LX7101
作者：齐岳
发布时间：2023-09-13
16:37:43
点击数：
产品名称：LX7101
产品描述：
| 产品描述 | LX7101 is an effective inhibitor of LIMK and ROCK2 (IC50: 24, 1.6, and 10 nM for LIMK1, LIMK2, and ROCK2, respectively). It also inhibits PKA (IC50 <1 nM). |
| 靶点活性 | LIMK2:1.6 nM, PKA:1 nM, LIMK1:24 nM, ROCK2:10 nM |
| 体外活性 | LX7101 is a dual LIM-kinase and ROCK inhibitor for the treatment of ocular hypertension and associated glaucoma. LX-7101 also shows effective inhibition of Akt1 (IC50<1 nM)[1]. The activity of LX7101 is primarily due to inhibition of LIMK2, under physiological conditions[2]. The overall selectivity of LX7101 for LIMK2 enhances the higher physiological ATP concentrations. |
| 体内活性 | Topical doses of LX-7101 are evaluated for tolerability in the eyes of mice, rats, and rabbits. It is well tolerated at doses up to 0.5% in non-GLP single-dose studies. LX-7101 is advanced to Phase-I clinical trials as intraocular pressure (IOP)-lowering agent for the treatment of glaucoma. LX-7101 shows a significant IOP reduction at time points ranging from 1 h to 6 h post-administration in rabbits[1]. LX-7101 (5%) achieved an additional reduction of IOP (5.0 mmHg total reduction) compared to the 0.1% formulation. It also demonstrated a long duration of action, in the mouse IOP assay, with IOP not returning to baseline until more than 8 h postdose[2]. |
| 分子量 | 451.52 |
| 分子式 | C23H29N7O3 |
| CAS No. | 1192189-69-7 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 150 mg/mL (332.21 mM),Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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