| CAS NO: | 109376-83-2 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 416.28 |
|---|---|
| Formula | C15H17IN2O2S |
| CAS No. | 109376-83-2 (free base); |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: ≥ 30mg/mL |
| Water: N/A | |
| Ethanol: N/A | |
| Chemical Name | Hexahydro-1-[(5-iodo-1-naphthalenyl)sulfonyl]-1H-1,4-diazepine |
| Synonyms | ML-7; ML-7 ML7. |
| SMILES Code | O=S(N1CCNCCC1)(C2=C3C=CC=C(I)C3=CC=C2)=O |
| 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<0.05 versus control)[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 Exp | 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. |
| 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. [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. [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 |
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