Bioactivity | LX7101 monohydrochloride is a potent dual LIM-kinase and ROCK inhibitor with IC50s of 24 nM, 1.6 nM, 10 nM and <1 nM for LIMK1, LIMK2, ROCK2 and PKA, respectively. LX7101 monohydrochloride proves significantly selective for LIMK2 with IC50 values of 4.3 nM and 32 nM for LIMK2 and LIMK1 at 2 μM ATP, respectively. LX7101 monohydrochloride has the potential for ocular hypertension and associated glaucoma research[1][2]. |
In Vivo | LX7101 (200 μg/40 μL 滴眼液) monohydrochloride 在眼压正常的新西兰白兔 (NZW) 中给药后 1 小时至 6 小时的时间点,眼压 (IOP) 显著降低[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
CAS | 2319882-48-7 |
Formula | C23H30ClN7O3 |
Molar Mass | 487.98 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |