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6-Iodopravadoline (AM630) is an antagonist of CB2 (Ki: 31.2 nM). And it shows 165-fold selectivity more than CB1 receptors.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $34 | In Stock | |
2 mg | $46 | In Stock | |
5 mg | $67 | In Stock | |
10 mg | $97 | In Stock | |
25 mg | $221 | In Stock | |
50 mg | $363 | In Stock | |
100 mg | $578 | In Stock | |
1 mL x 10 mM (in DMSO) | $106 | In Stock |
Description | 6-Iodopravadoline (AM630) is an antagonist of CB2 (Ki: 31.2 nM). And it shows 165-fold selectivity more than CB1 receptors. |
Targets&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. |
Alias | AM630 |
Molecular Weight | 504.36 |
Formula | C23H25IN2O3 |
Cas No. | 164178-33-0 |
Smiles | C(=O)(C=1C=2C(N(CCN3CCOCC3)C1C)=CC(I)=CC2)C4=CC=C(OC)C=C4 |
Relative Density. | 1.49 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline: 1 mg/mL (1.98 mM), In vivo: Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. DMSO: 33 mg/mL (65.43 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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