A positive allosteric modulator of δ-opioid receptors
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BMS 986187

Item No. 21549

Technical Information
Formal Name
3,4,5,6,7,9-hexahydro-3,3,6,6-tetramethyl-9-[4-[(2-methylphenyl)methoxy]phenyl]-1H-xanthene-1,8(2H)-dione
CAS Number
684238-37-7
Molecular Formula
C31H34O4
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 1 mg/mlDMF:PBS(pH7.2) (1:2): 0.33 mg/mlDMSO: Slightly solubleEthanol: Slightly soluble
λmax
226, 291 nm
SMILES
CC1=C(COC2=CC=C(C3C(C(CC(C)(C)C4)=O)=C4OC(CC(C)(C)C5)=C3C5=O)C=C2)C=CC=C1
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
InChi Key
UEKIYVKPQNKSDI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    BMS 986187 is a positive allosteric modulator of δ-opioid receptors.1 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, but has little to no activity in the absence of an agonist. It is 100-fold selective for δ- over µ-opioid receptors in the presence of leu-enkephalin and the endogenous µ-opioid receptor agonist endomorphin I, respectively.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Burford, N.T., Livingston, K.E., Canals, M., et alDiscovery, synthesis, and molecular pharmacology of selective positive allosteric modulators of the δ-opioid receptor. J. Med. Chem. 58(10), 4220-4229 (2015).