2,6-diisopropylphenyl 2-(2,4,6-triisopropylphenyl)acetylsulfamate
Avasimibe
CAS: 166518-60-1
Molecular Formula: C29H43NO4S
2,6-diisopropylphenyl 2-(2,4,6-triisopropylphenyl)acetylsulfamate - Names and Identifiers
2,6-diisopropylphenyl 2-(2,4,6-triisopropylphenyl)acetylsulfamate - Physico-chemical Properties
| Molecular Formula | C29H43NO4S |
| Molar Mass | 501.72 |
| Density | 1.072±0.06 g/cm3(Predicted) |
| Melting Point | 178-180° (Lee); mp 169.5-170.4° (Dozeman) |
| Solubility | DMSO: ≥40mg/mL |
| Appearance | powder |
| Color | white to tan |
| pKa | 1.97±0.70(Predicted) |
| Storage Condition | room temp |
| MDL | MFCD00934956 |
| Use | Avasimibe inhibits ACAT,IC50 is 3.3 μM, and human P450 isoenzymes CYP2C9, CYP1A2 and CYP2C19,IC50 is 2.9 μM, 13.9 μM and 26.5 μM respectively |
| In vitro study | Avasimibe, at a concentration of 1 μg/ml, acts on human monocyte-derived macrophages (HMMs) by inhibiting LDL binding and reducing the number of scavenger receptors during foam cell formation, while reducing total cholesterol (TC) and esterified cholesterol (EC). At a concentration of 2 μg/ml Avasimibe, preincubation with 10 μg/ml LDL enhanced the exoexcretion of cholesterol from HMM foam cells. Avasimibe inhibited the accumulation of lipoprotein (a) in the culture medium of primary monkey liver cells by 11.9-31.3% in a dose-dependent manner, and this change was related to the decrease of ApoA. Avasimibe was incubated in HepG2 cells for 24 h at concentrations of 10 nM, 1 μm, and 10 μm to reduce ApoB secretion into the medium by 25%, respectively, 27%, and 43%. Avasimibe reduces ApoB secretion by enhancing intracellular degradation of ApoB rather than reducing ApoB synthesis. Avasimibe acts on IC-21 macrophages and inhibits ACTC with an IC50 of 3.3 μm. Avasimibe inhibits the human P450 isoenzymes CYP2C9, CYP1A2 and CYP2C19 with IC50 of 2.9 μm, 13.9 μm and 26.5 μm, respectively. Avasimibe acts on glioma cells to inhibit ACAT-1 expression and cholesterol ester synthesis. Avasimibe inhibits glioma cell growth by inducing cell cycle arrest and apoptosis caused by caspase-8 and caspase-3 activation. |
| In vivo study | Avasimibe significantly reduced lipoprotein (a) and total cholesterol levels in 9 healthy male monkeys. Avasimibe was orally fed at a dose of 30 mg/kg per day for 3 weeks. Lipoprotein (a) total cholesterol levels were reduced to 68 and 73% of control levels, respectively. Avasimibe lowers total cholesterol mainly because it lowers low-density lipoprotein (LDL). |
2,6-diisopropylphenyl 2-(2,4,6-triisopropylphenyl)acetylsulfamate - Risk and Safety
| WGK Germany | 3 |
2,6-diisopropylphenyl 2-(2,4,6-triisopropylphenyl)acetylsulfamate - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.993 ml | 9.966 ml | 19.931 ml |
| 5 mM | 0.399 ml | 1.993 ml | 3.986 ml |
| 10 mM | 0.199 ml | 0.997 ml | 1.993 ml |
| 5 mM | 0.04 ml | 0.199 ml | 0.399 ml |
Last Update：2024-01-02 23:10:35
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Product Name: Avasimibe Visit Supplier Webpage Request for quotationCAS: 166518-60-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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