Atazanavir - CAS:198904-31-3

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Atazanavir (Synonyms:阿扎那韦; BMS-232632)

目录号 : KCM12342 CAS No. : 198904-31-3 纯度 : ≥95%

Data Sheet SDS 产品使用指南

Atazanavir is an azapeptide inhibitor of HIV-1 protease (K = 2.66 nM). It has antiviral activity against a variety of HIV-1 strains in several cell types with EC values ranging from 2.62 to 5.28 nM. Atazanavir exhibits a minor synergistic effect when used in combination with the reverse transcriptase inhibitor zidovudine in HIV-1-infected human peripheral blood mononuclear cells (PBMCs) and an additive effect when used in combination with several additional reverse transcriptase or HIV-1 protease inhibitors. Atazanavir also inhibits UDP-glucuronyltransferase 1A1 (UGT1A1), which is involved in bilirubin clearance. Formulations containing atazanavir have been used in combination therapy for the treatment of HIV-1 infection.

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10mg		In-stock
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10 mM * 1 mL in DMSO		In-stock

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生物活性

Atazanavir is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death.

体外研究

Atazanavir (1-10 μM, 72 h) alleviates hypoxia induced proliferation of rat cardiac fibroblasts (rCFs) by regulating the HMGB1/TLR9 pathway.
Atazanavir (1-10 μM, 72 h) inhibited the expression of collagen I, collagen III, HMGB1, p-I κ B α, and p-NF - κ B in rat cardiac fibroblasts.
Atazanavir (1-10 μM, 48 h) inhibits the growth of A, U251, T98G, and LN229 cells and induces endoplasmic reticulum stress in U251, T98G, and LN229 cells.
Atazanavir (6.0 μM) triggered Ca2+transient and plasma membrane foaming in C2C12 skeletal muscle myotubes cells.

Cell Proliferation Assay

Cell Line:	Rat cardiac fibroblasts (rCFs)
Concentration:	0, 1, 3, 10 μM
Incubation Time:	72 hours
Result:	Inhibited rCFs proliferation in a concentration-dependent manner.

Western Blot Analysis

Cell Line:	Rat cardiac fibroblasts (rCFs)
Concentration:	0, 1, 3, 10 μM
Incubation Time:	72 hours
Result:	Reduced collagen I and collagen III levels in a concentration-dependent manner. Inhibited HMGB1, p-IκBα and p-NF-κB expression.

Cell Viability Assay

Cell Line:

A, U251, T98G, LN229 glioblastoma cell

Concentration:

0, 12, 25, 50, 75, 100 μM

Incubation Time:

48 hours

Result:

Reduced cell growth and survival.

Western Blot Analysis

Cell Line:

U251, T98G, and LN229 glioblastoma cell lines

Concentration:

0, 12, 25, 50, 75, 100 μM

Incubation Time:

48 hours

Result:

Increased GRP78 and CHOP protein levels dose-dependently and activated caspase-4 in all cell lines.

体内研究

Atazanavir (30 mg/kg, i.g., once daily for 4 weeks) reduced collagen deposition and inhibited cardiac remodeling in myocardial infarction (MI) model rats.

Animal Model:	The myocardial infarction (MI) model was established in adult male Sprague-Dawley rats through surgical procedures^[4].
Dosage:	30 mg/kg
Administration:	i.g., daily, 4 weeks
Result:	Significantly improved systolic pressure (LVSP), +dp/dtmax and −dp/dtmax after MI. Decreased the non-infarcted LV and hypertrophy of the myocytes. Significantly attenuated an increase in morphometrical collagen volume fraction in the border left ventricle. Lowered the heart index (heart-weight to body-weight ratio). Decreased expressions of α-SMA, HMGB1, TLR 9, p-NF-κB, collagen I and collagen III, and the content of Hyp.

分子式

C₃₈H₅₂N₆O₇

分子量

704.86

CAS号

198904-31-3

中文名称

阿扎那韦

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO: 83.33 mg/mL (118.22 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.4187 mL	7.0936 mL	14.1872 mL
5 mM	0.5431 mL	1.4187 mL	5.4305 mL
10 mM	0.2715 mL	1.3576 mL	1.4187 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

纯度： ≥95%

Data Sheet

SDS

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