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.


Price and Availability

Size Price Shipping out time Quantity
100mg USD 450 2 weeks
200mg USD 850 2 weeks
500mg USD 1750 2 weeks
1g USD 2850 2 weeks
2g USD 4850 2 weeks
5g USD 7450 2 weeks
Inquire bulk and customized quantity

Pricing updated 2020-07-06. Prices are subject to change without notice.

R-1487, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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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


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


Technical Data

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


References

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.