WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 555669
CAS#: 449811-92-1
Description: R-1487 is an orally bioavailable and highly selective inhibitors of p38α mitogen-activated protein kinase. Pyruvate dehydrogenase (PDH) plays an important role in regulating carbohydrate oxidation in skeletal muscle. PDH is deactivated by a set of PDH kinases (PDK1, PDK2, PDK3, PDK4), with PDK2 and PDK4 being the most predominant isoforms in skeletal muscle.
MedKoo Cat#: 555669
Name: R1487
CAS#: 449811-92-1
Chemical Formula: C19H18F2N4O3
Exact Mass: 388.1347
Molecular Weight: 388.3748
Elemental Analysis: C, 58.76; H, 4.67; F, 9.78; N, 14.43; O, 12.36
Synonym: R-1487; R 1487; R1487;
IUPAC/Chemical Name: 6-(2,4-Difluorophenoxy)-8-methyl-2-(tetrahydropyran-4-ylamino)pyrido(2,3-d)pyrimidin-7-one
InChi Key: KKKRKRMVJRHDMG-UHFFFAOYSA-N
InChi Code: InChI=1S/C19H18F2N4O3/c1-25-17-11(10-22-19(24-17)23-13-4-6-27-7-5-13)8-16(18(25)26)28-15-3-2-12(20)9-14(15)21/h2-3,8-10,13H,4-7H2,1H3,(H,22,23,24)
SMILES Code: O=C1C(OC2=CC=C(F)C=C2F)=CC3=CN=C(NC4CCOCC4)N=C3N1C
1: Dunford EC, Herbst EA, Jeoung NH, Gittings W, Inglis JG, Vandenboom R, LeBlanc
PJ, Harris RA, Peters SJ. PDH activation during in vitro muscle contractions in
PDH kinase 2 knockout mice: effect of PDH kinase 1 compensation. Am J Physiol
Regul Integr Comp Physiol. 2011 Jun;300(6):R1487-93. doi:
10.1152/ajpregu.00498.2010. Epub 2011 Mar 16. PubMed PMID: 21411764.
2: Goldstein DM, Soth M, Gabriel T, Dewdney N, Kuglstatter A, Arzeno H, Chen J,
Bingenheimer W, Dalrymple SA, Dunn J, Farrell R, Frauchiger S, La Fargue J, Ghate
M, Graves B, Hill RJ, Li F, Litman R, Loe B, McIntosh J, McWeeney D, Papp E, Park
J, Reese HF, Roberts RT, Rotstein D, San Pablo B, Sarma K, Stahl M, Sung ML,
Suttman RT, Sjogren EB, Tan Y, Trejo A, Welch M, Weller P, Wong BR, Zecic H.
Discovery of
6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-p
yrido[2,3-d]pyrimidin-7-one (pamapimod) and
6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]py
rimidin-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. Epub 2011 Mar 4. PubMed PMID: 21375264.