Chemical Name: 1,4-Dihydro-4-[3-[[[[3-[4-(3-methoxyphenyl)-1-piperidinyl]propyl]amino]carbonyl]amino]phenyl]-2,6-dimethyl-3,5-pyridinedicarboxylic acid 3,5-dimethyl ester L-Lactate
Purity: ≥99% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Potent, competitive neuropeptide (NPY) Y1 antagonist (Ki = 3.3 nM, IC50 = 5.9 nM) that displays > 47, > 100, > 160, > 160 and > 160-fold selectivity over σ1, α1, Y2, Y4 and Y5 receptors respectively. Reduces food intake and body weight via central Y1 inhibition and is brain penetrant.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
68.08
100
water
13.62
20
Preparing Stock Solutions
The following data is based on the product molecular weight 680.79. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
1.47 mL
7.34 mL
14.69 mL
5 mM
0.29 mL
1.47 mL
2.94 mL
10 mM
0.15 mL
0.73 mL
1.47 mL
50 mM
0.03 mL
0.15 mL
0.29 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Poindexteret al (2004) Dihydropyridine neuropeptide Y Y1 receptor antagonists 2: bioisosteric urea replacements Bioorg.Med.Chem. 12 507 PMID: 14723969
Antal-Zimanyiet al (2008) Pharmacological characterization and appetite suppressive properties of BMS-193885, a novel and selective neuropeptide Y1 receptor antagonist Eur.J.Pharmacol. 590 224 PMID: 18573246
Poindexteret al (2002) Dihydropyridine neuropeptide Y Y1 receptor antagonists. Bioorg.Med.Chem.Letts. 12 379 PMID: