LX7101

Research use only, not for human use.

LX7101 is a potent, dual LIMK and ROCK inhibitor with IC50 of 4.3/32//69/32/ nM for LIMK2/LIMK1/ROCK1/ROCK2, respectively.

LX7101 is a potent, dual LIMK and ROCK inhibitor with IC50 of 4.3/32//69/32/ nM for LIMK2/LIMK1/ROCK1/ROCK2, respectively; kinase selectivity are eveluated in a panel of binding assays including 78 different receptors and transporters at Cerep (only 5 have >60% inhibition at 10 uM); demonstrates high efficacy in mouse model of ocular hypertension, ans shows potential for the treatment of glaucoma.Other Indication Phase 2 Clinical.

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.

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.

LX-7101

Cell Cycle/DNA Damage

LIM Kinase (LIMK)

LIM Kinase (LIMK)

Other Indications

Other Disease

1192189-69-7

451.5215

C23H29N7O3

>98% (HPLC)

DMSO: ≥ 24 mg/mL

O=C(OC1=CC=CC(NC(C2(CN)CCN(C3=C4C(NC=C4C)=NC=N3)CC2)=O)=C1)N(C)C.[H]Cl

Carbamic acid, N,N-dimethyl-, 3-[[[4-(aminomethyl)-1-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinyl]carbonyl]amino]phenyl ester

(-20℃)

With Ice Pack

≥ 2 years