货号	规格	价格	上海	北京	珠海	重庆	武汉
V49143-1mg	≥98%	￥670.00 V49143-1mg ￥670.00 3-5天	0 货期：3-5天	-	-	-	-
V49143-5mg	≥98%	￥1500.00 V49143-5mg ￥1500.00 3-5天	0 货期：3-5天	-	-	-	-
V49143-10mg	≥98%	￥2500.00 V49143-10mg ￥2500.00 3-5天	0 货期：3-5天	-	-	-	-
V49143-25mg	≥98%	￥5490.00 V49143-25mg ￥5490.00 3-5天	0 货期：3-5天	-	-	-	-
V49143-50mg	≥98%	￥8770.00 V49143-50mg ￥8770.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

TK-129 is an orally active, low-toxicity, potent KDM5B inhibitor (with high affinity; IC50=44 nM). TK-129 exerts cardioprotective effects by inhibiting KDM5B and blocking the KDM5B-associated Wnt pathway. TK-129 reduces ang II-induced activation of cardiac fibroblasts in vitro and reduces isoprenaline-induced myocardial remodelling and fibrosis in vivo. TK-129 can be used in studies of cardiovascular disease.

靶点：

KDM5:44 nM (IC50)

体外研究：

TK-129 (2 g/kg; p.o.; single) shows good bio-safety in mice.
TK-129 (50 mg/kg; p.o.; twice daily for 24 days) effectively reduces isoproterenol-induced pathological myocardial remodeling in vivo.
TK-129 (2 or 10 mg/kg; i.v. or p.o.; single) demonstrates favorable PK properties in vivo.

体内研究：

TK-129 mediates inhibition of KDM5B activity significantly reduces the activation, migration, and proliferation of myofibroblasts induced by Ang II in vitro.
TK-129 (10 μM; 48 h) shows low cytotoxicity in NRCFs and NRCMs.
TK-129 (0.1, 0.2, 0.3, 0.4, 0.5 μM; 48 h) can engage toand inhibit KDM5B activity in NRCFs.

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	3.275 ml	16.373 ml	32.746 ml
5 mM	0.655 ml	3.275 ml	6.549 ml
10 mM	0.327 ml	1.637 ml	3.275 ml
50 mM	0.065 ml	0.327 ml	0.655 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。

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