ML-193

SKU: orb1217710

Description

ML-193 is a potent and selective GPR55 antagonist( IC50 : 221 nM). It shows more than 27-fold selectivity for GPR55 over GPR35, CB1 and CB2, and can improve the motor and the sensorimotor deficits of Parkinson’s disease (PD) rats.

Key Properties

• CAS Number: 713121-80-3
• MW: 527.59
• Purity: >98% (HPLC)
• Formula: C₂₈H₂₅N₅O₄S
• SMILES: Cc1c(NS(c(cc2)ccc2NC(c2cc(-c3ncccc3)nc3c(C)cc(C)cc23)=O)(=O)=O)onc1C
• Target: Cannabinoid Receptor
• Solubility: In Vitro: DMSO : 33.33 mg/mL (63.17 mM)

Bioactivity

• In Vivo:
  ML193 (1 and 5 μg/rat; intra-striatal at a rate of 1 μL/min) attenuates sensorimotor deficits and slip steps, increases motor coordination in PD rats. Animal model: Male Wistar rats (200-250 g) were induced experimental Parkinson by 6-hydroxydopamine (6-OHDA, 10 μg/rat). Dosage: 1 and 5 μg/rat. Administration: Injected into the right striatum at a rate of 1 μL/min. Result: Increased the time on the rotarod, decreased latency to remove the label and slip steps in 6-OHDA-lesioned rats.
• In Vitro:
  ML-193 (0.01-100 μM; pretreated for 15 min) inhibits β-arrestin trafficking induced by L-α-lysophophosphatidylinositol (LPI, 10 μM) and ML186 (1 μM) with IC50s of 0.22 μM and 0.12 μM, respectively. ML-193 (0.01-10 μM; pretreated for 30 min) decreases the LPI-mediated ERK1/2 phosphorylation, with an IC50 of 0.2 μM in U2OS cells. ML-193 (5 μM; pretreated for 30 min) attenuates the GPR55 agonists induced increases in hNSCs proliferation rates. ML-193 (5 μM; 10 d) attenuates the ML184-induced increases in hNSCs differentiation.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CID 1261822

Quick Database Links

Gene Symbol

Cannabinoid Receptor