6-Iodopravadoline

SKU: orb1308667

Description

AM630 is a potent and selective cannabinoid CB2 receptor antagonist with a Ki of 31.2 nM, exhibiting 165-fold selectivity over the CB1 receptor. This compound is widely used in vitro and in vivo to investigate CB2 receptor function in immune modulation, neuroinflammation, and pain research.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 164178-33-0
• MW: 504.36
• Purity: 99.29% (May vary between batches)
• Formula: C₂₃H₂₅IN₂O₃
• SMILES: C(=O)(C=1C=2C(N(CCN3CCOCC3)C1C)=CC(I)=CC2)C4=CC=C(OC)C=C4
• Target: Cannabinoid Receptor
• Solubility: DMSO:25 mg/mL (49.57 mM);10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline:1 mg/mL (1.98 mM)

Bioactivity

• Target IC50:
  CB2:(ki)31.2 nM
• In Vivo:
  6-Iodopravadoline (AM630) (1, 2 or 3 mg/kg, i.p., twice a day) produces a significant anxiolytic effect, increasing the time spent in the light box at all of the doses used. 6-Iodopravadoline (AM630) (2, 3 mg/kg, i.p.) significantly reduces the time spent in the light box, compared with vehicle group.
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• In Vitro:
  6-Iodopravadoline is comparable in value in both TRPA1 and TRPV1/TRPA1 expressing CHO cells (2 and 4.6 μM, respectively). 6-Iodopravadoline (100 nM) substantially inhibits osteoclastogenesis in cultures with RANKL and Ti particles in a dose-dependent manner. 6-Iodopravadoline (1 μM) blocks the CP-55,940 dose response with EC50 of 170 nM at human and EC50 of 110 nM at rat cannabinoid CB2 receptor. The AM251 and 6-Iodopravadoline (AM630)-evoked Ca2+ influxes into TG sensory neurons aere concentration-dependent, and fitted. The EC50 for AM251 and 6-Iodopravadoline are 7.37 μM and 15.6 μM, respectively. AM251 and 6-Iodopravadoline activate TRPA1 in TG sensory neurons. AM251 and 6-Iodopravadoline activation of TRPA1 is modulated by TRPV1. 6-Iodopravadoline (0, 50, 100, and 200 nM) is not toxic to RAW264.7 cells.
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Storage & Handling

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

Alternative Names

Inhibitor, inhibit, Iodopravadoline, competitive, CB2, CB, 6 Iodopravadoline, 6Iodopravadoline, 6-Iodopravadoline, AM 630, AM630, AM-630, anxiolytic, Cannabinoid Receptor, CannabinoidReceptor, stimulated, selective, twitches

Compound Identifiers

PubChem CID

4302963