Research Area
Product Type
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Avasimibe(CI-1011) Chemical Structure
Voriconazole
Voriconazole (VFEND) is a triazole antifungal medication that is generally used to treat serious, invasive fungal infections.
Cytochrome P450 14a-demethylase inhibitor 1a
Cytochrome P450 14a-demethylase inhibitor 1a is an antifungal agent and an analog of fluconazole with an MIC80 of 3.9 ng/ml against Candida albicans.
Cytochrome P450 14a-demethylase inhibitor 1b
Cytochrome P450 14a-demethylase inhibitor 1b is an antifungal agent and an analog of fluconazole with an MIC80 of 3.9 ng/ml against Candida albicans and Microsporum gypseum.
Cytochrome P450 14a-demethylase inhibitor 1c
Cytochrome P450 14a-demethylase inhibitor 1c is an antifungal agent and an analog of fluconazole with an MIC80 of 15.6 ng/ml against Candida albicans and Microsporum gypseum.
Cytochrome P450 14a-demethylase inhibitor 1d
Cytochrome P450 14a-demethylase inhibitor 1d is an antifungal agent and an analog of fluconazole with an MIC80 of 15.6 ng/ml against Candida albicans and Microsporum gypseum.
Cytochrome P450 14a-demethylase inhibitor 1e
Cytochrome P450 14a-demethylase inhibitor 1e is an antifungal agent and an analog of fluconazole with an MIC80 of 15.6 ng/ml against Candida albicans.
Cytochrome P450 14a-demethylase inhibitor 1f
Cytochrome P450 14a-demethylase inhibitor 1f is an antifungal agent and an analog of fluconazole with an MIC80 of 15.6 ng/ml against Candida albicans.
Cytochrome P450 14a-demethylase inhibitor 1g
Cytochrome P450 14a-demethylase inhibitor 1g is an antifungal agent and an analog of fluconazole with an MIC80 of 0.25 µg/ml against Candida albicans.
Cytochrome P450 14a-demethylase inhibitor 1h
Cytochrome P450 14a-demethylase inhibitor 1h is an antifungal agent and an analog of fluconazole with an MIC80 of 15.6 ng/ml against Microsporum gypseum.
Cytochrome P450 14a-demethylase inhibitor 1i
Cytochrome P450 14a-demethylase inhibitor 1i is an antifungal agent and an analog of fluconazole with an MIC80 of 62.5 ng/ml against Candida albicans.
Biological Activity
Avasimibe(CI-1011) is a novel orally bioavailable acyl coenzyme A:cholesterol acyltransferase inhibitor with IC50 of 2.9, 13.9, 26.5 µM for CYP2C9, CYP1A2, and CYP2C19.
Avasimibe(CI-1011) has been previously shown to be a potent inducer of CYP3A4 and multiple drug resistance protein 1. [1] In a study, avasimibe decreased the VLDL apoB pool size by 40–43% and the hepatic secretion rate of VLDL apoB by 38–41%, but did not alter its fractional catabolism. Avasimibe decreased the LDL apoB pool size by 13–57%, largely due to a dose-dependent 25–63% in the LDL apoB production rate. Hepatic LDL receptor mRNA abundances were unchanged, consistent with a marginal decrease in LDL apoB FCRs. Hepatic ACAT activity was decreased by 51% (P = 0.050) and 68% (P = 0.087) by low and high dose avasimibe, respectively. [2][3]
References on Avasimibe(CI-1011)
- [1] Drug Metab Dispos. 2004 Dec;32(12):1370-6.
- [2] J Lipid Res. 1999 Jul;40(7):1317-27.
- [3] Cardiovasc Drug Rev. 2003;21(1):33-50.
Product Information
| Molecular Weight (WM): | 501.72 |
|---|---|
| Formula: | C29H43NO4S |
| CAS No.: | 166518-60-1 |
| Synonyms: |
CI-1011
|
| Dissolve in (25°C): | DMSO ≥100mg/mL |
| Water <1mg/mL | |
| Ethanol ≥8mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
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