[CAS NO. 1192189-69-7] LX7101
PRODUCTS SPECIFICATIONS [1192189-69-7]
DESCRIPTION [1192189-69-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 451.52 |
| Molecular Formula | C23H29N7O3 |
| SMILES | NCC1(C(NC2=CC(OC(N(C)C)=O)=CC=C2)=O)CCN(C3=C4C(NC=C4C)=NC=N3)CC1 |
1 Publications Citing Use of MCE
Summary
IC50 & Target
IC50: 24 nM (LIMK1), 1.6 nM (LIMK2), 10 nM (ROCK2), <1 nM (PKA) [1]
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 IC 50 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01528111 | Lexicon Pharmaceuticals |
Primary Open-angle Glaucoma|Ocular Hypertension
|
March 2012 | Phase 1|Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 150 mg/mL ( 332.21 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.2147 mL | 11.0737 mL | 22.1474 mL |
| 5 mM | 0.4429 mL | 2.2147 mL | 4.4295 mL |
| 10 mM | 0.2215 mL | 1.1074 mL | 2.2147 mL |
References
- [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.
