RTICBM-189 (RTICBM189) is brain penetrant and allosteric modulator of the cannabinoid 1 (CB1) receptor (pIC50 = 7.54 in Ca²⁺ mobilization assay). It lessens the resumption of drug-seeking behavior.

Physicochemical Properties

Molecular Formula	C15H14CL2N2O
Molecular Weight	309.19
Exact Mass	308.05
Elemental Analysis	C, 58.27; H, 4.56; Cl, 22.93; N, 9.06; O, 5.17
CAS #	551909-15-0
PubChem CID	5076367
Appearance	White to off-white solid powder
LogP	4.1
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	1
Rotatable Bond Count	4
Heavy Atom Count	20
Complexity	306
Defined Atom Stereocenter Count	0
InChi Key	PPKIPROVSKBYAT-UHFFFAOYSA-N
InChi Code	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)
Chemical Name	1-(4-chlorophenyl)-3-[2-(3-chlorophenyl)ethyl]urea
Synonyms	RTICBM189; RTICBM 189; RTICBM-189
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	CB1 ( pIC50 = 7.54 ); hCB1 ( pIC50 = 5.29 ); mCB1 ( pIC50 = 6.25 )
ln Vitro	RTICBM-189 (RTICBM189) is an allosteric modulator and brain penetrant of the cannabinoid 1 (CB1) receptor with a pIC50 of 7.54 in the Ca2+ mobilization assay. It lessens the likelihood of resuming drug-seeking behavior.
ln Vivo	RTICBM-189 (10 mg/kg; i.p.) significantly and selectively reduces the resumption of cocaine-seeking behavior in rats[1]. RTICBM-189 (10 mg/kg; i.p.) enters the systemic circulation quickly, and at 0.4 hours after dosage, the peak plasma concentration (Cmax,plasma=288.4 ng/mL) is seen. With a much greater Cmax,brain value of 594.6 ng/mL in the brain, peak brain levels are also reached at tmax,brain of 0.4 h[1].
Animal Protocol	Adult male Sprague-Dawley rats weighing 280-300 g 10 mg/kg IP
References	[1]. 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.

Solubility Data

Solubility (In Vitro)

DMSO: 62~100 mg/mL (200.5~323.4 mM) Ethanol: ~3 mg/mL

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (8.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: 2.08 mg/mL (6.73 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.2343 mL	16.1713 mL	32.3426 mL
	5 mM	0.6469 mL	3.2343 mL	6.4685 mL
	10 mM	0.3234 mL	1.6171 mL	3.2343 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.