Turofexorate isopropyl,英文名:3-(3,4-Difluorobenzoyl)-1,2,3,6-tetrahydro-1,1-dimethylazepino[4,5-b]indo
629664-81-9
Turofexorate isopropyl(3-(3,4-Difluorobenzoyl)-1,2,3,6-tetrahydro-1,1-dimethylazepino[4,5-b]indole-5-carboxylic acid 1-methylethyl ester)
CAS: 629664-81-9
化学式: C25H24F2N2O3
<"" ="xl" "">| Chinese name | Turofexorate isopropyl |
| English name | 3-(3,4-Difluorobenzoyl)-1,2,3,6-tetrahydro-1,1-dimethylazepino[4,5-b]indole-5-carboxylic acid 1-methylethyl ester |
| alias | tofen isopropyl ester 3- (3,4-difluorobenzoyl) -1,2,3,6-tetrahydro-1,1-dimethylazepine [4,5-B] indole-5-carboxylic acid 1-methylethyl ester 3- (3,4-Difluorobenzoyl) -1,2,3,6-tetrahydro-1,1-dimethylazepine [4,5-B] indole-5-carboxylate 1-methethyl ester (WAY-362450) |
| English alias | XL335 CS-899 Fxr 450 WAY-362450 WAY 362450 Turofexorate isopropyl TUROFEXORATE ISOPROPYL TUROFEXORATE ISOPROPYL Turofexorate isopropyl [usan] isopropyl 3-(3,4-difluorobenzoyl)-1,1-dimethyl-1,2,3,4,5,5a,6,10b-octahydroazepino[4,5-b]indole-5-carboxylate 3-(3,4-Difluorobenzoyl)-1,2,3,6-tetrahydro-1,1-dimethylazepino[4,5-b]indole-5-carboxylic acid 1-methylethyl ester |
| CAS | 629664-81-9 |
| chemical formula | C25H24F2N2O3 |
| molecular weight | 438.47 |
| density | 1.275 |
| Boiling Point | 617.3±55.0 °C(Predicted) |
| solubility | DMSO: 25 mg/ml (57.02 mm; requires ultrasound) |
| acidity coefficient | 16.49±0.60(Predicted) |
| storage conditions | room temp |
| appearance | powder |
| color | white to beige |
| target | FXR |
| in vitro study | WAY-362450 binds to the ligand-binding domain (LBD) of human FXR. WAY-362450 is mainly present in hydrophobic bags, and only a few polar molecules come into contact with WAY-362450. In promoter assays, WAY-362450 promoted transcription of human BSEP, human SHP, and mouse IBABP genes using reporter genes, with EC50 of 17, 230, and 33 nM, respectively. WAY-362450 significantly induced mRNAs encoding BSEP, SHP, and IBABP at 1 μM concentration, with 13-, 2-, and 20-fold effects in human cell culture, respectively. WAY-362450 inhibited interleukin-6-induced CRP expression in human Hep3B hepatoma cells at 1 μM concentration, and the inhibitory effect was attenuated when FXR was interfered with by short URL RNA. |
| in vivo research | WAY-362450 was administered intravenously or orally at a dose of 3 mg/kg with a durable half-life of 25 hours in rats, with moderate volume distribution, and a low clearance of 3.3 L/kg. WAY-362450 was administered orally to normal C57bl/6 mice at a dose of 10 mg/kg for 7 days and significantly reduced triglycerides to 62.0 ± 6.4 mg/dL and total cholesterol to 78.1 ± 5.0 mg/dL. WAY-362450 was administered intraperitoneally to wild-type C57BL/6 mice at doses of 1 and 3 mg/kg/day to LDLR WAY-362450 at a dose of 30 mg/kg/day for 4 days to attenuate lipopolysaccharide-induced serum amyloid P components and serum amyloid A3 mRNA levels in the liver. Oral administration of WAY-362450 to adult male C57BL/6 mice at a dose of 30 mg/kg/day reduced inflammatory cell infiltration and liver fibrosis. The reduction in inflammatory cell infiltration was associated with reduced serum levels of keratinocyte-derived chemokines (mKC) and MCP 1, as well as reduced liver gene expression of MCP-1 and VCAM-1. Treatment with WAY-362450 resulted in reduced liver fibrosis consistent with reduced liver gene expression of fibrosis markers. WAY-362450 treated LDLR at a dose of 30 mg/kg |
629664-81-9 - Configuration Solution Concentration Reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.281 ml | 11.403 ml | 22.806 ml |
| 5 mM | 0.456 ml | 2.281 ml | 4.561 ml |
| 10 mM | 0.228 ml | 1.14 ml | 2.281 ml |
| 5 mM | 0.046 ml | 0.228 ml | 0.456 ml |
629664-81-9 - brief introduction
Turofexorate isopropyl, also known as T-1095, is an organic compound. The following is an introduction to the properties, uses, preparation and safety information of Turofexorate isopropyl:Nature:
- Appearance: Turofexorate isopropyl as a white crystalline solid.
Hydrochloride form: Hydrochloride is a white to pale yellow crystalline solid.
Purpose:
- Turofexorate isopropyl acts as an agonist and can activate the synthesis of cellular deoxyribonucleic acid (DNA).
Production method:
- The preparation method of Turofexorate isopropyl is obtained through a series of organic synthesis reactions. The specific steps and conditions depend on the specific synthesis route.
Safety information:
- Turofexorate isopropyl is generally safe under the correct conditions of use and storage. Like all chemicals, it still needs to be treated with caution when used.
Personnel using or operating Turofexorate isopropyl need to have relevant knowledge and experience in chemical laboratory operations.
- Understand and adhere to relevant safety operating procedures and personal protective measures.
- When using Turofexorate isopropyl, avoid contact with the skin, eyes and respiratory tract. In case of accidental contact, rinse immediately with plenty of water and seek professional medical assistance if necessary.
When storing Turofexorate isopropyl, keep it sealed in a cool, dry place and away from sources of ignition and flammable substances.
Last Updated: 2024-04-09 20:45:29
