Description
RTICBM-189 is a Urea derivative and a CB1 allosteric modulator. RTICBM-189 showed no activity at >50 protein targets and excellent brain permeation but relatively low metabolic stability in rat liver microsomes. Pharmacokinetic studies in rats confirmed the excellent brain exposure of 31 with a brain/plasma ratio Kp of 2.0. Importantly, intraperitoneal administration of RTICBM-189 significantly and selectively attenuated the reinstatement of the cocaine-seeking behavior in rats without affecting locomotion.
Product information
CAS Number: 551909-15-0
Molecular Weight: 309.19
Formula: C15H14Cl2N2O
Chemical Name: N-(4-Chlorophenyl)-N'-[2-(3-chlorophenyl)ethyl]urea
Smiles: O=C(NC1=CC=C(Cl)C=C1)NCCC1C=CC=C(Cl)C=1
InChiKey: PPKIPROVSKBYAT-UHFFFAOYSA-N
InChi: InChI=1S/C15H14Cl2N2O/c16-12-4-6-14(7-5-12)19-15(20)18-9-8-11-2-1-3-13(17)10-11/h1-7,10H,8-9H2,(H2,18,19,20)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: To be determined
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
References:
- Nguyen T, Gamage TF, Finlay DB, Decker AM, Langston TL, Barrus D, Glass M, Li JX, Kenakin TP, Zhang Y. Development of 3-(4-Chlorophenyl)-1-(phenethyl)urea Analogues as Allosteric Modulators of the Cannabinoid Type-1 Receptor: RTICBM-189 is Brain Penetrant and Attenuates Reinstatement of Cocaine-Seeking Behavior. J Med Chem. 2021 Dec 20. doi: 10.1021/acs.jmedchem.1c01432. Epub ahead of print. PMID: 34929081
- Nguyen T, et al. Development of 3-(4-Chlorophenyl)-1-(phenethyl)urea Analogues as Allosteric Modulators of the Cannabinoid Type-1 Receptor: RTICBM-189 is Brain Penetrant and Attenuates Reinstatement of Cocaine-Seeking Behavior [published online ahead of print, 2021 Dec 20]. J Med Chem. 2021;10.1021/acs.jmedchem.1c01432.
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