Urea, N-(4-chlorophenyl)-N'-[2-(3-chlorophenyl)ethyl]-

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CAS:551909-15-0
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Urea, N-(4-chlorophenyl)-N'-[2-(3-chlorophenyl)ethyl]- manufacturers

  • RTICBM-189
  • RTICBM-189 pictures
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  • 2024-11-19
  • CAS:551909-15-0
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Urea, N-(4-chlorophenyl)-N'-[2-(3-chlorophenyl)ethyl]- Basic information
Product Name:Urea, N-(4-chlorophenyl)-N'-[2-(3-chlorophenyl)ethyl]-
Synonyms:Urea, N-(4-chlorophenyl)-N'-[2-(3-chlorophenyl)ethyl]-;RTICBM-189;Brain,Inhibitor,RTICBM-189,inhibit,Cocaine,RTICBM 189,Allosteric,Penetrant,Cannabinoid Receptor,Seeking,CB1,RTICBM189,Behavior;RTICBM-189, 10 mM in DMSO
CAS:551909-15-0
MF:C15H14Cl2N2O
MW:309.19
EINECS:
Product Categories:
Mol File:551909-15-0.mol
Urea, N-(4-chlorophenyl)-N'-[2-(3-chlorophenyl)ethyl]- Structure
Urea, N-(4-chlorophenyl)-N'-[2-(3-chlorophenyl)ethyl]- Chemical Properties
Boiling point 433.1±45.0 °C(Predicted)
density 1.330±0.06 g/cm3(Predicted)
storage temp. 4°C, protect from light
solubility DMSO : 100 mg/mL (323.43 mM; Need ultrasonic)
form Solid
pka13.54±0.46(Predicted)
color White to off-white
Safety Information
MSDS Information
Urea, N-(4-chlorophenyl)-N'-[2-(3-chlorophenyl)ethyl]- Usage And Synthesis
UsesRTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca2+ mobilization assay. RTICBM-189 has pIC50s of 5.29 and 6.25 for hCB1 and mCB1, respectively. RTICBM-189 significantly and selectively attenuates the reinstatement of the addictive agent-seeking behavior in rats[1].
Biological ActivityRTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca2+ mobilization assay. RTICBM-189 has pIC50s of 5.29 and 6.25 for hCB1 and mCB1, respectively. RTICBM-189 significantly and selectively attenuates the reinstatement of the cocaine-seeking behavior in rats[1]. RTICBM-189 (10 mg/kg; i.p.) significantly and selectively attenuates reinstatement of the cocaine-seeking behavior in rats[1].RTICBM-189 (10 mg/kg; i.p.) rapidly absorbs into systemic circulation, with peak plasma concentration (Cmax,plasma=288.4 ng/mL) observed at tmax,plasma of 0.4 h post-dose. Peak brain levels are also reached at tmax,brain of 0.4 h with a significantly higher Cmax,brain value of 594.6 ng/mL in the brain[1].
in vivo

RTICBM-189 (10 mg/kg; i.p.) rapidly absorbs into systemic circulation, with peak plasma concentration (Cmax,plasma=288.4 ng/mL) observed at tmax,plasma of 0.4 h post-dose. Peak brain levels are also reached at tmax,brain of 0.4 h with a significantly higher Cmax,brain value of 594.6 ng/mL in the brain[1].

Animal Model:Adult male Sprague-Dawley rats weighing 280-300 g[1]
Dosage:10 mg/kg
Administration:IP
Result:Significantly attenuated drug-induced reinstatement of the cocaine-seeking behavior.
Animal Model:Male Sprague-Dawley rats weighing 258-277 g[1]
Dosage:10 mg/kg (Pharmacokinetic Analysis)
Administration:IP
Result:Plasma: Cmax (288.4 ng/mL), tmax (0.4 hours), CL_F (240.6 mL/min/kg), AUCinf (715.2 ng/mL × h), half-life t1/2 (9.9 hours). Brain: Cmax (594.6 ng/mL), tmax (0.4 hours), CL_F (120.7 mL/min/kg), AUCinf (1438.2 ng/mL × h).
IC 50CB1: 7.54 (pIC50); hCB1: 5.29 (pIC50); mCB1: 6.25 (pIC50)
References[1]. 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.
Urea, N-(4-chlorophenyl)-N'-[2-(3-chlorophenyl)ethyl]- Preparation Products And Raw materials
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