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帕马皮莫德

p38α 选择性抑制剂
规格或纯度: 99%
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货号 (SKU) 包装规格 是否现货 价格 数量
P413914-1mg
 1mg 现货 Stock Image
P413914-5mg
 5mg 现货 Stock Image
P413914-10mg
 10mg 现货 Stock Image
P413914-50mg
 50mg 现货 Stock Image
P413914-100mg
 100mg 现货 Stock Image
P413914-250mg
 250mg 现货 Stock Image
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mitogen-activated protein kinase 10 Inhibitor mitogen-activated protein kinase 11 Inhibitor mitogen-activated protein kinase 14 Inhibitor mitogen-activated protein kinase 8 Inhibitor mitogen-activated protein kinase 9 Inhibitor
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基本描述

规格或纯度 99%
英文名称 Pamapimod
别名 帕吡莫德
英文别名 Pamapimod|449811-01-2|RO 4402257|R1503|PamapimodR-1503|Ro4402257|Ro-4402257|CHEMBL1090089|CHEBI:90685|R-1503|8S2C9V11K4|6-(2,4-Difluorophenoxy)-2-{[3-Hydroxy-1-(2-Hydroxyethyl)propyl]amino}-8-Methylpyrido[2,3-D]pyrimidin-7(8h)-One|Pamapimod (R-1503, Ro440
生化机理 Pamapimod (R-1503, Ro4402257) is a novel, selective inhibitor of p38 mitogen-activated protein kinase. It inhibits p38α and p38β enzymatic activity with IC50 values of 0.014±0.002 and 0.48± 0.04 microM, respectively with no activity against p38delta or p38gamma isoforms.
储存温度 -20°C储存
运输条件 超低温冰袋运输
产品介绍


Information

Pamapimod (R-1503, Ro4402257) is a novel, selective inhibitor ofp38 mitogen-activated protein kinase. It inhibits p38α and p38β enzymatic activity with IC50 values of 0.014±0.002 and 0.48± 0.04 microM, respectively with no activity against p38delta or p38gamma isoforms.


Targets

p38α (Cell-free assay); p38β (Cell-free assay) 0.014 μM; 0.48 μM


In vitro

Pamapimod inhibited p38, but inhibition of JNK was not detected. Pamapimod also inhibited lipopolysaccharide (LPS)-stimulated tumor necrosis factor (TNF) α production by monocytes, interleukin (IL)-1β production in human whole blood, and spontaneous TNFα production by synovial explants from RA patients.


In vivo

In murine collagen-induced arthritis, pamapimod reduced clinical signs of inflammation and bone loss at 50 mg/kg or greater. In a rat model of hyperalgesia, pamapimod increased tolerance to pressure in a dose-dependent manner, suggesting an important role of p38 in pain associated with inflammation. Pamapimod suppresses spontaneous production of TNFα by synovial explants from RA patients. LPS- and TNFα-stimulated production of TNFα and IL-6 in rodents also was inhibited by pamapimod.


Cell Research(from reference)

Cell lines：Human Monocytic Cell Line, THP-1?

Concentrations：15 μM?

Incubation Time：150 min?

产品属性

IC50 p38α, IC50: 0.014 μM
ALogP 1.298
HBD Count 3
Rotatable Bond 8

名称和标识符

IUPAC Name 6-(2,4-difluorophenoxy)-2-(1,5-dihydroxypentan-3-ylamino)-8-methylpyrido[2,3-d]pyrimidin-7-one
INCHI InChI=1S/C19H20F2N4O4/c1-25-17-11(10-22-19(24-17)23-13(4-6-26)5-7-27)8-16(18(25)28)29-15-3-2-12(20)9-14(15)21/h2-3,8-10,13,26-27H,4-7H2,1H3,(H,22,23,24)
InChi Key JYYLVUFNAHSSFE-UHFFFAOYSA-N
Canonical SMILES CN1C2=NC(=NC=C2C=C(C1=O)OC3=C(C=C(C=C3)F)F)NC(CCO)CCO
PubChem CID 16220188
分子量 406.38

化学和物理性质

溶解性 Solubility (25°C) In vitro DMSO: 81 mg/mL (199.32 mM); Ethanol: 28 mg/mL (68.9 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility 81
DMSO(mM) Max Solubility 199.3208327
Water(mg / mL) Max Solubility ＜1

关联配体

Ligand ID 9915
名称 pamapimod
别名 compound 2b [PMID: 21375264]
类别 Synthetic organic
学名 6-(2,4-difluorophenoxy)-2-(1,5-dihydroxypentan-3-ylamino)-8-methylpyrido[2,3-d]pyrimidin-7-one
生物活性评价 Pamapimod exhibits submicromolar binding affinity for only seven out of >300 kinases tested . It binds p38α (MAPK14) and p38β (MAPK11), but not p38γ (MAPK12) or p38δ (MAPK13). Pamapimod potently inhibited cytokine production in a selection of in vitro and in vivo models, including inhibition of TNFα production by human monocytic THP-1 cells, and inhibition of LPS-induced IL-1β production in human whole blood.
评价 Pamapimod is an ATP-competitive (Type I), orally bioavailable and highly selective inhibitor of p38α mitogen-activated protein kinase (MAPK14), that was developed for immunomodulatory potential .

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参考文献

1. Cohen SB, Cheng TT, Chindalore V, Damjanov N, Burgos-Vargas R, Delora P, Zimany K, Travers H, Caulfield JP.  (2009)  Evaluation of the efficacy and safety of pamapimod, a p38 MAP kinase inhibitor, in a double-blind, methotrexate-controlled study of patients with active rheumatoid arthritis..  Arthritis Rheum,  60  (2):  (335-44).  [PMID:19180516]
2. Alten RE, Zerbini C, Jeka S, Irazoque F, Khatib F, Emery P, Bertasso A, Rabbia M, Caulfield JP.  (2010)  Efficacy and safety of pamapimod in patients with active rheumatoid arthritis receiving stable methotrexate therapy..  Ann Rheum Dis,  69  (2):  (364-7).  [PMID:19357113]
3. Zhang X, Huang Y, Navarro MT, Hisoire G, Caulfield JP.  (2010)  A proof-of-concept and drug-drug interaction study of pamapimod, a novel p38 MAP kinase inhibitor, with methotrexate in patients with rheumatoid arthritis..  J Clin Pharmacol,  50  (9):  (1031-8).  [PMID:20100913]
4. Cohen S, Fleischmann R.  (2010)  Kinase inhibitors: a new approach to rheumatoid arthritis treatment..  Curr Opin Rheumatol,  22  (3):  (330-5).  [PMID:20164774]
5. Joos H, Albrecht W, Laufer S, Brenner RE.  (2010)  Differential effects of p38MAP kinase inhibitors on the expression of inflammation-associated genes in primary, interleukin-1beta-stimulated human chondrocytes..  Br J Pharmacol,  160  (5):  (1252-62).  [PMID:20590617]
6. Goldstein DM, Soth M, Gabriel T, Dewdney N, Kuglstatter A, Arzeno H, Chen J, Bingenheimer W, Dalrymple SA, Dunn J et al..  (2011)  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..  J Med Chem,  54  (7):  (2255-65).  [PMID:21375264]
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