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6-Iodopravadoline

Catalog No. T14204 CAS 164178-33-0

Synonyms: AM630

6-Iodopravadoline (AM630) is an antagonist of CB2 (Ki: 31.2 nM). And it shows 165-fold selectivity more than CB1 receptors.

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6-Iodopravadoline, CAS 164178-33-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 34.00
2 mg	In stock	$ 46.00
5 mg	In stock	$ 67.00
10 mg	In stock	$ 97.00
25 mg	In stock	$ 221.00
50 mg	In stock	$ 363.00
100 mg	In stock	$ 578.00
1 mL * 10 mM (in DMSO)	In stock	$ 106.00

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Purity: 99.86%

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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.

Synonyms	AM630
Molecular Weight	504.36
Formula	C23H25IN2O3
CAS No.	164178-33-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (99.14 mM), Sonification is recommended.

References and Literature

1. Garcia-Gutierrez, Maria S., et al. Chronic blockade of cannabinoid CB2 receptors induces anxiolytic-like actions associated with alterations in GABAA receptors. British Journal of Pharmacology (2012), 165(4), 951-964. 2. Patil, Mayur., et al. Cannabinoid receptor antagonists AM251 and AM630 activate TRPA1 in sensory neurons. Neuropharmacology (2011), 61(4), 778-788. 3. Geng, D. C., et al. Inhibition of titanium particle-induced inflammatory osteolysis through inactivation of cannabinoid receptor 2 by AM630. Journal of Biomedical Materials Research, Part A (2010), 95A(1), 321-326. 4. Mukherjee, Sutapa., et al. Species comparison and pharmacological characterization of rat and human CB2 cannabinoid receptors. European Journal of Pharmacology (2004), 505(1-3), 1-9. 5. Sun L, et al. Endocannabinoid activation of CB1 receptors contributes to long-lasting reversal of neuropathic pain by repetitive spinal cord stimulation. Eur J Pain. 2017 May;21(5):804-814.

Citations

1. Zhang L, Yi Y, Wang T, et al.25-Hydroxycholesterol inhibits classical swine fever virus entry into porcine alveolar macrophages by depleting plasma membrane cholesterol.Veterinary Microbiology.2023: 109668.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library GPCR Compound Library Covalent Inhibitor Library Bioactive Compounds Library Max NO PAINS Compound Library Bioactive Compound Library

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Keywords

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

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