Basic information Safety Supplier Related

MK 0557

Basic information Safety Supplier Related

MK 0557 Basic information

Product Name:
MK 0557
Synonyms:
  • MK 0557
  • 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
  • N'-Dicyanomethylene-N-(2,4,5-trichloro-phenyl)-hydrazinecarboxylic acid ethyl ester
  • CS-2471
  • MK0557;MK 0557
  • Spiro[cyclohexane-1,3'(1'H)-furo[3,4-c]pyridine]-4-carboxamide, N-[1-(2-fluorophenyl)-1H-pyrazol-3-yl]-1'-oxo-, trans-
  • N-[1-(2-fluorophenyl)pyrazol-3-yl]-1'-oxospiro[cyclohexane-4,3'-furo[3,4-c]pyridine]-1-carboxamide
CAS:
328232-95-7
MF:
C22H19FN4O3
MW:
406.41
Mol File:
328232-95-7.mol
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MK 0557 Chemical Properties

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
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MK 0557 Usage And Synthesis

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). 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

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

MK 0557Supplier

Shanghai Boyle Chemical Co., Ltd.
Tel
Email
sales@boylechem.com
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Email
sales@BioChemBest.com
Bide Pharmatech Ltd.
Tel
400-164-7117 13681763483
Email
product02@bidepharm.com
Hangzhou J&H Chemical Co., Ltd.
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0571-87396432
Email
sales@jhechem.com
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
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MK 0557(328232-95-7)Related Product Information