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R1487 Hydrochloride

Cat. No. M9013
R1487 Hydrochloride Structure
Synonym:

R1487 HCl

Size Price Availability Quantity
5mg USD 120  USD120 In stock
10mg USD 180  USD180 In stock
50mg USD 550  USD550 In stock
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Quality Control & Documentation
Biological Activity

R1487 Hydrochloride is an orally bioavailable and highly selective inhibitors of p38α mitogen-activated protein kinase. R1487 HCl potently inhibits cytokine production in a variety of in vitro and in vivo models. R1487 hydrochloride inhibits production of TNFR by human monocytic cells (THP-1) and inhibits production of IL-1β in human whole blood (HWB) induced by LPS.

Chemical Information
Molecular Weight 424.83
Formula C19H19ClF2N4O3
CAS Number 449808-64-4
Solubility (25°C) DMSO: ≥ 25 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Goldstein DM, et al. J Med Chem. Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitors of p38α mitogen-activated protein kinase.

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  Catalog
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Keywords: R1487 Hydrochloride, R1487 HCl supplier, p38 MAPK, inhibitors, activators


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