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

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 98 In-stock
Solution
10 mM * 1 mL in DMSO USD 98 In-stock
Solid
5 mg USD 95 In-stock
10 mg USD 150 In-stock
25 mg USD 290 In-stock
50 mg USD 420 In-stock
100 mg USD 650 In-stock
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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

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  • Purity & Documentation

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  • 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].

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 : 25 mg/mL (53.12 mM; Need ultrasonic; 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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Purity & Documentation
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
15 mM 0.1417 mL 0.7083 mL 1.4166 mL 3.5416 mL
20 mM 0.1062 mL 0.5312 mL 1.0625 mL 2.6562 mL
25 mM 0.0850 mL 0.4250 mL 0.8500 mL 2.1249 mL
30 mM 0.0708 mL 0.3542 mL 0.7083 mL 1.7708 mL
40 mM 0.0531 mL 0.2656 mL 0.5312 mL 1.3281 mL
50 mM 0.0425 mL 0.2125 mL 0.4250 mL 1.0625 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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