| 產品描述： | RWJ-67657 (JNJ 3026582) is an orally active and selective p38α and p38β MAPK inhibitor with IC50s of 1 and 11 μM, respectively. RWJ-67657 displays no activity at p38γ and p38δ, and exhibits cardio protective effect. Anti-inflammatory and anti-tumor activity |
| 靶點： |
p38α:1 μM (IC50);p38β:11 μM (IC50);p38MAPK |
| 體外研究： |
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 Assay Cell Line: MCF-7 breast carcinoma cells Concentration: 10 μM Incubation Time: 24 hours Result: Decreased colony formation. |
| 體內研究： |
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. |
| 參考文獻： |
1. Shahin R, et al. Research advances in kinase enzymes and inhibitors for cardiovascular disease treatment. Future Sci OA. 2017 Aug 8;3(4):FSO204. 2. Wadsworth SA, et al. RWJ 67657, a potent, orally active inhibitor of p38 mitogen-activated protein kinase. J Pharmacol Exp Ther. 1999 Nov;291(2):680-7. 3. Frigo DE, et al. p38 mitogen-activated protein kinase stimulates estrogen-mediated transcription and proliferation through the phosphorylation and potentiation of the p160 coactivator glucocorticoid receptor-interacting protein 1. Mol Endocrinol. 2006 May;20(5):971-83. 4. Bai YY, et al. Synergistic Effects of Transplanted Endothelial Progenitor Cells and RWJ 67657 in Diabetic Ischemic Stroke Models. Stroke. 2015 Jul;46(7):1938-46. |
| 溶解性： |
Soluble in DMSO |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.35 ml |
11.751 ml |
23.502 ml |
| 5 mM |
0.47 ml |
2.35 ml |
4.7 ml |
| 10 mM |
0.235 ml |
1.175 ml |
2.35 ml |
| 50 mM |
0.047 ml |
0.235 ml |
0.47 ml |
|
| 注意： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學品經營許可證（不帶存儲）
營業執照(三證合一)
北京