1. IRAK
  2. HS271

HS271 

Cat. No.: HY-131903
Handling Instructions

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.

For research use only. We do not sell to patients.

HS271 Chemical Structure

HS271 Chemical Structure

CAS No. : 2410393-15-4

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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[1].

IC50 & Target[1]

IRAK4

7.2 μM (IC50)

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[1].
HS271 exhibits a t1/2 of 3.3 h and Cmax of 2107 ng/mL[1].
HS271 is stable in liver microsome assays across other species, including rat, mouse, monkey, and human[1].
HS271 exhibits oral bioavailability of 67.3%, 58.2%, 14.4&% and 49% in mouse, rat, dog and monkey, respectively[1].

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

Animal Model: A rat model of collagen induced arthritis (CIA)[1].
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.
Molecular Weight

435.44

Formula

C₂₁H₂₄F₃N₅O₂

CAS No.

2410393-15-4

SMILES

O=C(NC1=CC2=CN(CCN(C)C)N=C2C=C1C(C)(O)C)C3=NC(C(F)(F)F)=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

HS271HS 271HS-271IRAKInterleukin-1 receptor associated kinaseIL-1R associated kinaseArthritisCIATNFαInhibitorinhibitorinhibit

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HS271
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HY-131903
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