WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H527097
CAS#: 684238-37-7
Description: BMS-986187 is a novel Potent and Selective Positive Allosteric Modulators of the delta-Opioid Receptor.
Hodoodo Cat#: H527097
Name: BMS-986187
CAS#: 684238-37-7
Chemical Formula: C31H34O4
Exact Mass: 470.25
Molecular Weight: 470.609
Elemental Analysis: C, 79.12; H, 7.28; O, 13.60
Synonym: BMS 986187; BMS986187; BMS-986187
IUPAC/Chemical Name: 3,3,6,6-Tetramethyl-9-(4-((2-methylbenzyl)oxy)phenyl)-3,4,5,6,7,9-hexahydro-1H-xanthene-1,8(2H)-dione
InChi Key: UEKIYVKPQNKSDI-UHFFFAOYSA-N
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
SMILES Code: O=C1C(C(C2=CC=C(OCC3=CC=CC=C3C)C=C2)C4=C(CC(C)(C)CC4=O)O5)=C5CC(C)(C)C1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | Potent positive allosteric modulator of δ receptors. |
| In vitro activity: | BMS 986187 stimulated GTPγ35S binding in a concentration‐dependent manner, giving a potency value (EC50) of 301 ± 85 nM. significantly less potent than SNC80 (19 ± 11nM). Reference: Br J Pharmacol. 2019 Jun; 176(11): 1649–1663. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6514288/ |
| In vivo activity: | TBD |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 9.4 | 20.00 | |
| DMF | 1.0 | 2.12 | |
| DMF:PBS (pH 7.2) (1:2) | 0.3 | 0.70 |
The following data is based on the product molecular weight 470.61 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. Stanczyk MA, Livingston KE, Chang L, Weinberg ZY, Puthenveedu MA, Traynor JR. The δ-opioid receptor positive allosteric modulator BMS 986187 is a G-protein-biased allosteric agonist. Br J Pharmacol. 2019 Jun;176(11):1649-1663. doi: 10.1111/bph.14602. Epub 2019 Apr 14. PMID: 30710458; PMCID: PMC6514288. |
| In vitro protocol: | 1. Stanczyk MA, Livingston KE, Chang L, Weinberg ZY, Puthenveedu MA, Traynor JR. The δ-opioid receptor positive allosteric modulator BMS 986187 is a G-protein-biased allosteric agonist. Br J Pharmacol. 2019 Jun;176(11):1649-1663. doi: 10.1111/bph.14602. Epub 2019 Apr 14. PMID: 30710458; PMCID: PMC6514288. |
| In vivo protocol: | TBD |
1: Livingston KE, Stanczyk MA, Burford N, Alt A, Canals M, Traynor JR. Pharmacological Evidence for a Putative Conserved Allosteric Site on Opioid Receptors. Mol Pharmacol. 2017 Dec 12. pii: mol.117.109561. doi: 10.1124/mol.117.109561. [Epub ahead of print] PubMed PMID: 29233847.
2: Shang Y, Yeatman HR, Provasi D, Alt A, Christopoulos A, Canals M, Filizola M. Proposed Mode of Binding and Action of Positive Allosteric Modulators at Opioid Receptors. ACS Chem Biol. 2016 May 20;11(5):1220-9. doi: 10.1021/acschembio.5b00712. Epub 2016 Feb 17. PubMed PMID: 26841170; PubMed Central PMCID: PMC4950826.
