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MEK&P38 MAPK

R1487 (Hydrochloride) (449808-64-4)

R1487 (Hydrochloride) is highly potent and highly selective inhibitors of p38α. target: p38α; R1487 (Hydrochloride) potently inhibits cytokine production in a variety of in vitro and in vivo models.

Not Intended for Therapeutic Use. For research use only.

CAS: 449808-64-4 Category

R1487 (Hydrochloride) (449808-64-4) Description:

R1487 is an orally bioavailable and highly potent and highly selective inhibitors of p38α. target: p38α; R1487 (Hydrochloride) potently inhibits cytokine production in a variety of in vitro and in vivo models. R1487 (Hydrochloride) inhibits production of TNFR by human monocytic cells (THP-1) and inhibits production of IL-1β in human whole blood (HWB) induced by LPS.

R1487 (Hydrochloride) (449808-64-4) Specifications:

Product Name R1487 HCl
Synonym R1487 ; R 1487 ; R-1487 ; R1487 HCl.
Chemical Name 6-(2,4-difluorophenoxy)-8-methyl-2-(oxan-4-ylamino)pyrido[2,3-d]pyrimidin-7-one hydrochloride
Drug Class N/A
Purity >98% (or refer to the Certificate of Analysis)
CAS Number 449808-64-4
Molecular Formula C19H19ClF2N4O3
Molecular Weight 424.8328
Monoisotopic Mass
424.111 g/mol

 

MDL number MFCD18711690
InChIKey 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 O=C1C(OC2=CC=C(F)C=C2F)=CC3=CN=C(NC4CCOCC4)N=C3N1C.[H]Cl
Form solid powder
Color N/A
Solubility  Soluble in DMSO, not soluble in water.
Storage Temp.  Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application P38 inhibitor

 


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RIDADR NONH for all modes of transport

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.
  • 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. Goldstein DM, et al. J Med Chem. 2011 Apr 14;54(7):2255-65.

1 review for R1487 (Hydrochloride) (449808-64-4)

  1. Cofttek

    Never had such good experience before,The R1487 (Hydrochloride) (449808-64-4) is high purity,also customer service is pretty nice !gotta try!!

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