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Atazanavir Sulfate/阿扎那韦硫酸盐 {[allProObj[0].p_purity_real_show]}

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。

Atazanavir Sulfate/阿扎那韦硫酸盐 化学结构 CAS号:229975-97-7
Atazanavir Sulfate/阿扎那韦硫酸盐 化学结构
CAS号:229975-97-7
Atazanavir Sulfate/阿扎那韦硫酸盐 3D分子结构
CAS号:229975-97-7
Atazanavir Sulfate/阿扎那韦硫酸盐 化学结构 CAS号:229975-97-7
Atazanavir Sulfate/阿扎那韦硫酸盐 3D分子结构 CAS号:229975-97-7
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Atazanavir Sulfate/阿扎那韦硫酸盐 纯度/质量文件 产品仅供科研

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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。

Atazanavir Sulfate/阿扎那韦硫酸盐 生物活性

靶点
  • HIV Protease

    HIV protease, Ki:2.66 nM

  • HIV Protease

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.

Atazanavir Sulfate/阿扎那韦硫酸盐 细胞实验

Cell Line
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.

Atazanavir Sulfate/阿扎那韦硫酸盐 动物实验

Species
Animal Model
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

Atazanavir Sulfate/阿扎那韦硫酸盐 临床研究

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 - -

Atazanavir Sulfate/阿扎那韦硫酸盐 参考文献

[1]Zhang D, Chando TJ, et al. In vitro inhibition of UDP glucuronosyltransferases by atazanavir and other HIV protease inhibitors and the relationship of this property to in vivo bilirubin glucuronidation. Drug Metab Dispos. 2005 Nov;33(11):1729-39.

[2]Robinson BS, Riccardi KA, et al. BMS-232632, a highly potent human immunodeficiency virus protease inhibitor that can be used in combination with other available antiretroviral agents. Antimicrob Agents Chemother. 2000 Aug;44(8):2093-9.

[3]Robinson BS, Riccardi KA, Gong YF, Guo Q, Stock DA, Blair WS, Terry BJ, Deminie CA, Djang F, Colonno RJ, Lin PF. BMS-232632, a highly potent human immunodeficiency virus protease inhibitor that can be used in combination with other available antiretroviral agents. Antimicrob Agents Chemother. 2000 Aug;44(8):2093-9. doi: 10.1128/AAC.44.8.2093-2099.2000. PMID: 10898681; PMCID: PMC90019.

[4]Noor MA, Flint OP, Maa JF, Parker RA. Effects of atazanavir/ritonavir and lopinavir/ritonavir on glucose uptake and insulin sensitivity: demonstrable differences in vitro and clinically. AIDS. 2006 Sep 11;20(14):1813-21. doi: 10.1097/01.aids.0000244200.11006.55. PMID: 16954722.

[5]Croom KF, Dhillon S, Keam SJ. Atazanavir: a review of its use in the management of HIV-1 infection. Drugs. 2009 May 29;69(8):1107-40. doi: 10.2165/00003495-200969080-00009. PMID: 19496633.

[6]Song S, Ji Y, Zhang G, Zhang X, Li B, Li D, Jiang W. Protective Effect of Atazanavir Sulphate Against Pulmonary Fibrosis In Vivo and In Vitro. Basic Clin Pharmacol Toxicol. 2018 Feb;122(2):199-207. doi: 10.1111/bcpt.12871. Epub 2017 Sep 6. PMID: 28816009.

[7]Zhang G, Zhang X, Li D, Tian J, Jiang W. Long-term oral atazanavir attenuates myocardial infarction-induced cardiac fibrosis. Eur J Pharmacol. 2018 Jun 5;828:97-102. doi: 10.1016/j.ejphar.2018.03.041. Epub 2018 Mar 29. PMID: 29605419.

Atazanavir Sulfate/阿扎那韦硫酸盐 实验方案

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

Atazanavir Sulfate/阿扎那韦硫酸盐 技术信息

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

请根据您的动物给药指南选择适当的溶解方案。
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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