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BMS 986187

Names

[ CAS No. ]:
684238-37-7

[ Name ]:
BMS 986187

[Synonym ]:
1H-Xanthene-1,8(2H)-dione, 3,4,5,6,7,9-hexahydro-3,3,6,6-tetramethyl-9-[4-[(2-methylphenyl)methoxy]phenyl]-
3,3,6,6-Tetramethyl-9-{4-[(2-methylbenzyl)oxy]phenyl}-3,4,5,6,7,9-hexahydro-1H-xanthene-1,8(2H)-dione

Biological Activity

[Description]:

BMS-986187 is an δ-opioid receptor-selective positive allosteric 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)[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Opioid Receptor
Signaling Pathways >> Neuronal Signaling >> Opioid Receptor
Research Areas >> Neurological Disease

[In Vitro]

BMS-986187 (1 nM-100 uM) produces little or no activity in agonist mode, but in PAM mode (in the presence of an EC20 of leu-enkephalin (in CHO-OPRD1 cells) or endomorphin 1 (in CHO-OPRM1 cells)) produces a response with an EC50 of 48 nM in CHO-OPRD1 cells and 2 μM in CHO-OPRM1 cells[1].

[References]

[1]. Neil T Burford, et al. Discovery, synthesis, and molecular pharmacology of selective positive allosteric modulators of the δ-opioid receptor. J Med Chem. 2015 May 28;58(10):4220-9.

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
627.0±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C31H34O4

[ Molecular Weight ]:
470.599

[ Flash Point ]:
265.5±31.5 °C

[ Exact Mass ]:
470.245697

[ LogP ]:
6.19

[ Vapour Pressure ]:
0.0±1.8 mmHg at 25°C

[ Index of Refraction ]:
1.604

[ Storage condition ]:
-20°C

Related Compounds