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  3. LX7101

LX7101 

Cat. No.: HY-12659 Purity: 99.29%
Handling Instructions

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.

For research use only. We do not sell to patients.

LX7101 Chemical Structure

LX7101 Chemical Structure

CAS No. : 1192189-69-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 286 In-stock
Estimated Time of Arrival: December 31
2 mg USD 156 In-stock
Estimated Time of Arrival: December 31
5 mg USD 288 In-stock
Estimated Time of Arrival: December 31
10 mg USD 480 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1680 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2640 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

    LX7101 purchased from MCE. Usage Cited in: Sci Rep. 2018 Aug 2;8(1):11585.

    Western blot analysis of GFAP protein levels in LX7101 and DMSO-treated iNPC-KO lines. GAPDH is used as a loading control.

    View All ROCK Isoform Specific Products:

    • Biological Activity

    • Technical Information

    • Purity & Documentation

    • References

    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].

    Clinical Trial
    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 24 mg/mL (53.15 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    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
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Molecular Weight

    451.52

    Formula

    C₂₃H₂₉N₇O₃

    CAS No.

    1192189-69-7

    SMILES

    NCC1(C(NC2=CC(OC(N(C)C)=O)=CC=C2)=O)CCN(C3=C4C(NC=C4C)=NC=N3)CC1

    Shipping

    Room temperature in continental US; may vary elsewhere

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    Product Name:
    LX7101
    Cat. No.:
    HY-12659
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    LX7101

    Cat. No.: HY-12659