LX7101

CAS No. 1192189-69-7

LX7101( LX-7101 )

Catalog No. M10664 CAS No. 1192189-69-7

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

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    LX7101
  • Note
    Research use only, not for human use.
  • Brief Description
    LX7101 is a potent, dual LIMK and ROCK inhibitor with IC50 of 4.3/32//69/32/ nM for LIMK2/LIMK1/ROCK1/ROCK2, respectively.
  • Description
    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.
  • 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. 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.
  • 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. 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.
  • Synonyms
    LX-7101
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    LIM Kinase (LIMK)
  • Recptor
    LIM Kinase (LIMK)
  • Research Area
    Other Indications
  • Indication
    Other Disease

Chemical Information

  • CAS Number
    1192189-69-7
  • Formula Weight
    451.5215
  • Molecular Formula
    C23H29N7O3
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥ 24 mg/mL
  • SMILES
    O=C(OC1=CC=CC(NC(C2(CN)CCN(C3=C4C(NC=C4C)=NC=N3)CC2)=O)=C1)N(C)C.[H]Cl
  • Chemical Name
    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

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Harrison BA, et al. ACS Med Chem Lett. 2014 Nov 24;6(1):84-8.
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