A positive allosteric modulator of μ-opioid receptors
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BMS 986122

Item No. 23269

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-(3-bromo-4-methoxyphenyl)-3-[(4-chlorophenyl)sulfonyl]-thiazolidine
CAS Number
313669-88-4
Molecular Formula
C16H15BrClNO3S2
Formula Weight
448.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 2 mg/ml
λmax
234 nm
SMILES
COC1=CC=C(C2N(S(C3=CC=C(Cl)C=C3)(=O)=O)CCS2)C=C1Br
InChi Code
InChI=1S/C16H15BrClNO3S2/c1-22-15-7-2-11(10-14(15)17)16-19(8-9-23-16)24(20,21)13-5-3-12(18)4-6-13/h2-7,10,16H,8-9H2,1H3
InChi Key
PNGJPVDGZNPZHY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $54

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    5 mg

    $250

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    Product Description

    BMS 986122 is a positive allosteric modulator of μ-opioid receptors that increases β-arrestin recruitment stimulated by endomorphin 1 (Item No. 23280) in U2OS-OPRM1 human osteosarcoma cells expressing μ-opioid receptors (EC50 = 3 μM).1 It potentiates endomorphin 1-induced inhibition of forskolin-stimulated adenylyl cyclase activity in CHO cells expressing human recombinant μ-opioid receptors (EC50 = 8.9 μM). BMS 986122 also enhances [35S]GTPγ binding stimulated by the μ-opioid agonist DAMGO (Item No. 21553) by 7- and 4.5-fold in C6μ glioma cell membranes that express μ-opioid receptors and mouse brain membranes, respectively.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Burford, N.T., Clark, M.J., Wehrman, T.S., et al. Discovery of positive allosteric modulators and silent allosteric modulators of the μ-opioid receptor. Proc. Natl. Acad. Sci. USA 110(26), 10830-10835 (2013).