A selective GPR55 antagonist
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ML-193

Item No. 15184

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-[[(3,4-dimethyl-5-isoxazolyl)amino]sulfonyl]phenyl]-6,8-dimethyl-2-(2-pyridinyl)-4-quinolinecarboxamide
CAS Number
713121-80-3
Synonyms
  • CID-1261822
Molecular Formula
C28H25N5O4S
Formula Weight
527.6
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMF:PBS (pH 7.2) (1:4): 0.1 mg/mlDMSO: 1 mg/mlEthanol: 0.1 mg/ml
λmax
261, 279 nm
SMILES
O=C(C1=C(C=C(C)C=C2C)C2=NC(C3=CC=CC=N3)=C1)NC4=CC=C(S(NC5=C(C)C(C)=NO5)(=O)=O)C=C4
InChi Code
InChI=1S/C28H25N5O4S/c1-16-13-17(2)26-22(14-16)23(15-25(31-26)24-7-5-6-12-29-24)27(34)30-20-8-10-21(11-9-20)38(35,36)33-28-18(3)19(4)32-37-28/h5-15,33H,1-4H3,(H,30,34)
InChi Key
HTSLEZOTMYUPLU-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    ML-193 is a potent antagonist of GPR55 (IC50 = 221 nM).1,2 It displays selectivity for GPR55 over CB1, CB2, and GPR35. ML-193 inhibits GPR55-dependent ERK phosphorylation (IC50 = 65 nM) and blocks translocation of PKCβII.1 ML-193 blocks increases in intracellular calcium levels induced by lysophosphatidylinositol (LPI) in dissociated rat periaqueductal gray neurons and modulates pain perception in LPI-treated rats.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Heynen-Genel, S., Dahl, R., Shi, S., et al. Screening for selective ligands for GPR55. NIH Molecular Libraries (2010).

    2. Kotsikorou, E., Sharir, H., Shore, D.M., et al. Identification of the GPR55 antagonist binding site using a novel set of high-potency GPR55 selective ligands. Biochemistry 52(52), 9456-9469 (2013).

    3. Deliu, E., Sperow, M., Console-Bram, L., et al. The lysophosphatidylinositol receptor GPR55 modulates pain perception in the periaqueductal gray. Mol. Pharmacol. 88(2), 265-272 (2015).