货号	规格	价格	上海	北京	珠海	重庆	武汉
S84188-1mg	≥99%	￥295.00 S84188-1mg ￥295.00 3-5天	0 货期：3-5天	-	-	-	-
S84188-2mg	≥99%	￥425.00 S84188-2mg ￥425.00 3-5天	0 货期：3-5天	-	-	-	-
S84188-5mg	≥99%	￥690.00 S84188-5mg ￥690.00 3-5天	0 货期：3-5天	-	-	-	-
S84188-10mg	≥99%	￥1180.00 S84188-10mg ￥1180.00 3-5天	0 货期：3-5天	-	-	-	-
S84188-25mg	≥99%	￥2500.00 S84188-25mg ￥2500.00 3-5天	0 货期：3-5天	-	-	-	-
S84188-50mg	≥99%	￥3700.00 S84188-50mg ￥3700.00 3-5天	0 货期：3-5天	-	-	-	-
S84188-100mg	≥99%	￥5400.00 S84188-100mg ￥5400.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

SB-242235 is a potent and selective p38 MAP kinase inhibitor, with an IC50 of 1.0　μM in primary human chondrocytes

靶点：

IC50: 1.0　μM (p38 MAPK, primary human chondrocytes);p38MAPK; Autophagy

体外研究：

SB 242235 (0-10　μM) dose-dependently inhibits the activation of MAPKAP K2 with an IC50 of 1.0 μM in human chondrocytes stimulated with IL-1β. SB 242235 inhibits intracellular p38 activity, MAPKAP K2 was then isolated from these cells and assayed using HSP27 as a substrate. Western Blot Analysis Cell Line: Human chondrocytes Concentration: 0 μM,0.01 μM,0.1 μM,1 μM,10　μM Incubation Time: 15 minutes Result: Dose-dependently inhibited the activation of MAPKAP K2 with an IC50 of 1.0 μM.

体内研究：

SB242235 (100 mg/kg; p.o.) abolishes MAP-KAPK-2 activity and HSP27 phosphorylation. SB242235 inhibits expression of the pro-inflammatory cytokines interleukin (IL)-6 and KC (murine IL-8) and COX-2. SB-242235 is demonstrated non-linear elimination kinetics that manifested as a decrease in clearance with increasing dose and apparent oral bioavailability > 100% at high oral doses in rat and monkey. Animal Model: Female SKH-1 hairless mice (4–6 weeks) Dosage: 100 mg/kg Administration: Oral administered, 30 minutes prior to ultraviolet B (UVB) irradiation Result: Abolished MAP-KAPK-2 activity and heat shock protein 27 (HSP27) phosphorylation.

参考文献：

1. Badger, A.M., et al., Differential effects of SB 242235, a selective p38 mitogen-activated protein kinase inhibitor, on IL-1 treated bovine and human cartilage/chondrocyte cultures. Osteoarthritis Cartilage, 2000. 8(6): p. 434-43. 2. Kim AL , et al. Role of p38 MAPK in UVB-induced inflammatory responses in the skin of SKH-1 hairless mice. J Invest Dermatol. 2005 Jun;124(6):1318-25. 3. Ward, K.W., et al., SB-242235, a selective inhibitor of p38 mitogen-activated protein kinase. I: preclinical pharmacokinetics. Xenobiotica, 2002. 32(3): p. 221-33.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.83 ml	14.149 ml	28.297 ml
5 mM	0.566 ml	2.83 ml	5.659 ml
10 mM	0.283 ml	1.415 ml	2.83 ml
50 mM	0.057 ml	0.283 ml	0.566 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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