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Cat. No. M21375
BMS-986187  Structure
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Biological Activity

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).

Chemical Information
Molecular Weight 470.60
Formula C31 H34 O4
CAS Number 684238-37-7
Solubility (25°C) N/A
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.


[1] Jesse J DiCello, et al. Am J Physiol Gastrointest Liver Physiol. Positive allosteric modulation of endogenous delta opioid receptor signaling in the enteric nervous system is a potential treatment for gastrointestinal motility disorders

[2] M Alexander Stanczyk, et al. Br J Pharmacol. The δ-opioid receptor positive allosteric modulator BMS 986187 is a G-protein-biased allosteric agonist

[3] Kathryn E Livingston, et al. Mol Pharmacol. Pharmacologic Evidence for a Putative Conserved Allosteric Site on Opioid Receptors

[4] Yi Shang, et al. ACS Chem Biol. Proposed Mode of Binding and Action of Positive Allosteric Modulators at Opioid Receptors

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Keywords: BMS-986187 supplier, Opioid Receptor, inhibitors, activators

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