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.
Product information
CAS Number: 2410393-15-4
Molecular Weight: 435.44
Formula: C21H24F3N5O2
Chemical Name: N-{2-[2-(dimethylamino)ethyl]-6-(2-hydroxypropan-2-yl)-2H-indazol-5-yl}-6-(trifluoromethyl)pyridine-2-carboxamide
Smiles: CC(C)(O)C1=CC2=NN(CCN(C)C)C=C2C=C1NC(=O)C1C=CC=C(N=1)C(F)(F)F
InChiKey: QAOWCAZEVIIQTF-UHFFFAOYSA-N
InChi: InChI=1S/C21H24F3N5O2/c1-20(2,31)14-11-16-13(12-29(27-16)9-8-28(3)4)10-17(14)26-19(30)15-6-5-7-18(25-15)21(22,23)24/h5-7,10-12,31H,8-9H2,1-4H3,(H,26,30)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 100 mg/mL (229.65 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
Products are for research use only. Not for human use.
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