LX7101

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Menge 100mg
ArtNr HY-12659-100mg
Eclass 6.1 30220300
Eclass 9.0 32160605
Lieferbar
Synonyms
LX-7101
CAS No.
1192189-69-7
Purity
>98%
MW
4515215
Formula
C23H29N7O3
Solubility
DMSO: >= 24 mg/mL
Biological 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.


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 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].
Menge: 100mg
Lieferbar: In stock
Listenpreis: 2.626,79 €
Preis: 2.626,79 €
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