PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor with Kis of 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM, 16 nM for Rat BB1 and BB2 receptors, respectively; PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells.
| Molecular Weight | 584.67 |
| Formula | C32H36N6O5 |
| CAS Number | 204067-01-6 |
| Form | Solid |
| Solubility (25°C) | DMSO 115 mg/mL (ultrasonic) |
| Storage | 4°C, 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 Bombesin Receptor Products |
|---|
| RC-3095 TFA
RC-3095 TFA is a selective bombesin/gastrin releasing peptide receptor (GRPR) antagonist. |
| Litorin
Litorin, an amphibian bombesin peptide derivative, is an bombesin receptor agonist. |
| (D-Phe6, Leu-NHEt13, des-Met14)-Bombesin (6-14)
(D-Phe6,Leu-NHEt13,des-Met14)-Bombesin (6-14) is a bombesin (BBN) antagonist and can be used for the research of cancer. |
| BIM 23042
BIM 23042, a certain somatostatin (SS) octapeptide analogue, is a selective neuropeptide neuromedin B receptor (NMB-R, BB1) antagonist. |
| BIM-26226
BIM-26226, gastrin-releasing peptide, is a potent and selective antagonist of bombesin receptor. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
