1192189-69-7
1192189-69-7 structure
- Name: LX7101
- Chemical Name: 3-(4-(aminomethyl)-1-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamido)phenyl N.N-dimethylcarbamate
- CAS Number: 1192189-69-7
- Molecular Formula: C23H29N7O3
- Molecular Weight: 451.52100
- Catalog: Signaling Pathways Cell Cycle/DNA Damage ROCK
- Create Date: 2018-06-16 07:15:25
- Modify Date: 2024-01-11 14:58:05
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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.
| Name | 3-(4-(aminomethyl)-1-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamido)phenyl N.N-dimethylcarbamate |
|---|---|
| Synonyms |
LX7101
3-(4-(aminomethyl)-1-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamido)phenyl dimethylcarbamate 3-(4-(aminomethyl)-1-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamido)phenyldimethylcarbamate |
| Description | 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. |
|---|---|
| Related Catalog | |
| Target |
ROCK2:10 nM (IC50) LIMK2:1.6 nM (IC50) LIMK1:24 nM (IC50) PKA:1 nM (IC50) |
| 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 IC50 of 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]. |
| 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]. |
| References |
| Molecular Formula | C23H29N7O3 |
|---|---|
| Molecular Weight | 451.52100 |
| Exact Mass | 451.23300 |
| PSA | 129.47000 |
| LogP | 3.34900 |
| Storage condition | 2-8℃ |