| Size | Price | Stock | Qty |
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| Targets |
BMS-986188 targets the δ-opioid receptor (DOR), a G protein-coupled receptor (GPCR) that is a member of the opioid receptor family. DOR is involved in the modulation of pain, mood, and other physiological functions. BMS-986188 is a positive allosteric modulator (PAM) of DOR. Unlike orthosteric agonists, PAMs bind to a site distinct from the endogenous ligand-binding site and enhance the receptor's response to its endogenous agonist, leu-enkephalin. This mechanism can provide a more nuanced modulation of receptor activity, potentially leading to a more favorable side-effect profile.
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| ln Vitro |
In vitro, BMS-986188 is a potent and selective positive allosteric modulator of the δ-opioid receptor. Its activity is typically measured using functional assays, such as β-arrestin recruitment or G protein activation assays. In the presence of the opioid receptor agonist leu-enkephalin, BMS-986188 potentiates the recruitment of β-arrestin, demonstrating its PAM activity. It has an EC50 of 0.05 μM for this effect. The compound's selectivity for DOR over other opioid receptor subtypes has been confirmed, though specific values are not detailed.
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| ln Vivo |
In vivo activity data for BMS-986188 is limited, as the compound is primarily used as a research tool in in vitro studies. However, as a selective PAM of the δ-opioid receptor, it has potential applications in studying the role of DOR in pain, mood disorders, and other conditions. The compound could be used in animal models to investigate the effects of DOR modulation on nociception, reward, and emotional behavior. However, specific in vivo protocols and results are not detailed in standard product descriptions.
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| Enzyme Assay |
In vitro assays for BMS-986188 measure its binding and functional activity at the δ-opioid receptor. Functional assays, such as β-arrestin recruitment assays, are used to characterize its PAM activity. Cells co-expressing the DOR and a β-arrestin reporter are treated with a sub-maximal concentration of the orthosteric agonist leu-enkephalin and varying concentrations of BMS-986188. The potentiation of β-arrestin recruitment is measured, and the EC50 is determined from the dose-response curve. These assays confirm the compound's activity as a PAM of DOR.
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| Cell Assay |
In vitro cell-based assays for BMS-986188 are conducted using cells expressing the δ-opioid receptor. Cells are treated with BMS-986188 in the presence or absence of the endogenous agonist leu-enkephalin. The activation of downstream signaling pathways, such as the inhibition of cAMP accumulation or the activation of G protein-coupled inwardly rectifying potassium channels (GIRKs), is measured. The compound's ability to potentiate the effects of leu-enkephalin is assessed. These assays confirm the compound's PAM activity at the DOR.
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| Animal Protocol |
In vivo animal experiments for BMS-986188 are not extensively described in the available literature. As a research compound, its use in vivo would be determined by the specific research question being addressed. A typical protocol for studying a DOR PAM would involve its administration to animal models of pain or other conditions. However, specific protocols for BMS-986188 are not detailed.
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| ADME/Pharmacokinetics |
BMS-986188 has a molecular weight of 535.47 g/mol and a molecular formula of C30H31BrO4. It has a CAS number of 1776115-10-6. It is a solid compound. For storage, it is recommended to keep the powder at -20°C. Detailed pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have not been extensively characterized. As a research compound, its stability is maintained by proper storage as a dry powder.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for BMS-986188 is not provided in standard product descriptions. As a research compound, its toxicity profile has not been extensively characterized. BMS-986188 is a selective PAM of the δ-opioid receptor, and its toxicity would be related to its effects on DOR-mediated signaling in normal tissues. However, comprehensive toxicological studies have not been reported. As with all research chemicals, standard laboratory safety precautions should be followed when handling BMS-986188.
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| References | |
| Additional Infomation |
BMS-986188 is a research compound and is not approved for any clinical or therapeutic use. It is a selective positive allosteric modulator (PAM) of the δ-opioid receptor (DOR), with an EC50 of 0.05 μM. It was developed to study the pharmacology of the δ-opioid receptor and its role in pain and other physiological processes. Its mechanism of action involves potentiating the receptor's response to its endogenous agonist, leu-enkephalin. BMS-986188 is a valuable research tool for studying opioid receptor biology and allosteric modulation.
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| Molecular Formula |
C30H31BRO4
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| Molecular Weight |
535.46874833107
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| Exact Mass |
534.14
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| Elemental Analysis |
C, 67.29; H, 5.84; Br, 14.92; O, 11.95
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| CAS # |
1776115-10-6
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| PubChem CID |
118737394
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
6.1
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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 |
882
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1(CC2=C(C(C3=C(O2)CC(CC3=O)(C)C)C4=CC=C(C=C4)OCC5=CC=CC=C5Br)C(=O)C1)C
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| InChi Key |
BBCHHZHONQIODT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C30H31BrO4/c1-29(2)13-22(32)27-24(15-29)35-25-16-30(3,4)14-23(33)28(25)26(27)18-9-11-20(12-10-18)34-17-19-7-5-6-8-21(19)31/h5-12,26H,13-17H2,1-4H3
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| Chemical Name |
9-[4-[(2-bromophenyl)methoxy]phenyl]-3,3,6,6-tetramethyl-4,5,7,9-tetrahydro-2H-xanthene-1,8-dione
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| Synonyms |
BMS-986188, BMS986188; BMS-986188;
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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 |
| 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 : ~62.5 mg/mL (~116.72 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 | 1.8675 mL | 9.3376 mL | 18.6752 mL | |
| 5 mM | 0.3735 mL | 1.8675 mL | 3.7350 mL | |
| 10 mM | 0.1868 mL | 0.9338 mL | 1.8675 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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