Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 56.00 | |
5 mg | In stock | $ 163.00 | |
10 mg | In stock | $ 289.00 | |
25 mg | In stock | $ 579.00 | |
50 mg | 6-8 weeks | $ 987.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 235.00 |
Description | 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). |
Targets&IC50 | ROCK2:10 nM, LIMK1:24 nM, PKA:1 nM, LIMK2:1.6 nM |
In vitro | 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. |
In vivo | 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]. |
Molecular Weight | 451.52 |
Formula | C23H29N7O3 |
CAS No. | 1192189-69-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 150 mg/mL (332.21 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
LX7101 1192189-69-7 Cell Cycle/Checkpoint Cytoskeletal Signaling Stem Cells Tyrosine Kinase/Adaptors ROCK LIM Kinase PKA inhibit Inhibitor LX 7101 Rho-associated protein kinase LX-7101 Rho-associated kinase Rho-kinase ROK inhibitor