化合物IQP-0528 T27625

Product Introduction
Bioactivity


英文名: IQP-0528

描述: IQP-0528是一种高效的非核苷类逆转录酶抑制剂（NNRTI），通过阻断病毒进入，有可能用于治疗HIV 感染，并且作为杀微生物凝胶显示出抗病毒活性。IQP-0528对HIV-1和HIV-2都显示出抑制作用，对HIV-1的EC50为0.2 nM，对HIV-2的EC50为100 nM。

体外活性: The in vitro safety evaluations showed no significant loss in cell viability or significant inflammatory response after treatment with a 3.0% HEC gel containing 0.25% IQP-0528. In an in vitro HIV-1 entry inhibition assay, the lead formulation showed an 50% effective concentration of 0.14 μg/ml for gel in culture media, which corresponds to ∼0.001 μM IQP-0528.[5]

体内活性: we report the first-in-human evaluation of such a gel containing 1% IQP-0528, an investigational antiretroviral. Seven HIV-1-negative participants received one 10 mL rectal dose of radiolabeled 1% IQP-0528 gel. Median IQP-0528 concentrations in rectal tissue exceeded the in vitro EC95 against HIV-1 (0.07 ng/mg) by 3-5 h of dosing and remained above this concentration for at least 24 h, despite a 3-log reduction in concentration over this duration of time. Rectal tissue PD assessed by ex vivo HIV challenge-demonstrated significant p24 antigen reduction 3-5 h postdose compared with baseline , but not 24-26 h postdose. The IQP-0528 gel possesses desirable features for a topical microbicide including local safety with no systemic absorption, delivery of locally high IQP-0528 concentrations, and significant reductions in ex vivo HIV infectivity.[6]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 4 mg/mL (11.75 mM)


关键字: SJ 3991 | IQP 0528 | IQP-0528

相关产品: Cephalotaxine | LHF-535 | Compound TN1582(SC) | SIRT1-IN-1 | pocapavir | SARS-CoV-2 3CLpro-IN-20 | Merimepodib | 3-Methoxycatechol | A2ti-2 | Epigoitrin

相关库: Bioactive Compounds Library Max | Inhibitor Library | Anti-Viral Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途