RWJ 67657

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的、口服活性的 p38 MAPK 抑制剂，可抑制 LPS 刺激的人 PBMC 产生 TNF-α 和 IL-1β，IC50 分别为 3 和 11 nM。

A potent, selective, orally active p38 MAPK inhibitor that inhibits the production of TNF-α and IL-1β by LPS-stimulated human PBMCs with IC50 of 3 and 11 nM, respectively; inhibits p38α from purified LPS-activated human monocytes with IC50 of 30 nM, less potent for p38β; also inhibits Src (IC50=5 uM), p65 Lck and no activity against other MAPKs and serine-threonine kinases; inhibits TNF-alpha production in LPS-injected mice.

RWJ-67657 inhibits the release of TNF-α by lipopolysaccharide (LPS)-treated human peripheral blood mononuclear cells with an IC50 of 3 nM, as well as the release of TNF-α from peripheral blood mononuclear cells treated with the superantigen staphylococcal enterotoxin B, with an IC50 value of 13 nM. RWJ67657 (10 μM; 24 hours) decreases colony formation in MCF-7 cells.Cell Proliferation AssayCell Line:MCF-7 breast carcinoma cells Concentration:10 μM Incubation Time:24 hours Result:Decreased colony formation.

RWJ-67657 inhibits TNF-alpha production in lipopolysaccharide-injected mice (87% inhibition at 50 mg/kg) and in rats (91% inhibition at 25 mg/kg) after oral administration. RWJ-67657 (50 mg/kg; administered orally; once per day for 7 consecutive days) displays a potent anti-inflammatory effect. By both improving the functioning of endothelial progenitor cells (EPCs) and reducing inflammation, EPC transplantation plus RWJ-67657 administration synergistically promotes angiogenesis and neurogenesis after diabetic stroke. Animal Model:The db/db mice (male, 8 weeks old) with EPCs Dosage:50 mg/kg Administration:Administered orally; once per day for 7 consecutive days Result:Increased angiogenesis and neurogenesis of diabetic mice after cotreatment with EPCs transplantation.

RWJ67657 | RWJ-67657

MAPK/ERK Signaling

p38 MAPK

p38 MAPK

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215303-72-3

425.5

C27H24FN3O

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (293.77 mM)

FC(C=C1)=CC=C1C2=C(C3=CC=NC=C3)N(CCCC4=CC=CC=C4)C(C#CCCO)=N2

4-[4-(4-fluorophenyl)-1-(3-phenylpropyl)-5-(4-pyridinyl)-1H-imidazol -2-yl]-3-butyn-1-ol

(-20℃)

With Ice Pack

≥ 2 years