货号:A276573
同义名:
硫酸阿扎那韦
/ BMS-232632 sulfate; BMS-232632-05
Atazanavir Sulfate 是一种蛋白酶抑制剂,作为抗逆转录病毒试剂,广泛用于 HIV/AIDS 机制及预防策略的研究。


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| 产品名称 | HIV Protease ↓ ↑ | HIV-1 caspid ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Dextran sulfate sodium salt(MW 40000) | ✔ | M.W 40000 | |||||||||||||||||
| Vicriviroc maleate | ✔ | 95% | |||||||||||||||||
| Rosamultin | ✔ | 97% | |||||||||||||||||
| Darunavir | ✔ | 98% | |||||||||||||||||
| Lopinavir |
++++
HIV protease, Ki: 1.3 pM |
99+% | |||||||||||||||||
| Chloroquine | ✔ | Autophagy | 95% | ||||||||||||||||
| Amprenavir |
+
HIV protease, IC50: 14.6 ng/mL |
PXR | 99%+ | ||||||||||||||||
| NBD-556 | ✔ | 99%+ | |||||||||||||||||
| Nelfinavir Mesylate |
+++
HIV protease, Ki: 2 nM |
99%+ | |||||||||||||||||
| Atazanavir Sulfate | ✔ | 98% | |||||||||||||||||
| Limonin | ✔ | 98% | |||||||||||||||||
| Saquinavir |
++
HIV proteinase, IC50: 2.7 nM |
98% | |||||||||||||||||
| Ritonavir | ✔ | 98% | |||||||||||||||||
| Azvudine | ✔ | 98% | |||||||||||||||||
| Lenacapavir |
++++
HIV-1 capsid, EC50: 0.1 nM |
97% | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 靶点 |
|
| 描述 | Human immunodeficiency virus type 1 (HIV-1) protease specifically processes gag (p55) and gag-pol (p160) viral polyproteins to yield the viral structural proteins (p17, p24, p7, and p6)[3]. Atazanavir Sulfate (BMS-232632 Sulfate) is a protease inhibitor used to treat and prevent HIV/AIDS. Atazanavir is an azapeptide HIV-1 protease inhibitor that exhibits potent anti-HIV activity with EC50 of 2.6 to 5.3 nM and EC90 of 9 to 15 nM in cell culture[3]. Atazanavir/ritonavir (300/100 mg once daily) inhibited glucose uptake in vitro significantly less than lopinavir/ritonavir (400/100 mg twice daily) for 10 day[4]. In clinical trial, mean reductions from baseline in plasma HIV RNA levels in antiretroviral therapy-naive patients were not significantly different between once-daily atazanavir 400mg and two- or three-times daily nelfinavi or once-daily efavirenz[5]. After 21 days of treatment with atazanavir sulfate plus ritonavir (30 + 10 mg/kg) in Bleomycin (BLM)-induced pulmonary fibrosis model, the BLM-induced pathology score was reduced by 51.0%, and increase in collagen contents and Hyp content were also decreased compared with the BLM group[6]. In myocardial infarction (MI)-induced cardiac fibrosis rats, intragastric administration of atazanavir sulfate 30 mg/k ameliorated changes in the left ventricular systolic pressure (LVSP), + dp/dtmax, and - dp/dtmax after 4 weeks[7]. Recently, it is reported that Atazanavir showed anti-2019-novel coronavirus activity. |
| Concentration | Treated Time | Description | References | |
| Bovine cardiac myocytes | 70–21,120 ng/mL | 2 hours | Enhanced RyR2 open probability | Int J Mol Sci. 2022 Dec 23;24(1):274. |
| Whole blood | 0, 1, 5, 10 µM | 24 hours | To assess the effect of atazanavir on LPS-induced cytokine release. Results showed that atazanavir did not influence the release of TNF-α or IL-10. | Front Immunol. 2023 May 16;14:1176775. |
| Human primary monocytes | 1 µM and 10 µM | 24 hours | To evaluate the effects of ATV and ATV/RTV on viral replication, cell death, and inflammatory mediator release in SARS-CoV-2-infected monocytes. Results showed ATV and ATV/RTV significantly reduced viral RNA levels, cell death, and IL-6 and TNF-α release. | Antimicrob Agents Chemother. 2020 Sep 21;64(10):e00825-20. |
