R1487
R1487 Basic information
- Product Name:
- R1487
- Synonyms:
-
- R1487
- SY-R1487
- Pyrido[2,3-d]pyriMidin-7(8H)-one, 6-(2,4-difluorophenoxy)-8-Methyl-2-[(tetrahydro-2H-pyran-4-yl)aMino]-, (Hydrochloride) (1:1)
- 6-(2,4-Difluorophenoxy)-8-methyl-2-[(tetrahydro-2H-pyran-4-yl)amino]pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride
- R1487 HCL
- R1487 (Hydrochloride)
- R-1487 HYDROCHLORIDE;R 1487 HYDROCHLORIDE
- R1487 (SY-R1487)
- CAS:
- 449808-64-4
- MF:
- C19H19ClF2N4O3
- MW:
- 424.8289664
- Mol File:
- 449808-64-4.mol
R1487 Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- DMF: 1 mg/ml; DMSO: 1 mg/ml; DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml
- form
- A crystalline solid
- color
- Light yellow to yellow
R1487 Usage And Synthesis
Uses
R1487 Hydrochloride is a highly potent and selective p38α inhibitor, with Kd values of 0.2 nM and 29 nM for p38α and p38β, respectively[1].
in vivo
R1487 (Compounds 2a, orally) demonstrates significant dose-dependent inhibition of serum TNFα and IL-1β[1].
Oral bioavailability of 10 mg/kg R1487 (Compounds 2a) in monkey, rat, and dog was 51.6%, 29.3%, 10.3%, respectively[1].
IC 50
p38α: 0.2 nM (Kd); p38β: 29 nM (Kd)
References
[1] Goldstein DM et al. 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. J Med Chem. 2011 Apr 14;54(7):2255-65. DOI:10.1021/jm101423y
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