Chemical Structure : TXX-522
CAS No.:
2047608-84-2
TXX-522
(TXX522)
Catalog No.: PC-28693Not For Human Use, Lab Use Only.
TXX-522 is a potent, selective and peripherally restricted cannabinoid 1 receptor (CB1R) antagonist/inverse agonist with Ki and IC50 of 0.15 uM and 0.17 uM respectively, >100-fold selecive over CB2 receptor.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
TXX-522 is a potent, selective and peripherally restricted cannabinoid 1 receptor (CB1R) antagonist/inverse agonist with Ki and IC50 of 0.15 uM and 0.17 uM respectively, >100-fold selecive over CB2 receptor.
binds with the CB1R in a mode similar to that of SR141716A.
TXX-522 shows good binding, CB1R-selectivity (over the CB2R), and functional antagonist activities in a range of in vitro molecular and cellular assays.
TXX-522 shows minimal brain penetration.
TXX-522 has good oral bioavailability and a potent anti-obesity effect, and ameliorates insulin resistance in high-fat diet-induced obese mice.
Physicochemical Properties
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M.Wt
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478.78
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Formula
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C20H14Cl3N5OS
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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1-(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazol-3-yl)-3-(thiazol-2-yl)urea
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References
1. Chen W, et al. Front Pharmacol. 2017 Oct 5;8:707.
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