R1487
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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.


Chemical Structure

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R1487
CAS# 449811-92-1

Theoretical Analysis

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

Price and Availability

Size Price Availability Quantity
100.0mg USD 450.0 2 weeks
200.0mg USD 850.0 2 weeks
500.0mg USD 1750.0 2 weeks
1.0g USD 2850.0 2 weeks
2.0g USD 4850.0 2 weeks
5.0g USD 7450.0 2 weeks
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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

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 388.3748 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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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.

R1487

100.0mg / USD 450.0