
Pirmitegravir
CAS No. 2245231-10-9
Pirmitegravir( —— )
Catalog No. M35151 CAS No. 2245231-10-9
Pirmitegravir (STP0404) is a potent and selective inhibitor of allosteric integrase (ALLINI) targeting the LEDGF/p75 binding site. Pirmitegravir inhibits PBMC.
Purity : >98% (HPLC)






Size | Price / USD | Stock | Quantity |
2MG | 207 | Get Quote |
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5MG | 321 | Get Quote |
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10MG | 519 | Get Quote |
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25MG | 1003 | Get Quote |
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50MG | 1647 | Get Quote |
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100MG | 2151 | Get Quote |
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500MG | Get Quote | Get Quote |
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Biological Information
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Product NamePirmitegravir
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NoteResearch use only, not for human use.
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Brief DescriptionPirmitegravir (STP0404) is a potent and selective inhibitor of allosteric integrase (ALLINI) targeting the LEDGF/p75 binding site. Pirmitegravir inhibits PBMC.
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DescriptionPirmitegravir 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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In VitroPirmitegravir (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).
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In VivoPirmitegravir (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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Synonyms——
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PathwayMicrobiology/Virology
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TargetHIV
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RecptorHIV Protease
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Research Area——
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Indication——
Chemical Information
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CAS Number2245231-10-9
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Formula Weight495.01
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Molecular FormulaC27H31ClN4O3
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Purity>98% (HPLC)
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Solubility——
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SMILES[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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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Maehigashi T, et al. A highly potent and safe pyrrolopyridine-based allosteric HIV-1 integrase inhibitor targeting host LEDGF/p75-integrase interaction site. PLoS Pathog. 2021;17(7):e1009671.
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