Pirmitegravir

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

Pirmitegravir 是一种有效的、一流的变构整合酶 (ALLINI) 抑制剂，靶向 LEDGF/p75 结合位点。 Pirmitegravir 在人类 PBMC 中显示皮摩尔 IC50，对 HIV-1 的安全指数 >24,000。Pirmitegravir 具有出色的抗病毒和安全特性。

Pirmitegravir is a potent and first-in-class inhibitor of allosteric integrase (ALLINI) that targets LEDGF/p75 binding site. Pirmitegravir displays picomolar IC50 in human PBMCs with a >24,000 therapeutic index against HIV-1. Pirmitegravir harbors outstanding anti-virus and safety properties.

Pirmitegravir (Compound STP0404) inhibits dual tropic HIV-189.6 at 1.4 nM IC50 in CEMx174 cells.Pirmitegravir (Compound STP0404) is a highly potent ALLINI with picomolar to single-digit nanomolar IC50 values that inhibits both wild type and Ral-resistant HIV-1 strains.Pirmitegravir (Compound STP0404) displays IC50 of 0.41 nM against HIV-1NL4-3 without observable cytotoxicity in human PBMCs at 10 μM (TC50 >10μM).

Pirmitegravir (Compound STP0404) displays appropriate PK profiles for once daily administration.Pirmitegravir (Compound STP0404) lacks micronucleus-inducing and bone marrow cell proliferation inhibitory potentials in rats (500, 1000 and 2000 mg/kg/day), supporting that STP0404 is not genotoxic.Assessment of Pharmacokinetics (PK) profile of Pirmitegravir (Compound STP0404) in rat and dog.Animal Model:SD rats and beagle dogs Dosage:1, 2, 5, and 10 mg/kg Administration:i.v.; p.o.Result:The half-life (T1/2) was 3–7 h, and oral bioavailability (Ft) was 50–93% in these two animal species. Systemic exposure, which was determined by area under the curve and maximum concentration of STP0404 in plasma (AUC and Cmax), increased dose-dependently from 2 to 10 mg/kg.

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Microbiology/Virology

HIV

HIV Protease

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2245231-10-9

495.01

C27H31ClN4O3

>98% (HPLC)

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[C@@H](OC(C)(C)C)(C(O)=O)C=1C(=C2C(N(CC=3C=NN(C)C3)C(C)=C2C)=NC1C)C4=CC=C(Cl)C=C4

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(-20℃)

With Ice Pack

≥ 2 years