BMS-193885 is a potent, selective Y1 antagonist that is active in both acute and chronic animal models of food intake. Although it is active in vivo, it is not orally bioavailable due to poor intestinal absorption, so it is not being pursued for pharmaceutical development. BMS-193885 has been used as a pre-clinical proof of concept tool for showing efficacy of Y1 antagonism in treating obesity.
| Molecular Weight | 590.71 |
| Formula | C33H42N4O6 |
| CAS Number | 186185-03-5 |
| Solubility (25°C) | DMSO: ≥10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Zhenlin Yang, et al. Structural basis of ligand binding modes at the neuropeptide Y Y 1 receptor
| Related Neuropeptide Receptor Products |
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Neuropeptide Y (human, rat, mouse) TFA is involved in Alzheimer's disease (AD) and protects rat cortical neurons against β-Amyloid toxicity. |
| N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36)
N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36) is a selective agonist of neuropeptide Y Y2 receptor. |
| Neuropeptide Y (13-36), amide, human
Neuropeptide Y (13-36), amide, human is a selective neuropeptide Y2 receptor agonist. |
| Neuropeptide FF
Neuropeptide FF (NPFF), an octapeptide belonging to the RF-amide family of peptides, interacts with two distinct G-protein-coupled receptors, NPFF(1) and NPFF(2). |
| CART(55-102) (human)
CART(55-102)(human) is an endogenous satiety factor with potent appetite-suppressing activity. |
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