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ML-184 (CAS 794572-10-4) LS-H142

CB1 antagonist, CB2 antagonist
LS-H142-500 / 500 µg / $185
LS-H142-1000 / 1000 µg / $205
LS-H142-5000 / 5000 µg / $355
LS-H142-10000 / 10000 µg / $515
USA Shipment Only
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Description: GPR55 is a G protein-coupled receptor that is weakly activated by some cannabinoids (CBs) at nM concentrations but displays a 5- to 10-fold greater stimulation in response to 1 µM lysophosphatidylinositol (LPI). ML-184 is a potent synthetic agonist of GPR55 (EC50 = 0.26 µM). It does not act at the related kynurenic acid receptor GPR35 and is a weak antagonist of CB1 and CB2 (IC50s = 21.8 and 15.1 µM, respectively). Like LPI, ML-184 induces phosphorylation of ERK1/2 and translocation of PKC beta II to the plasma membrane by activating GPR55. H142_ChemicalStructureImage.png
3-[[4-(2,3-dimethylphenyl)-1-piperazinyl]carbonyl]-N,N-dimethyl-4-(1-pyrrolidinyl)-benzenesulfonamide
CID-2440433
biochemical, chemical, antagonist
LS-H142
794572-10-4
C25H34N4O3S
≥98%
A crystalline solid
 
CC1=CC=CC(N2CCN(C(C3=CC(S(N(C)C)(=O)=O)=CC=C3N4CCCC4)=O)CC2)=C1C
InChI=1S/C25H34N4O3S/c1-19-8-7-9-23(20(19)2)28-14-16-29(17-15-28)25(30)22-18-21(33(31,32)26(3)4)10-11-24(22)27-12-5-6-13-27/h7-11,18H,5-6,12-17H2,1-4H3
VRSJAHQGJHDACS-UHFFFAOYSA-N
Shipped Ambient, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: CNR1 / CB1 related products

Usage Information

ML-184 is supplied as a crystalline solid. A stock solution may be made by dissolving the ML-184 in the solvent of choice. ML-184 is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF), which should be purged with an inert gas. The solubility of ML-184 in these solvents is approximately 1, 20, and 30 mg/ml. ML-184 is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, ML-184 should first be dissolved in DMF and then diluted with the aqueous buffer of choice. ML-184 has a solubility of approximately 0.2 mg/ml in a 1:4 solution of DMF:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Ryberg, E., Larsson, N., Sjögren, S., et al. The orphan receptor GPR55 is a novel cannabinoid receptor. Br. J. Pharmacol. 152, 1092-1101 (2007).
  2. Oka, S., Nakajima, K., Yamashita, A., et al. Identification of GPR55 as a lysophosphatidylinositol receptor. Biochem. Biophys. Res. Commun. 362, 928-934 (2007).
  3. Kotsikorou, E., Madrigal, K.E., Hurst, D.P., et al. Identification of the GPR55 agonist binding site using a novel set of high potency GPR55 selective ligands. Biochemistry 50(25), 5633-5647 (2011).

 


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