RF 9 is a selective NPFF receptor antagonist (Ki values are 58 and 75 nM at hNPFF1 and hNPFF2 receptors respectively). Displays selectivity over several related receptors including NPY Y1 GPR10, GPR54, GPR103 and the opioid receptors. Blocks NPFF-induced hypothermia and increases in atrial blood pressure and heart rate, and prevents opioid-induced tolerance associated with hyperalgesia in vivo.
| Molecular Weight | 482.62 |
| Formula | C26H38N6O3 |
| CAS Number | 876310-60-0 |
| Solubility (25°C) | DMSO ≥ 10 mg/mL Water ≥ 5 mg/mL |
| Storage | -20°C, dry, sealed |
| 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.
| Related Neuropeptide Receptor Products |
|---|
| Neuropeptide Y (human, rat, mouse) TFA
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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