2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor
  4. BMS-986187

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).

For research use only. We do not sell to patients.

BMS-986187 Chemical Structure

BMS-986187 Chemical Structure

CAS No. : 684238-37-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

BMS-986187 Related Antibodies

Top Publications Citing Use of Products

View All Opioid Receptor Isoform Specific Products:

View All Isoforms
μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

IC50 & Target

δ Opioid Receptor/DOR

 

Cellular Effect
Cell Line Type Value Description References
CHO EC50
0.03 μM
Compound: 2, BMS-986187
Positive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assay
Positive allosteric modulation of human delta opioid receptor-1 expressed in CHO cells assessed as potentiation of leu-enkephalin-induced response after 90 mins by beta-arrestin recruitment assay
[PMID: 25901762]
CHO EC50
2.6 μM
Compound: 2, BMS-986187
Positive allosteric modulation of human mu opioid receptor-1 expressed in CHO cells assessed as potentiation of endomorphin 1-induced response after 90 mins by beta-arrestin recruitment assay
Positive allosteric modulation of human mu opioid receptor-1 expressed in CHO cells assessed as potentiation of endomorphin 1-induced response after 90 mins by beta-arrestin recruitment assay
[PMID: 25901762]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BMS-986187 Related Antibodies
Molecular Weight

470.60

Formula

C31H34O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=C(C=CC=C1)COC2=CC=C(C=C2)C3C4=C(OC(CC(C)(C5)C)=C3C5=O)CC(C)(C)CC4=O
Shipping

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)

Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (10.62 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1249 mL 10.6247 mL 21.2495 mL
5 mM 0.4250 mL 2.1249 mL 4.2499 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.66%

SDS (252 KB)

COA (252 KB) HNMR (262 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1249 mL 10.6247 mL 21.2495 mL 53.1237 mL
5 mM 0.4250 mL 2.1249 mL 4.2499 mL 10.6247 mL
10 mM 0.2125 mL 1.0625 mL 2.1249 mL 5.3124 mL
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BMS-986187 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BMS-986187684238-37-7BMS986187BMS 986187Opioid Receptorδ-opioidPAMμ-receptorleu-enkephalinCHO-OPRD1 cellendomorphin 1Inhibitorinhibitorinhibit

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