1. Immunology/Inflammation
  2. IRAK
  3. HS271

HS271 

Cat. No.: HY-131903 Purity: 99.92%
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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 580 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1700 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2500 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
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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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (229.65 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2965 mL 11.4826 mL 22.9653 mL
5 mM 0.4593 mL 2.2965 mL 4.5931 mL
10 mM 0.2297 mL 1.1483 mL 2.2965 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

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

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Product Name:
HS271
Cat. No.:
HY-131903
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