URB602

SKU: orb1304022

Description

URB602 is a non-competitive, selective monoacylglycerol lipase (MGL) inhibitor with an IC50 of 28±4 μM against rat brain MGL. This small molecule is a valuable research tool for studying endocannabinoid signaling in neurological and metabolic research, applicable in both in vitro and in vivo experimental models.

Research Area

Infectious Disease & Virology, Metabolism Research

Key Properties

• CAS Number: 565460-15-3
• MW: 295.38
• Purity: 99.64% (May vary between batches)
• Formula: C₁₉H₂₁NO₂
• SMILES: O=C(Nc1cccc(c1)-c1ccccc1)OC1CCCCC1
• Target: Lipase,Antibacterial
• Solubility: DMSO:55 mg/mL (186.2 mM);10% DMSO+90% Corn Oil:2.5 mg/mL (8.46 mM)

Bioactivity

• Target IC50:
  MGL:28±4 μM
• In Vivo:
  URB602 (20-40 mg/kg) can reduce upper GI transit and slow colonic propulsion. In whole gut transit, URB602 dose-dependently inhibits transit (P<0.05) compared with the vehicle control group. The inhibitory action of URB602 (40 mg/kg) on whole gut transit is absent in these mice, demonstrating CB1 receptor involvement in the inhibitory action. During the early phase of the formalin test, URB602 decreases the AUC of pain behavior for JZL184 (ED50: 0.06±0.028 μg) and for URB602 (ED50: 120±51.3 μg) in adult male Sprague-Dawley rats. Both MGL inhibitors also suppress pain behavior during the late phase of formalin pain for JZL184 (ED50: 0.03±0.011 μg) and for URB602 (ED50: 66±23.9 μg).
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• In Vitro:
  The apparent Km of MGL for 2-AG is 24±1.7 μM and the Vmax is 1814±51 nmol/min/mg protein; with URB602, the Km is 20±0.4 μM and the Vmax is 541±20 nmol/min/mg protein (n=4). When organotypic slice cultures of rat forebrain are incubated with URB602 (100 μM), both baseline and Ca2+-ionophore-stimulated 2-arachidonoylglycerol (2-AG) concentrations are increased. URB602 weakly inhibits recombinant MGL (IC50: 223±63 μM) through a rapid and noncompetitive mechanism.
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Storage & Handling

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

Alternative Names

Bacterial, Inhibitor, inhibit, rat brain MGL, URB 602, URB602, URB-602

Compound Identifiers

PubChem CID

10979337