貨號	規格	價格	上海	北京	武漢	南京	購買數量
S82266-5mg	≥99%	￥2000.00 S82266-5mg ￥2000.00 2-3天	0 貨期：2-3天	-	-	-
S82266-10mg	≥99%	￥3500.00 S82266-10mg ￥3500.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

LX7101 is a potent inhibitor of LIMK and ROCK2 with IC50 values of 24, 1.6 and 10 nM for LIMK1, LIMK2 and ROCK2, respectively; also inhibits PKA with an IC50 less than 1 nM.

產品描述：

LX7101 is a potent inhibitor of LIMK and ROCK2 with IC50 values of 24, 1.6 and 10 nM for LIMK1, LIMK2 and ROCK2, respectively; also inhibits PKA with an IC50 less than 1 nM.

靶點：

ROCK2:10 nM (IC50);LIMK2:1.6 nM (IC50);LIMK1:24 nM (IC50);PKA:1 nM (IC50);ROCK;?LIMKinase;?PKA

體外研究：

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 IC50 of less than 1 nM. 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

體內研究：

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. 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

參考文獻：

1. Boland S, et al. Design, synthesis and biological characterization of selective LIMK inhibitors. Bioorganic & Medicinal Chemistry Letters (2015), 25(18), 4005-4010. 2. Harrison BA, et al. Discovery and Development of LX7101, a Dual LIM-Kinase and ROCK Inhibitor for the Treatment of Glaucoma. ACS Medicinal Chemistry Letters (2015), 6(1), 84-88.

溶解性：

soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.215 ml	11.074 ml	22.147 ml
5 mM	0.443 ml	2.215 ml	4.429 ml
10 mM	0.221 ml	1.107 ml	2.215 ml
50 mM	0.044 ml	0.221 ml	0.443 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。

參考文獻

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