产品
编 号：F750363
分子式：C27H31ClN4O3
分子量：495.01
分子式：C27H31ClN4O3
分子量：495.01
产品类型
规格
价格
是否有货
结构图
CAS No: 2245231-10-9
产品详情
生物活性：
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.
体内研究：
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.PK ValuesRatDog
10 mg/kg (p.o)5 mg/kg (i.v)2 mg/kg (p.o)2 mg/kg (i.v)
T1/2 (hr)4.563.836.906.11
AUC (hr.nM)780744267646839260
Cmax (nM)21380-3983-
Ft (%)92.8-50.6-
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.
体外研究：
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 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.
体内研究：
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.PK ValuesRatDog
10 mg/kg (p.o)5 mg/kg (i.v)2 mg/kg (p.o)2 mg/kg (i.v)
T1/2 (hr)4.563.836.906.11
AUC (hr.nM)780744267646839260
Cmax (nM)21380-3983-
Ft (%)92.8-50.6-
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.
体外研究：
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).
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备