| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
BMS-986187 targets the δ-opioid receptor (DOR), a G protein-coupled receptor that mediates the effects of endogenous opioid peptides such as enkephalins. It acts as a positive allosteric modulator (PAM) at this receptor, meaning it binds to a site distinct from the orthosteric (agonist) binding site and enhances the receptor's response to agonists. In the presence of the endogenous δ-opioid receptor agonist leu-enkephalin, BMS-986187 has an average EC50 value of 30 nM for β-arrestin recruitment. It exhibits 100-fold selectivity for the δ-opioid receptor over the μ-opioid receptor, with little to no PAM activity at the μ receptor at concentrations up to 3 μM.
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| ln Vitro |
In the presence of EC20 of leucine enkephalin (in CHO-OPRD1 cells) or endomorphin 1 (in CHO-OPRM1 cells), BMS-986187 (1 nM-100 uM) exhibits little to no action in the agonist mode but not in the PAM mode. In CHO-OPRD1 cells, it produces an EC50 of 48 nM, while in CHO-OPRM1 cells, it produces an EC50 of 2 μM [1].
In vitro, BMS-986187 acts as a δ-opioid receptor positive allosteric modulator with an EC50 of 30 nM for enhancing agonist-mediated β-arrestin recruitment. It enhances the affinity of [Leu5]-enkephalin, SNC 80, and TAN 67 for the δ-opioid receptor, amplifying opioid signaling. The compound has little to no activity in the absence of an agonist, demonstrating its pure allosteric modulator profile. BMS-986187 exhibits a pKB of 6.02 (~1 μM) and shows no observable PAM activity at the μ receptor (EC50 = 3 μM), confirming its selectivity for the δ-opioid receptor. |
| ln Vivo |
Specific in vivo activity data for BMS-986187 is not detailed in the provided search results. As a δ-opioid receptor positive allosteric modulator, it is being studied for its potential to enhance opioid signaling in a spatially and temporally restricted manner. By binding to an allosteric site, BMS-986187 amplifies opioid signaling, potentially allowing for lower doses of opioids to achieve effective analgesia. This strategy may help reduce the side effects associated with high-dose opioid therapy, including tolerance, dependence, and respiratory depression.
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| Enzyme Assay |
The in vitro activity of BMS-986187 is assessed using cell-based functional assays, such as β-arrestin recruitment assays. Cells expressing the δ-opioid receptor are treated with a sub-maximal concentration of an agonist (e.g., leu-enkephalin) in the presence of varying concentrations of BMS-986187. The potentiation of β-arrestin recruitment is measured to determine the EC50. For receptor binding studies, competitive binding assays can be performed using radiolabeled δ-opioid receptor ligands to assess the compound's ability to enhance agonist affinity.
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| Cell Assay |
For cellular assays, cell lines stably expressing the δ-opioid receptor, such as CHO or HEK293 cells, are cultured in appropriate media. Cells are pre-incubated with various concentrations of BMS-986187 (typically 1 nM to 10 μM) for 15-30 minutes, followed by stimulation with a sub-maximal concentration of a δ-opioid receptor agonist. The activation of downstream signaling pathways (e.g., β-arrestin recruitment, cAMP inhibition, or G protein activation) is measured using standard assay formats such as BRET, FRET, or ELISA-based cAMP detection. The EC50 is determined from dose-response curves.
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| Animal Protocol |
In vivo, BMS-986187 is typically administered orally to animal models. The compound is formulated in a suitable vehicle (e.g., 5% DMSO, 40% PEG300, 5% Tween-80, and 50% ddH2O) and administered at various doses (typically 1-30 mg/kg). Efficacy is assessed in pain models, such as the formalin test, hot plate test, or tail-flick test, by measuring the compound's ability to enhance the analgesic effects of sub-effective doses of δ-opioid receptor agonists. Pharmacodynamic studies involve measuring the modulation of pain thresholds and assessing the compound's effects on opioid-related side effects.
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| ADME/Pharmacokinetics |
BMS-986187 has a molecular weight of 470.61 g/mol and a molecular formula of C31H34O4. It is soluble in DMSO at up to 20 mM. For in vivo administration, it can be formulated in 10% DMSO, 40% PEG300, 5% Tween-80, and 45% saline. The compound should be stored as a powder at -20°C under desiccated conditions. Specific pharmacokinetic parameters such as bioavailability, half-life, and volume of distribution are not detailed in the provided search results.
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| Toxicity/Toxicokinetics |
Specific toxicity data for BMS-986187 is not available in the provided search results. As a δ-opioid receptor positive allosteric modulator, its safety profile is still under investigation. The compound is intended for research purposes only and is not approved for human or veterinary use. Standard laboratory safety precautions should be followed when handling the compound. Comprehensive toxicological studies are required to establish its full safety profile for potential therapeutic applications.
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| References | |
| Additional Infomation |
BMS-986187 is a research compound that has been developed as a selective δ-opioid receptor positive allosteric modulator. It is not approved for clinical use and is intended for research purposes only. The compound is a valuable tool for studying δ-opioid receptor function and for exploring the therapeutic potential of allosteric modulation of the opioid system. Its ability to enhance opioid signaling without directly activating the receptor may offer advantages for pain management with reduced side effects.
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| Molecular Formula |
C31H34O4
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| Molecular Weight |
470.609
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| Exact Mass |
470.245
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| Elemental Analysis |
C, 79.12; H, 7.28; O, 13.60
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| CAS # |
684238-37-7
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| PubChem CID |
17379334
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
627.0±55.0 °C at 760 mmHg
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| Flash Point |
265.5±31.5 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.604
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| LogP |
6.19
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
35
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| Complexity |
876
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1CC(C)(C)CC2OC3CC(C)(C)CC(=O)C=3C(C3C=CC(OCC4C=CC=CC=4C)=CC=3)C1=2
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| InChi Key |
UEKIYVKPQNKSDI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H34O4/c1-19-8-6-7-9-21(19)18-34-22-12-10-20(11-13-22)27-28-23(32)14-30(2,3)16-25(28)35-26-17-31(4,5)15-24(33)29(26)27/h6-13,27H,14-18H2,1-5H3
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| Chemical Name |
3,3,6,6-tetramethyl-9-[4-[(2-methylphenyl)methoxy]phenyl]-4,5,7,9-tetrahydro-2H-xanthene-1,8-dione
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| Synonyms |
BMS-986187; BMS986187; BMS 986187
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~53.12 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1249 mL | 10.6245 mL | 21.2490 mL | |
| 5 mM | 0.4250 mL | 2.1249 mL | 4.2498 mL | |
| 10 mM | 0.2125 mL | 1.0625 mL | 2.1249 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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