temp.
- Store at -20°C
- solubility
- DMSO : ≥ 205.5 mg/mL (415.44 mM)
- form
- Solid
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- CS-5007
- Product name
- INT-767
- Purity
- >98.0%
- Packaging
- 5mg
- Price
- $900
- Updated
- 2021/12/16
- Product number
- orb611413
- Product name
- INT-767
- Packaging
- 5mg
- Price
- $1089.7
- Updated
- 2021/12/16
- Product number
- CS-5007
- Product name
- INT-767
- Purity
- >98.0%
- Packaging
- 10mg
- Price
- $1440
- Updated
- 2021/12/16
- Product number
- orb611413
- Product name
- INT-767
- Packaging
- 10mg
- Price
- $1771.4
- Updated
- 2021/12/16
- Product number
- orb611413
- Product name
- INT-767
- Packaging
- 25mg
- Price
- $3105.9
- Updated
- 2021/12/16
INT-767 Chemical Properties,Usage,Production
Description
INT-767 is a G-protein coupled/Farnesoid X-activated receptor agonist potentially for the treatment of hepatic fibrosis. INT-767 significantly improved serum liver enzymes, hepatic inflammation, and biliary fibrosis in Mdr2(-/-) mice. INT-767 significantly induced bile flow and biliary HCO?3- output, as well as gene expression of carbonic anhydrase 14, an important enzyme able to enhance HCO?3- transport, in an Fxr-dependent manner. In addition, INT-767 dramatically reduced bile acid synthesis via the induction of ileal Fgf15 and hepatic Shp gene expression, thus resulting in significantly reduced biliary bile acid output in Mdr2(-/-) mice.
Uses
INT-767 is a dual farnesoid X receptor (FXR)/TGR5 agonist with mean EC50s of 30 and 630 nM, respectively[1][2].
in vivo
INT-767 (10-20 mg/kg; i.p.; daily for 2 weeks) decreases plasma total cholesterol and triglyceride levels in db/m and db/db mice [2].
| Animal Model: | Male 8-week old C57BKS/J db/db mice, control nondiabetic db/m mice[2] |
| Dosage: | 10, 20 mg/kg |
| Administration: | Intraperitoneal injection; daily for 2 weeks |
| Result: | Decreased plasma total cholesterol and triglyceride levels. |
References
[1] Baghdasaryan A, et al. Dual farnesoid X receptor/TGR5 agonist INT-767 reduces liver injury in the Mdr2-/- (Abcb4-/-) mousecholangiopathy model by promoting biliary HCO3- output. Hepatology. 2011 Oct;54(4):1303-1312. DOI:10.1002/hep.24537
[2] Rizzo G, et al. Functional characterization of the semisynthetic bile acid derivative INT-767, a dual farnesoid X receptor andTGR5 agonist. Mol Pharmacol. 2010 Oct;78(4):617-630. DOI:10.1124/mol.110.064501
INT-767 Preparation Products And Raw materials
Raw materials
Preparation Products
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