CAS NO: | 1228690-19-4 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
2mg | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | AM966 is a high affinity, selective, oralLPA1-antagonist, inhibits LPA-stimulated intracellular calcium release (IC50=17 nM). | ||||||||||||||||
IC50& Target | LPA1[1] | ||||||||||||||||
体外研究 (In Vitro) | AM966 is a potent, selective, orally bioavailable LPA1receptor antagonist. AM966 inhibits LPA1-mediated chemotaxis of human A2058 melanoma cells (IC50=138±43 nM), IMR-90 human lung fibroblasts (IC50=182±86 nM) and CHO mLPA1cells (IC50=469±54 nM)[1]. LPA-induced ERK1/2 activation is completely blocked by AM966 (100 nM), which selectively antagonizes LPA1over LPA2-5, with an IC50value of 3.8±0.4 nM. Pre-treatment with AM966 (100 nM) completely blocks ERK1/2 phosphorylation induced by either amitriptyline or mianserin[2]. | ||||||||||||||||
体内研究 (In Vivo) | AM966 (30 mg/kg, BID) reduces vascular leakage, inflammation and lung injury and inflammation in a 3 day bleomycin model. AM966 inhibits lung fibrosis, maintains mouse body weight and decreases lung inflammation 14 days after bleomycin lung injury. AM966 reduces vascular leakage, tissue injury and pro-fibrotic cytokine production in the 14 day bleomycin study. AM966 demonstrates greater efficacy compared to pirfenidone in the 14 day bleomycin model. AM966 decreases mortality and fibrosis at late time points after bleomycin injury[1]. | ||||||||||||||||
分子量 | 490.93 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C27H23ClN2O5 | ||||||||||||||||
CAS 号 | 1228690-19-4 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 100 mg/mL(203.70 mM;Need ultrasonic) 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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