| C2C12 skeletal muscle myotubes | 6 µM | 3 minutes | To evaluate the effect of Atazanavir on intracellular calcium homeostasis in skeletal muscle cells, results showed that ATV induced Ca2+ transients and mobilized Ca2+ from the SR via activation of RyR1. | Antiviral Res. 2021 Mar;187:104975. |
| Candida auris AR0390 | 16 mg/mL | 48 hours | To evaluate the killing kinetics of atazanavir in combination with itraconazole, showing significant reduction in fungal burden. | Antimicrob Agents Chemother. 2023 May 17;67(5):e0163122. |
| A549 cells | 0.22 µM | 48 hours | To evaluate the inhibitory effects of ATV and ATV/RTV on SARS-CoV-2 replication in human lung epithelial cells. Results showed ATV had an EC50 of 0.22 μM in A549 cells, more potent than in Vero cells. | Antimicrob Agents Chemother. 2020 Sep 21;64(10):e00825-20. |
| Vero cells | 0.5 µM | 48 hours | To evaluate the inhibitory effects of ATV and ATV/RTV on SARS-CoV-2 replication. Results showed ATV/RTV was more effective than ATV, with EC50 values of 0.5 μM and 2.0 μM, respectively. | Antimicrob Agents Chemother. 2020 Sep 21;64(10):e00825-20. |
| Candida auris AR0390 | 8 mg/mL | To assess the effect of atazanavir on ATP content, showing a decrease in cellular ATP levels. | Antimicrob Agents Chemother. 2023 May 17;67(5):e0163122. | |
| Candida auris | 32 mg/mL | To evaluate the impact of atazanavir on glucose utilization, showing significant obstruction of glucose utilization. | Antimicrob Agents Chemother. 2023 May 17;67(5):e0163122. | |
| Candida auris clinical isolates | 8 mg/mL | To assess the effect of atazanavir on efflux pump activity, showing significant inhibition of Nile red efflux. | Antimicrob Agents Chemother. 2023 May 17;67(5):e0163122. | |
| Administration | Dosage | Frequency | Description | References | ||
| Rat | Primary rat ventricular myocytes | Culture medium | 5.0 µM | Single dose, recorded for 60 seconds | Induced Ca2+ transients/waves | Int J Mol Sci. 2022 Dec 23;24(1):274. |
| Female immunocompromised CD-1 mice | Disseminated C. auris infection model | Oral | Atazanavir 90 mg/kg, Ritonavir 30 mg/kg, Itraconazole 5 mg/kg | Treatment started 2 hours post-infection and continued for 48 hours | To evaluate the in vivo efficacy of atazanavir in combination with itraconazole, showing significant reduction in fungal burden in kidneys. | Antimicrob Agents Chemother. 2023 May 17;67(5):e0163122. |
| Healthy volunteers | Human model | Oral | ATV/r 300/100 mg | Once daily | Evaluate DDI between ATV/r and rifampicin | Clin Pharmacokinet. 2022 Mar;61(3):375-386 |
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT01003990 | HIV | Phase 3 | Completed | - | - |
| NCT01591850 | Healthy Volunteer | Phase 1 | Completed | - | United States, Florida ... 展开 >> Merritt Island, Florida, United States, 32953 收起 << |
| NCT01003990 | - | Completed | - | - | |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
1.25mL 0.25mL 0.12mL |
6.23mL 1.25mL 0.62mL |
12.45mL 2.49mL 1.25mL |
|
| CAS号 | 229975-97-7 |
| 分子式 | C38H54N6O11S |
| 分子量 | 802.93 |
| SMILES Code | O=C(OC)N[C@@H](C(C)(C)C)C(NN(CC1=CC=C(C2=NC=CC=C2)C=C1)C[C@H](O)[C@H](CC3=CC=CC=C3)NC([C@H](C(C)(C)C)NC(OC)=O)=O)=O.O=S(O)(O)=O |
| MDL No. | MFCD08067748 |
| 别名 | 硫酸阿扎那韦 ;BMS-232632 sulfate; BMS-232632-05; Reyataz; Atazanavir(sulfate) |
| 运输 | 蓝冰 |
| InChI Key | DQSGVVGOPRWTKI-QVFAWCHISA-N |
| Pubchem ID | 158550 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, 2-8°C |
| 溶解方案 |
DMSO: 160 mg/mL(199.27 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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