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

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.

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Pirmitegravir Chemical Structure

Pirmitegravir Chemical Structure

CAS No. : 2245231-10-9

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Pirmitegravir Related Antibodies

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Description

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]
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].

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

Pirmitegravir Related Antibodies
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 -

MedChemExpress (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
Molecular Weight

495.01

Formula

C27H31ClN4O3
CAS No.
SMILES

O=C([C@H](C1=C(N=C(C2=C1C3=CC=C(C=C3)Cl)N(C(C)=C2C)CC4=CN(N=C4)C)C)OC(C)(C)C)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Pirmitegravir Related Classifications

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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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