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HS271

CAS No. 2410393-15-4

HS271( —— )

Catalog No. M28114 CAS No. 2410393-15-4

HS271 is a highly potent, orally active and selective IRAK4 inhibitor, with an IC50 of 7.2 μM. HS271 exhibits superior enzymatic and cellular activities, as well as excellent pharmacokinetic properties.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    HS271
  • Note
    Research use only, not for human use.
  • Brief Description
    HS271 is a highly potent, orally active and selective IRAK4 inhibitor, with an IC50 of 7.2 μM. HS271 exhibits superior enzymatic and cellular activities, as well as excellent pharmacokinetic properties.
  • Description
    HS271 is a highly potent, orally active and selective IRAK4 inhibitor, with an IC50 of 7.2 μM. HS271 exhibits superior enzymatic and cellular activities, as well as excellent pharmacokinetic properties.(In Vivo):In rat models of LPS-induced TNFα production collagen-induced arthritis, HS271 (15-150 mg/kg) shows robust antiinflammatory efficacy with a t1/2 of 3.3 h and Cmax of 2107 ng/mL. The oral bioavailability of HS271 is 67.3%, 58.2%, 14.4&% and 49% in mice, rats, dogs, and monkeys, respectively.
  • In Vitro
    ——
  • In Vivo
    HS271 (15-150 mg/kg) displays robust in vivo antiinflammatory efficacy as evaluated in rat models of LPS induced TNFα production collageninduced arthritis.HS271 exhibits a t1/2 of 3.3 h and Cmax of 2107 ng/mL.HS271 is stable in liver microsome assays across other species, including rat, mouse, monkey, and human.HS271 exhibits oral bioavailability of 67.3%, 58.2%, 14.4&% and 49% in mouse, rat, dog and monkey, respectively. Animal Model:A rat model of collagen induced arthritis (CIA).Dosage:15, 50, 150 mg/kg.Administration:PO, once daily.Result:Led to a significant reduction in paw swelling as compared to vehicle control, with a minimum effective dose at 15 mg/kg QD. Notably, at 150 mg/kg QD, HS271 eliminated the paw swelling.
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    G2019S LRRK2|LRRK2
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2410393-15-4
  • Formula Weight
    435.44
  • Molecular Formula
    C21H24F3N5O2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (229.65 mM)
  • SMILES
    N/A
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Nigel Ramsden, et al. Chemoproteomics-based design of potent LRRK2-selective lead compounds that attenuate Parkinson's disease-related toxicity in human neurons. ACS Chem Biol. 2011 Oct 21;6(10):1021-8.
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