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MedChemExpressModel ML-7 hydrochloride -110448-33-4

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ML-7 hydrochloride is a naphthalene sulphonamide derivative, potently inhibits MLCK (IC50=300 nM). ML-7 hydrochloride also inhibits YAP/TAZ.
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ML-7 hydrochloride

MCE China:ML-7 hydrochloride

Brand:MedChemExpress (MCE)

Cat. No.HY-15417

CAS:110448-33-4

Purity:99.63%

Storage:4°C, sealed storage, away from moisture *In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

Shipping:Room temperature in continental US; may vary elsewhere.

Description:ML-7 hydrochloride is a naphthalene sulphonamide derivative, potently inhibits MLCK (IC50=300 nM). ML-7 hydrochloride also inhibits YAP/TAZ.

In Vitro:ML-7 hydrochloride inhibits rabbit portal vein α1-adrenoceptor NSCC with IC50 of 0.8 μM[1]. The myosin light chain kinase (MLCK) inhibitor ML-7 hydrochloride (3 μ M and 10 μM) also attenuates the Dexmedetomidine (DMT)-induced contraction (p[2].

In Vivo:In sham operated animals Evans Blue extravasation is not different between ML-7 hydrochloride and vehicle group (sham+vehicle: 0.26±0.02 OD/g; sham+ML-7: 0.26±0.02 OD/g). After CCI inhibition of MLCK with ML-7 results in a significant lower amount of intracerebral Evans Blue compared to vehicle treated animals (CCI+vehicle: 0.42±0.04 OD/g; CCI+ML-7: 0.35±0.05 OD/g, p=0.048)[3].

Animal Administration:Mice[3]Mice are treated with intraperitoneal injection of the selective MLCK inhibitor ML-7 (1 mg/kg) or vehicle solution (0.9% NaCl,control group) 1 h prior to and 6 h after trauma. Hemispheric brain water content and neurological function are measured 24 h after controlled cortical impact (CCI) in animals randomized to: (i) vehicle+sham surgery, (ii) vehicle+CCI, (iii) ML-7+shamsurgery or (iv) ML-7+CCI (n=8 per group) and 15 min after CCI in animals randomized to: (i) vehicle+sham surgery, (ii) vehicle+CCI, (iii) ML-7+sham surgery or (iv) ML-7+CCI (n=6 per group). Mice are treated with intraperitoneal injection of the selective MLCK inhibitor ML-7 (1 mg/kg) or vehicle solution (0.9% NaCl, control group) 1 h prior to and 6 h after trauma. Evans Blue extravasation is determined 24 h after surgery in animals randomized to: (i) vehicle + CCI or (ii) ML-7+CCI (n=5 per group) and in animals randomized to (iii) vehicle + sham surgery or (iv) ML-7+sham surgery (n=6 per group). ICP is measured 24 h CCI and sham surgery.

IC50 & Target:IC50: 300 nM (MLCK)[1] In Vitro ML-7 hydrochloride inhibits rabbit portal vein α1-adrenoceptor NSCC with IC50 of 0.8 μM[1]. The myosin light chain kinase (MLCK) inhibitor ML-7 hydrochloride (3 μ M and 10 μM) also attenuates the Dexmedetomidine (DMT)-induced contraction (p[2]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> ML-7 hydrochloride Related Antibodies

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References:

[1]. Shi J, et al. Myosin light chain kinase-independent inhibition by ML-9 of murine TRPC6 channels expressed in HEK293cells. Br J Pharmacol. 2007 Sep;152(1):122-31.  [Content Brief]

[2]. Yu J, et al. Dexmedetomidine-Induced Contraction in the Isolated Endothelium-Denuded Rat Aorta Involves PKC-δ-mediated JNK Phosphorylation. Int J Med Sci. 2015 Sep 4;12(9):727-36  [Content Brief]

[3]. Luh C, et al. Inhibition of myosin light chain kinase reduces brain edema formation after traumatic brain injury. J Neurochem. 2010 Feb;112(4):1015-25.  [Content Brief]

[4]. Pobbati AV, et, al. A combat with the YAP/TAZ-TEAD oncoproteins for cancer therapy. Theranostics. 2020 Feb 18;10(8):3622-3635.  [Content Brief]

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