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R1487 Hydrochloride

Cat. No. M9013
R1487 Hydrochloride Structure
Synonym:

R1487 HCl

Size Price Availability Quantity
5mg USD 120 In stock
10mg USD 180 In stock
50mg USD 550 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 424.83
Formula C19H19ClF2N4O3
CAS Number 449808-64-4
Purity >98%
Solubility DMSO: ≥ 25 mg/mL
Storage at -20°C
References

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.
Goldstein DM, et al. J Med Chem. 2011 Apr 14;54(7):2255-65. PMID: 21375264.

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  Catalog
Abmole Inhibitor Catalog 2017




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

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