3-Thiophenecarboxylic acid, 2-[(4-chlorobenzoyl)amino]-4-ethyl-5-methyl-, methyl ester manufacturers
- COR659
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- $48.00 / 1mg
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2024-11-19
- CAS:544450-68-2
- Min. Order:
- Purity: 99.56%
- Supply Ability: 10g
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| | 3-Thiophenecarboxylic acid, 2-[(4-chlorobenzoyl)amino]-4-ethyl-5-methyl-, methyl ester Basic information |
| Product Name: | 3-Thiophenecarboxylic acid, 2-[(4-chlorobenzoyl)amino]-4-ethyl-5-methyl-, methyl ester | | Synonyms: | 3-Thiophenecarboxylic acid, 2-[(4-chlorobenzoyl)amino]-4-ethyl-5-methyl-, methyl ester;COR659;Methyl 2-(4-chlorobenzamido)-4-ethyl-5-methylthiophene-3-carboxylate;COR 659,Gamma-aminobutyric acid Receptor,sucrose,inhibit,chocolate,γ-Aminobutyric acid Receptor,GABA Receptor,COR-659,Inhibitor,COR659,alcohol;COR659, 10 mM in DMSO | | CAS: | 544450-68-2 | | MF: | C16H16ClNO3S | | MW: | 337.82 | | EINECS: | | | Product Categories: | | | Mol File: | 544450-68-2.mol | ![3-Thiophenecarboxylic acid, 2-[(4-chlorobenzoyl)amino]-4-ethyl-5-methyl-, methyl ester Structure](CAS/20200611/GIF/544450-68-2.gif) |
| | 3-Thiophenecarboxylic acid, 2-[(4-chlorobenzoyl)amino]-4-ethyl-5-methyl-, methyl ester Chemical Properties |
| storage temp. | 4°C, away from moisture and light | | solubility | DMSO: 33.33 mg/mL (98.66 mM) | | form | Solid | | color | Off-white to light yellow |
| | 3-Thiophenecarboxylic acid, 2-[(4-chlorobenzoyl)amino]-4-ethyl-5-methyl-, methyl ester Usage And Synthesis |
| Uses | COR659 is a potent and effective GABAB positive allosteric modulator (PAM). COR659 suppresses alcohol and chocolate self-administration in rats[1]. | | Biological Activity | COR659 is a potent positive allosteric modulator (PAM) of GABAB. It alleviates drug addiction to alcohol and chocolate in rats. | | in vitro | COR659 apparently exerts its effects via a composite mechanism, including positive allosteric modulation of the GABA B receptor and an action at the cannabinoid CB1 receptor. | | 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.
It is able to suppress lever-responding for a sucrose solution in sP rats and a chocolate solution in Wistar rats.
| Animal Model: | Male sP and Wistar rats. | | Dosage: | 0, 2.5, 5 and 10 mg/kg. | | Administration: | Intraperitoneally (administered 30 min before the start of the self-administration, reinstatement, and locomotor activity sessions.). | | Result: | The magnitude of the reducing effect of the compound on number of lever-responses for alcohol averaged approximately 30, 55, and 70%, in com parison to the vehicle-treated rat group, in the rat groups treated with 2.5, 5, and 10 mg/kg COR659, respectively.
The magnitude of the reducing effect of COR659 on number of lever-responses for alcohol averaged approximately 20, 40, and 80%, in comparison to the vehicletreated rat group, in the rat groups treated with 2.5, 5, and 10 mg/kg COR659, respectively.
| | | References | [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. DOI:10.1007/s00213-017-4644-3
[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. DOI:10.1007/s00213-017-4644-3
[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. DOI:10.1016/j.alcohol.2018.05.007 |
| | 3-Thiophenecarboxylic acid, 2-[(4-chlorobenzoyl)amino]-4-ethyl-5-methyl-, methyl ester Preparation Products And Raw materials |
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