BMS 193885

BMS 193885

Catalog Number:
L002372333APE
Mfr. No.:
APE-B7327
Price:
$620
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      • Overview
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          Background

          BMS-193885 is a potent and selective neuropeptide Y1 receptor antagonist with IC50 of 5.9nM.
          Neuropeptide Y receptor 1 is G-protein coupled receptors and implicated in the modulation of food intake and energy homeostasis. Neuropeptide Y1 is expressed in many tissues including the hippocampus, hypothalamus, amygdala and the cortex of the brain as well as in peripheral tissues heart, kidney, skeletal muscle. The localization and expression suggests their involvement in the regulation of food intake and body weight.
          In cellular culture, BMS-193885 displayed functional antagonism of Neuropeptide Y1 in a
          forskolin-stimulated c-AMP production assay using CHO cells expressing the human Y(1) receptor 1.
          In vivo, administration of BMS-193885 at a dosage of 10mg/kg leads to 1h neuropeptide Y-induced food intake in rat and the spontaneous overnight food consumpetion 2 . Chronic administration of BMS-193885 (10 mg/kg) i.p. for 44 days significantly reduced food intake and the rate of body weight gain as compared to their control without developing tolerance or affecting water intake 2.

          1. Poindexter GS, Bruce MA, LeBoulluec KL, et al. Dihydropyridine neuropeptide Y Y(1) receptor antagonists. Bioorganic & medicinal chemistry letters. 2002;12(3):379-382.
          2. Antal-Zimanyi I, Bruce MA, Leboulluec KL, et al. Pharmacological characterization and appetite suppressive properties of BMS-193885, a novel and selective neuropeptide Y(1) receptor antagonist. European journal of pharmacology. 2008;590(1-3):224-232.

      • Properties
        • Categories
          Competitive NPY Y1 receptor antagonist
          Alternative Name
          (S)-2-hydroxypropanoic acid compound with (Z)-N-(3-(3,5-bis(methoxycarbonyl)-2,6-dimethyl-1,4-dihydropyridin-4-yl)phenyl)-N'-(3-(4-(3-methoxyphenyl)piperidin-1-yl)propyl)carbamimidic acid (1:1)
          CAS Number
          679839-66-8
          Molecular Formula
          C33H42N4O6·C3H6O3
          Molecular Weight
          680.79
          Appearance
          Pale yellow solid
          Purity
          98.00%
          Solubility
          <68.08mg/ml in DMSO; <13.62mg/ml in H2O
          Storage
          Desiccate at RT
          SMILES
          CC(N1)=C(C(OC)=O)C(C(C(OC)=O)=C1C)C2=CC(N/C(O)=N/CCCN3CCC(C4=CC(OC)=CC=C4)CC3)=CC=C2.C[[email protected]@](O)([H])C(O)=O

          * For Research Use Only

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