产品说明书
Atazanavir
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同义名 : | BMS-232632;CGP 73547;Reyataz;Zrivada;Latazanavir |
| CAS号 : | 198904-31-3 | |
| 货号 : | A182779 | |
| 分子式 : | C38H52N6O7 | |
| 纯度 : | 98% | |
| 分子量 : | 704.856 | |
| MDL号 : | MFCD08435966 | |
| 存储条件： |
粉末 Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 85 mg/mL(120.59 mM)，配合低频超声助溶，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 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 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]. The use of HIV protease inhibitors for the treatment of HIV infection remains a primary and effective component of combination antiretroviral therapy. 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]. In a phase I clinical trial of atazanavir, single oral doses of 100, 300, 600, 900 or 1200 mg were given to healthy volunteers, pharmcokinetic profile showed that atazanavir had good oral bioavailability and that peak concentrations and area under the curve increased in a greater-than-dose proportional manner[4]. In a phase II study, atazanavir 400 or 600 mg o.d combined with saquinavir-sgc 1200 mg o.d were compared to ritonavir 400 mg plus saquinavir-sgc 400 mg both twice-daily, at the end of 48 weeks, all 3 arms showed similar declines in viral load (range: 1.19 - 1.6 log10) and increases in CD4 cell counts[4]. Atazanavir significantly attenuated CoCl2-induced neonatal rat cardiac fibroblast (rCFs) proliferation in a concentration-dependent manner[5]. Recently, Atazanavir is undergoing clinical trial for 2019-novel coronavirus treatment. | ||
| 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 |
| NCT00544128 | HIV Infections | Phase 4 | Completed | - | Japan ... 展开 >> International Medical Center of Japan Shinjuku, Tokyo, Japan, 1628655 收起 << |
| NCT01105611 | HIV Infections ... 展开 >> Hepatitis C 收起 << | Phase 4 | Unknown | December 2012 | Ireland ... 展开 >> Department of Genitourinary Medicine and Infectious Diseases, St. James's Hospital Recruiting Dublin, Ireland Contact: Colm Bergin, MD, FRCPI +35314162507 cbergin@stjames.ie Contact: James Woo, MB, MRCPI +353868108086 wooj@tcd.ie Principal Investigator: Colm Bergin, MD, FRCPI Sub-Investigator: James Woo, MB, MRCPI Mater Misericordiae University Hospital Not yet recruiting Dublin, Ireland Contact: Patrick Mallon, MB FRCPI PhD +35317166311 Paddy.Mallon@ucd.ie Principal Investigator: Patrick Mallon, MB FRCPI PhD 收起 << |
| NCT01458769 | Healthy Volunteers | Phase 1 | Completed | - | - |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.42mL 0.28mL 0.14mL |
7.09mL 1.42mL 0.71mL |
14.19mL 2.84mL 1.42mL |
| 参考文献 |
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