| Identification | Back Directory | [Name]
MK 0557 | [CAS]
328232-95-7 | [Synonyms]
MK 0557
CS-2471
MK0557;MK 0557
N'-Dicyanomethylene-N-(2,4,5-trichloro-phenyl)-hydrazinecarboxylic acid ethyl ester
N-[1-(2-fluorophenyl)pyrazol-3-yl]-1'-oxospiro[cyclohexane-4,3'-furo[3,4-c]pyridine]-1-carboxamide
trans-N-[1-(2-Fluorphenyl)-1H-pyrazol-3-yl]-1'-oxospiro[cyclohexane-1,3'(1'H)-furo[3,4-c]pyridine]-4-carboxamide
(1r,4r)-N-(1-(2-fluorophenyl)-1H-pyrazol-3-yl)-1'-oxo-1'H-spiro[cyclohexane-1,3'-furo[3,4-c]pyridine]-4-carboxamide
Spiro[cyclohexane-1,3'(1'H)-furo[3,4-c]pyridine]-4-carboxamide, N-[1-(2-fluorophenyl)-1H-pyrazol-3-yl]-1'-oxo-, trans- | [Molecular Formula]
C22H19FN4O3 | [MDL Number]
MFCD25976714 | [MOL File]
328232-95-7.mol | [Molecular Weight]
406.41 |
| Chemical Properties | Back Directory | [Melting point ]
240.0-240.6 °C | [Boiling point ]
708.7±60.0 °C(Predicted) | [density ]
1.46±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 5 mg/ml; DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml; DMSO: 3 mg/ml | [form ]
A crystalline solid | [pka]
13.40±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
MK-0557 is a potent antagonist of the neuropeptide Y (NPY) receptor Y5 (Kis = 1.3, 0.79, 0.74, and 1.4 nM for human, rhesus monkey, mouse, and rat receptors, respectively).1 It is >7,500-fold selective for Y5 over other receptors and lacks activity in a panel of 180 receptors, enzymes, and ion channels at concentrations up to 1 μM. MK-0557 increases intracellular calcium in CHO cells expressing the human Y5 receptor in a concentration-dependent manner. In vivo, MK-0557 (30 mg/kg) reduces body weight gain in wild-type and diet-induced obese mice. It also reduces retroperitoneal fat pad weight, epididymal and mesenteric fat pad weights, leptin levels, and food intake in lean mice fed a high-fat diet. | [Uses]
MK-0557 is a highly selective, orally available neuropeptide Y5 receptor antagonist with a Ki of 1.6 nM. | [in vivo]
MK-0557 antagonizes the effects of the NPY5R-selective agonist on body-weight gain and hyperphagia in C57BL/6J mice and significantly suppresses the body-weight gain in diet-induced obese (DIO) mice. When lean mice on regular chow are switched to a medium high-fat diet (4.2 kcal/g) and treated with MK-0557 at 30 mg/kg PO QD, MK-0557 causes a 40% reduction in
body-weight gain at day 35[2]. | [IC 50]
NPY Y5 receptor | [storage]
Store at -20°C | [References]
[1] Fichtner M, et al. Discovery and evaluation of spirocyclic derivatives as antagonists of the neuropeptide Y5 receptor. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2738-43. DOI:10.1016/j.bmcl.2012.02.098
[2] Erondu N, et al. Neuropeptide Y5 receptor antagonism does not induce clinically meaningful weight loss in overweight and obese adults. Cell Metab. 2006 Oct;4(4):275-82. DOI:10.1016/j.cmet.2006.08.002 |
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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
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