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COR659

🥰Excellent
Catalog No. T36520Cas No. 544450-68-2

COR659 is a 2-acylaminothiophene derivative able to suppress alcohol and chocolate self-administration in rats, likely via positive allosteric modulation of the GABAB receptor and antagonism/inverse agonism at the cannabinoid CB1 receptor.

COR659

COR659

🥰Excellent
Purity: 99.56%
Catalog No. T36520Cas No. 544450-68-2
COR659 is a 2-acylaminothiophene derivative able to suppress alcohol and chocolate self-administration in rats, likely via positive allosteric modulation of the GABAB receptor and antagonism/inverse agonism at the cannabinoid CB1 receptor.
Pack SizePriceAvailabilityQuantity
1 mg$48In Stock
2 mg$69In Stock
5 mg$118In Stock
10 mg$188In Stock
25 mg$341In Stock
50 mg$476In Stock
100 mg$653In Stock
200 mg$888In Stock
1 mL x 10 mM (in DMSO)$130In Stock
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Purity:99.56%
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Product Introduction

Bioactivity
Description
COR659 is a GABAB positive allosteric modulator (PAM) . COR659 suppresses alcohol and chocolate self-administration in rats[1].
COR659 apparently exerts its effects via a composite mechanism, including positive allosteric modulation of the GABAB receptor and an action at the cannabinoid CB1 receptor[3].
COR659 (0, 2.5, 5 and 10 mg/kg) treatment is completely ineffective on lever-responding (FR10) for regular food pellets in food-deprived Wistar rats[1].COR659 is able to suppress lever-responding for a sucrose solution in sP rats and a chocolate solution in Wistar rats[2]. Animal Model: Male sP and Wistar rats[1].
[1]. Paola Maccioni, et al. Suppressing effect of COR659 on alcohol, sucrose, and chocolate self-administration in rats: involvement of the GABA B and cannabinoid CB 1 receptors. Psychopharmacology (Berl). 2017 Sep;234(17):2525-2543. [2]. Francesca Ferlenghi, et al. The GABA B receptor positive allosteric modulator COR659: In vitro metabolism, in vivo pharmacokinetics in rats, synthesis and pharmacological characterization of metabolically protected derivatives. Eur J Pharm Sci. 2020 Dec 1;155:105544. [3]. Paola Maccioni, et al. Anti-addictive properties of COR659 - Additional pharmacological evidence and comparison with a series of novel analogues. Alcohol. 2019 Mar;75:55-66.
In vitro
COR659 exerts its effects through a composite mechanism, including positive allosteric modulation of the GABAB receptor and action at the cannabinoid CB1 receptor [3].
In vivo
COR659 (0, 2.5, 5, and 10 mg/kg) treatment is completely ineffective on lever-responding (FR10) for regular food pellets in food-deprived Wistar rats[1]. However, COR659 suppresses lever-responding for a sucrose solution in sP rats and a chocolate solution in Wistar rats[2]. Animal Model: Male sP and Wistar rats[1].
Chemical Properties
Molecular Weight337.82
FormulaC16H16ClNO3S
Cas No.544450-68-2
SmilesCCc1c(C)sc(NC(=O)c2ccc(Cl)cc2)c1C(=O)OC
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 33.33 mg/mL (98.66 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.9602 mL14.8008 mL29.6016 mL148.0078 mL
5 mM0.5920 mL2.9602 mL5.9203 mL29.6016 mL
10 mM0.2960 mL1.4801 mL2.9602 mL14.8008 mL
20 mM0.1480 mL0.7400 mL1.4801 mL7.4004 mL
50 mM0.0592 mL0.2960 mL0.5920 mL2.9602 mL

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