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)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Pirmitegravir
  • Note
    Research use only, not for human use.
  • Brief Description
    Pirmitegravir (STP0404) is a potent and selective inhibitor of allosteric integrase (ALLINI) targeting the LEDGF/p75 binding site. Pirmitegravir inhibits PBMC.
  • 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.
  • In Vitro
    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).
  • In Vivo
    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.
  • Synonyms
    ——
  • Pathway
    Microbiology/Virology
  • Target
    HIV
  • Recptor
    HIV Protease
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2245231-10-9
  • Formula Weight
    495.01
  • Molecular Formula
    C27H31ClN4O3
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • 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
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • 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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