货号:A732241 同义名: 沙奎拉韦 / Ro 31-8959/003;Saquinavir (mesylate)
Saquinavir mesylate is an HIV Protease inhibitor used in antiretroviral therapy. Saquinavir could inhibit SARS-CoV-2 3CLpro main protease.
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产品名称 | HIV Protease ↓ ↑ | HIV-1 caspid ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Dextran sulfate sodium, mw 40,000 | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Vicriviroc maleate | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Rosamultin | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Darunavir | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Lopinavir |
++++
HIV protease, Ki: 1.3 pM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Chloroquine | ✔ | Autophagy | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Amprenavir |
+
HIV protease, IC50: 14.6 ng/mL |
PXR | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||
NBD-556 | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Nelfinavir Mesylate |
+++
HIV protease, Ki: 2 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Atazanavir Sulfate | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Limonin | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Saquinavir |
++
HIV proteinase, IC50: 2.7 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Ritonavir | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Azvudine | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Lenacapavir |
++++
HIV-1 capsid, EC50: 0.1 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
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。 |
描述 | Saquinavir (SAQ) mesylate is a potent inhibitor of the HIV-1 protease indicated in combination with other antiretrovirals for the management of HIV-1 infection[3]. Saquinavir is an anti-retroviral drug with very low oral bioavailability (e.g. 0.7-4.0%) due to its affinity toward efflux transporters (P-gp) and metabolic enzymes (CYP3A4)[4]. As with other HIV protease inhibitors, saquinavir inhibits the cleavage of the gag-pol protein substrate leading to the release of structurally defective and functionally inactive viral particles. It is active on both HIV-1 and HIV-2, and also has activity on chronically infected cells and HIV strains resistant to reverse transcriptase inhibitors. Saquinavir is characterised by a low bioavailability which is further reduced in the fasting state. Because of its metabolic interference with the CYP system, saquinavir cannot be coadministered with astemizole, terfenadine or cisapride. Saquinavir is generally well tolerated, with mild gastrointestinal symptoms representing the most commonly observed adverse effects[5]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00035932 | HIV Infections | Phase 3 | Completed | - | - |
NCT00197145 | Infection, Human Immunodeficie... 展开 >>ncy Virus I 收起 << | Phase 3 | Terminated | - | - |
NCT00197145 | - | Terminated | - | - | |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.30mL 0.26mL 0.13mL |
6.52mL 1.30mL 0.65mL |
13.04mL 2.61mL 1.30mL |
CAS号 | 149845-06-7 |
分子式 | C39H54N6O8S |
分子量 | 766.947 |
别名 | 沙奎拉韦 ;Ro 31-8959/003;Saquinavir (mesylate) |
运输 | 蓝冰 |
存储条件 |
粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 16 mg/mL(20.86 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 |
动物实验配方 |