Powder: -20°C for 3 years | In solvent: -80°C for 1 year
6-Iodopravadoline (AM630) is an antagonist of CB2 (Ki: 31.2 nM). And it shows 165-fold selectivity more than CB1 receptors.
説明 | 6-Iodopravadoline (AM630) is an antagonist of CB2 (Ki: 31.2 nM). And it shows 165-fold selectivity more than CB1 receptors. |
ターゲット&IC50 | CB2:(ki)31.2 nM |
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[3]. 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[4]. 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[2]. 6-Iodopravadoline (0, 50, 100, and 200 nM) is not toxic to RAW264.7 cells. |
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[1]. 6-Iodopravadoline (AM630) (2, 3 mg/kg, i.p.) significantly reduces the time spent in the light box, compared with vehicle group. |
別名 | AM630 |
分子量 | 504.36 |
分子式 | C23H25IN2O3 |
CAS No. | 164178-33-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (99.14 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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6-Iodopravadoline 164178-33-0 GPCR/G Protein Cannabinoid Receptor Inhibitor Iodopravadoline selective AM 630 6Iodopravadoline competitive 6 Iodopravadoline AM-630 anxiolytic twitches inhibit AM630 stimulated inhibitor