| Bioactivity | 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]. |
| Invitro | 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]. |
| Name | BMS-986187 |
| CAS | 684238-37-7 |
| Formula | C31H34O4 |
| Molar Mass | 470.60 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| Reference | [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. |
BMS-986187
CAS: 684238-37-7 F: C31H34O4 W: 470.60
BMS-986187 is an δ-opioid receptor-selective positive allosteric modulator (PAM) with an EC50 of 0.03 μM and a pKB of
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