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BI 224436
CAS No. 1155419-89-8
BI 224436 ( BI224436 )
产品货号. M10545 CAS No. 1155419-89-8
BI 224436 是一种有效的、特异性的、HIV-1 非催化位点整合酶抑制剂 (NCINI)，针对不同的 HIV-1 实验室毒株的 EC50 为 11-27 nM。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 5MG | ￥68305 | 有现货 |
|
| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
生物学信息
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产品名称BI 224436
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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BI 224436 是一种有效的、特异性的、HIV-1 非催化位点整合酶抑制剂 (NCINI)，针对不同的 HIV-1 实验室毒株的 EC50 为 11-27 nM。
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产品描述BI 224436 is a potent, specific, noncatalytic site integrase inhibitor (NCINI) of HIV-1 with EC50 of 11-27 nM against different HIV-1 laboratory strains, with minimal cellular cytotoxicity; exhibits a low, ～2.1-fold decrease in antiviral potency in the presence of 50% human serum andserum-shifted EC95 values ranging between 22 and 75 nM; also retains full antiviral activity against recombinant viruses encoding INSTI resistance substitutions N155S, Q148H, and E92Q; displays an additive effect in combination with most approved antiretrovirals, including INSTIs.HIV Infection Phase 1 Clinical.
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体外实验BI 224436 has cellular cytotoxicity of more than 90 μM. BI 224436 has a low, 2.1-fold decrease in antiviral potency in the presence of 50% human serum. BI 224436 retains full antiviral activity against recombinant viruses encoding INSTI resistance substitutions N155S, Q148H, and E92Q. BI 224436 displays an additive effect in combination with most approved antiretrovirals, including INSTIs. BI 224436 has drug-like in vitro absorption, distribution, metabolism, and excretion (ADME) properties, including Caco-2 cell permeability, solubility, and low cytochrome P450 inhibition.
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体内实验BI 224436 exhibits excellent pharmacokinetic profiles in rat (clearance as a percentage of hepatic flow [CL], 0.7%; bioavailability [F], 54%), monkey (CL, 23%; F, 82%), and dog (CL, 8%; F, 81%).
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同义词BI224436
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通路Microbiology/Virology
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靶点HIV
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受体HIV
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研究领域Infection
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适应症HIV Infection
化学信息
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CAS Number1155419-89-8
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分子量391.467
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分子式C24H25NO4
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纯度>98% (HPLC)
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溶解度DMSO : ≥ 50 mg/mL 112.99 mM
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SMILESO=C(O)[C@H](C1=C(C2=CC(CCCO3)=C3C=C2)C4=CC=CC=C4N=C1)OC(C)(C)C
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化学全称(2S)-[4-(3,4-Dihydro-2H-chromen-6-yl)-3-quinolinyl][(2-methyl-2-propanyl)oxy]acetic acid
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. Fader LD, et al. ACS Med Chem Lett. 2014 Jan 22;5(4):422-7.
2. Fenwick C, et al. Antimicrob Agents Chemother. 2014 Jun;58(6):3233-44.
3. Demeulemeester J, et al. Expert Opin Ther Pat. 2014 Jun;24(6):609-32.
