MedKoo Cat#: 527097 | Name: BMS-986187
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

BMS-986187 is a novel Potent and Selective Positive Allosteric Modulators of the delta-Opioid Receptor.

Chemical Structure

BMS-986187
BMS-986187
CAS#684238-37-7

Theoretical Analysis

MedKoo Cat#: 527097

Name: BMS-986187

CAS#: 684238-37-7

Chemical Formula: C31H34O4

Exact Mass: 470.2457

Molecular Weight: 470.61

Elemental Analysis: C, 79.12; H, 7.28; O, 13.60

Price and Availability

Size Price Availability Quantity
25mg USD 250.00 2 Weeks
50mg USD 450.00 2 Weeks
100mg USD 750.00 2 Weeks
200mg USD 1,250.00 2 Weeks
500mg USD 2,650.00 2 Weeks
1g USD 3,850.00 2 Weeks
2g USD 5,950.00 2 Weeks
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Related CAS #
No Data
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
Product Data
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 mg/mL mM
Solubility
DMSO 9.4 20.00
DMF 1.0 2.12
DMF:PBS (pH 7.2) (1:2) 0.3 0.70
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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.