CAS NO: | 1192189-69-7 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
2mg | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | LX7101 is a potent inhibitor ofLIMKandROCK2withIC50values of 24, 1.6 and 10 nM forLIMK1,LIMK2andROCK2, respectively; also inhibitsPKAwith anIC50less than 1 nM. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | LX7101 is a dual LIM-kinase and ROCK inhibitor for the treatment of ocular hypertension and associated glaucoma. LX-7101 also displays potent inhibition of Akt1 with an IC50of less than 1 nM[1]. The overall selectivity of LX7101 for LIMK2 increases at the higher physiological ATP concentrations. Under physiological conditions, the activity of LX7101 is primarily due to inhibition of LIMK2[2]. | ||||||||||||||||
体内研究 (In Vivo) | LX-7101 is advanced to Phase-I clinical trials as an intraocular pressure (IOP)-lowering agent for treatment of glaucoma. LX-7101 displays a significant IOP reduction at time points ranging from 1 h to 6 h post administration in rabbits[1]. Topical doses of LX-7101 are evaluated for tolerability on the eyes of mice, rats, and rabbits. It is well tolerated at doses up to 0.5% in non-GLP single dose studies. In the mouse IOP assay, LX-7101 (5%) achieved additional reduction of IOP (5.0 mmHg total reduction) compared to the 0.1% formulation and demonstrated a long duration of action, with IOP not returning to baseline until more than 8 h postdose[2]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 451.52 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C23H29N7O3 | ||||||||||||||||
CAS 号 | 1192189-69-7 | ||||||||||||||||
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 : 150 mg/mL(332.21 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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