| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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Purity: ≥98%
MK-0557 (MK0557) is a novel, highly selective, orally bioavailable neuropeptide Y5 receptor antagonist with anti-obesity effects. It inhibits neuropeptide Y5 receptor with a Ki of 1.6 nM. MK-0557 has the potential to treat obesity because it may prevent weight gain following weight loss that is brought about by a very-low-calorie diet (VLCD). Strongly orexigenic neuropeptide Y (NPY) is known, and antagonistic effects on NPY Y1 and NPY Y5 receptors (NPYxR) are thought to represent a promising therapeutic target for obesity prevention.
| Targets |
NPY Y5 receptor
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| ln Vitro |
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| ln Vivo |
MK-0557 significantly inhibits the body-weight gain in diet-induced obese (DIO) mice and counteracts the effects of the NPY5R-selective agonist on hyperphagia and body-weight gain in C57BL/6J mice. Day 35 body-weight gain is reduced by 40% when lean mice fed regular chow are given a medium high-fat diet (4.2 kcal/g) and administered MK-0557 at a dose of 30 mg/kg PO QD[2].
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| References |
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| Additional Infomation |
MK0557 has been investigated for the treatment of Schizophrenia and Paranoid Schizophrenia.
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| Molecular Formula |
C22H19FN4O3
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|---|---|
| Molecular Weight |
406.4097
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| Exact Mass |
406.144
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| Elemental Analysis |
C, 65.02; H, 4.71; F, 4.67; N, 13.79; O, 11.81
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| CAS # |
328232-95-7
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| Related CAS # |
935765-76-7 (alternate)
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| PubChem CID |
11491176
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| Appearance |
White to off-white solid powder
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| LogP |
3.022
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
30
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| Complexity |
669
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1=C([H])C([H])=C([H])C([H])=C1N1C([H])=C([H])C(=N1)N([H])C(C1([H])C([H])([H])C([H])([H])C2(C3C([H])=NC([H])=C([H])C=3C(=O)O2)C([H])([H])C1([H])[H])=O
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| InChi Key |
RMYZIRFUCOMQRH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H19FN4O3/c23-17-3-1-2-4-18(17)27-12-8-19(26-27)25-20(28)14-5-9-22(10-6-14)16-13-24-11-7-15(16)21(29)30-22/h1-4,7-8,11-14H,5-6,9-10H2,(H,25,26,28)
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| Chemical Name |
N-[1-(2-fluorophenyl)pyrazol-3-yl]-1'-oxospiro[cyclohexane-4,3'-furo[3,4-c]pyridine]-1-carboxamide
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| Synonyms |
MK-0557; MK 0557; MK0557
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~200 mg/mL (~492.1 mM)
H2O: < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (12.30 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4606 mL | 12.3028 mL | 24.6057 mL | |
| 5 mM | 0.4921 mL | 2.4606 mL | 4.9211 mL | |
| 10 mM | 0.2461 mL | 1.2303 mL | 2.4606 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00482430 | Completed | Drug: MK0557 Drug: Comparator: Placebo (unspecified) |
Schizophrenia Paranoid Schizophrenia |
Merck Sharp & Dohme LLC | September 2007 | Phase 2 |
| NCT00533598 | Completed | Drug: MK0557 | Obesity | Merck Sharp & Dohme LLC | September 2002 | Phase 2 |
| NCT00092872 | Completed | Drug: MK0557 | Obesity | Merck Sharp & Dohme LLC | November 2003 | Phase 3 |
| NCT00092859 | Completed | Drug: MK0557 | Obesity | Merck Sharp & Dohme LLC | August 2003 | Phase 3 |
| NCT00533481 | Completed | Drug: MK0557 | Obesity | Merck Sharp & Dohme LLC | February 2004 | Phase 2 |
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