BMS-986187 is a δ-opioid receptor selective orthosteric modulator (PAM) with an EC50 of 0.03 μM and a pKB of 6.02 (~1 μM). bms-986187 has no observable PAM activity at the μ receptor (EC50=3 μM).
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.
Molecular Weight | 470.60 |
Formula | C31 H34 O4 |
CAS Number | 684238-37-7 |
Purity | >99% |
Solubility | N/A |
Storage | at -20°C |
Related Opioid Receptor Products |
---|
TRV-130
TRV 130 is a novel μ-opioid receptor (MOR) G protein-biased ligand; elicits robust G protein signaling(pEC50=8.1), with potency and efficacy similar to morphine, but with far less β-arrestin recruitment and receptor internalization. |
β-Casomorphin, human
β-Casomorphin, human is an opioid-like peptide that is an opioid receptor agonist. Sequence: Tyr-Pro-Phe-Val-Glu-Pro-Ile. |
β-Casomorphin, bovine
β-casomorphin, bovine (β-Casomorphin-7 (bovine)) is an opioid-active peptide with an IC50 value of 14 μM for binding to opioid receptors.Sequence:Tyr-Pro-Phe-Pro-Gly-Pro-Ile. |
EST73502
EST73502 is a selective, orally active, μ-opioid receptor (μ-opioid receptor/MOR) agonist and σ1 receptor (σ1R) antagonist that crosses the blood-brain barrier with Ki values of 64 nM and 118 nM for MOR and σ1R effects, respectively. EST73502 can be used in pain relief studies. |
(-)-Menthol
(-)-Menthol is a levo isomer of menthol and used as a cooling agent that strongly activates TRPM8. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.