2. Metabolic Enzyme/Protease Anti-infection
  3. HIV Integrase HIV
  4. Pirmitegravir

Pirmitegravir  (Synonyms: STP0404)

目录号: HY-130000
产品使用指南

摩尔计算器

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。

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Pirmitegravir Chemical Structure

Pirmitegravir Chemical Structure

CAS No. : 2245231-10-9

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Pirmitegravir 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1].

IC50 & Target

allosteric integrase (ALLINI)[1]
体外研究
(In Vitro)

Pirmitegravir (Compound STP0404) inhibits dual tropic HIV-189.6 at 1.4 nM IC50 in CEMx174 cells[1].
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[1].
Pirmitegravir (Compound STP0404) displays IC50 of 0.41 nM against HIV-1NL4-3 without observable cytotoxicity in human PBMCs at 10 μM (TC50 >10μM)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Pirmitegravir 相关抗体:
体内研究
(In Vivo)

Pirmitegravir (Compound STP0404) displays appropriate PK profiles for once daily administration[1].
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[1].
Assessment of Pharmacokinetics (PK) profile of Pirmitegravir (Compound STP0404) in rat and dog[1].

PK Values Rat Dog
10 mg/kg (p.o) 5 mg/kg (i.v) 2 mg/kg (p.o) 2 mg/kg (i.v)
T1/2 (hr) 4.56 3.83 6.90 6.11
AUC (hr.nM) 78074 42676 4683 9260
Cmax (nM) 21380 - 3983 -
Ft (%) 92.8 - 50.6 -

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SD rats and beagle dogs[1]
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.
Clinical Trial
分子量

495.01

Formula

C27H31ClN4O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Pirmitegravir 相关分类

  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pirmitegravir2245231-10-9STP0404STP 0404STP-0404HIV IntegraseHIVHuman immunodeficiency virusallosteric integraseALLINILEDGF/p75HIV-1anti-virussafetycytotoxicityInhibitorinhibitorinhibit

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