WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H407302
CAS#: 449808-64-4
Description: R1487 is an orally bioavailable and highly selective inhibitors of p38α mitogen-activated protein kinase.
Hodoodo Cat#: H407302
Name: R1487 HCl
CAS#: 449808-64-4
Chemical Formula: C19H19ClF2N4O3
Exact Mass: 0.00
Molecular Weight: 424.833
Elemental Analysis: C, 53.72; H, 4.51; Cl, 8.34; F, 8.94; N, 13.19; O, 11.30
Synonym: R1487 ; R 1487 ; R-1487 ; R1487 HCl.
IUPAC/Chemical Name: 6-(2,4-difluorophenoxy)-8-methyl-2-(oxan-4-ylamino)pyrido[2,3-d]pyrimidin-7-one hydrochloride
InChi Key: RQHSAIGGUWVOBG-UHFFFAOYSA-N
InChi Code: InChI=1S/C19H18F2N4O3.ClH/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);1H
SMILES Code: O=C1C(OC2=CC=C(F)C=C2F)=CC3=CN=C(NC4CCOCC4)N=C3N1C.[H]Cl
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, not in water
Shelf Life: >2 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
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 424.83 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.
| 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 |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
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.
