An antagonist of NYP receptor Y5
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MK-0557

Item No. 22134

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
trans-N-[1-(2-fluorophenyl)-1H-pyrazol-3-yl]-1'-oxo-spiro[cyclohexane-1,3'(1'H)-furo[3,4-c]pyridine]-4-carboxamide
CAS Number
328232-95-7
Molecular Formula
C22H19FN4O3
Formula Weight
406.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 3 mg/ml
λmax
271 nm
SMILES
O=C(O1)C2=C(C=NC=C2)[C@]31CC[C@H](C(NC4=NN(C5=CC=CC=C5F)C=C4)=O)CC3
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)/t14-,22-
InChi Key
RMYZIRFUCOMQRH-CAJLXGCNSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    25 mg

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Erondu, N., Gantz, I., Musser, B., et al. Neuropeptide Y5 receptor antagonism does not induce clinically meaningful weight loss in overweight and obese adults. Cell Metab. 4(4), 275-282 (2006).