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Tipranavir
CAS No. 174484-41-4
Tipranavir ( —— )
产品货号. M35286 CAS No. 174484-41-4
Tipranavir (PNU-140690) 有效抑制 HIV-1 蛋白酶 酶活性和二聚化，对抗多种蛋白酶抑制剂(PI)的HIV-1分离株具有有效的活性，IC50 为 66-410 nM。Tipranavir 抑制 SARS-CoV-2 3CLpro 活性。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 5MG | ￥2594 | 有现货 |
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| 10MG | ￥3914 | 有现货 |
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| 25MG | ￥6008 | 有现货 |
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| 50MG | ￥8082 | 有现货 |
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| 100MG | ￥10530 | 有现货 |
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| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
| 1 mL x 10 mM in DMSO | ￥3449 | 有现货 |
|
生物学信息
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产品名称Tipranavir
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注意事项本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
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产品简述Tipranavir (PNU-140690) 有效抑制 HIV-1 蛋白酶 酶活性和二聚化，对抗多种蛋白酶抑制剂(PI)的HIV-1分离株具有有效的活性，IC50 为 66-410 nM。Tipranavir 抑制 SARS-CoV-2 3CLpro 活性。
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产品描述Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM. Tipranavir inhibits SARS-CoV-2 3CLpro activity.
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体外实验Tipranavir (PNU-140690) inhibits the enzymatic activity of HIV-1 protease, blocks the dimerization of protease subunits, and exerts potent activity against a wide spectrum of wild-type and multi-PI-resistant HIV-1 variants. When a mixture of 11 multi-PI-resistant (but TPV-sensitive) clinical isolates (HIV11MIX), which include HIVB and HIVC, is selected against Tipranavir, HIV11MIX rapidly (by 10 passages [HIV11MIXP10]) acquires high-level Tipranavir (PNU-140690) resistance and replicates at high concentrations of Tipranavir (PNU-140690). cHIVBI54V and cHIVBI54V/V82T are significantly resistant to Tipranavir (PNU-140690), with IC50s of 2.9 and 3.2 μM, respectively, which are 11- and 12-fold increases in comparison to the IC50 against cHIVB, respectively.
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体内实验Tipranavir (PNU-140690) is administered orally twice daily and must be given in combination with low-dose ritonavir (RTV) to boost Tipranavir bioavailability. In Tipranavir/r-cotreated mice, the Tipranavir (PNU-140690) abundance in the liver, spleen, and eyes is significantly higher than that in mice treated with Tipranavir alone. Tipranavir (PNU-140690) metabolites accounts for 31 and 38% in the serum and liver in the Tipranavir-alone group. In Tipranavir (PNU-140690) and Tipranavir (TPV/r)-cotreated mice, only 1 and 2% of metabolites are detected in the serum and liver. Sprague-Dawley rats are administered a single dose of [14C]Tipranavir (PNU-140690) with coadministration of RTV. The most abundant metabolite in feces is an oxidation metabolite. In urine, no single metabolite is found to be significantly present.
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同义词——
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通路Microbiology/Virology
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靶点HIV
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受体SARS-CoV | HIV Protease
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研究领域——
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适应症——
化学信息
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CAS Number174484-41-4
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分子量602.66
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分子式C31H33F3N2O5S
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纯度>98% (HPLC)
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溶解度In Vitro:?DMSO 中的溶解度 : 200 mg/mL (331.86 mM; 超声助溶 ) Ethanol 中的溶解度 : ≥ 50 mg/mL (82.97 mM)
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SMILESCCC[C@@]1(CCc2ccccc2)CC(O)=C([C@H](CC)c2cccc(NS(=O)(=O)c3ccc(cn3)C(F)(F)F)c2)C(=O)O1
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Aoki M, et al. Loss of the protease dimerization inhibition activity of tipranavir (TPV) and its association with the acquisition of resistance to TPV by HIV-1. J Virol. 2012 Dec;86(24):13384-96.?
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