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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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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.
| Targets |
CB1 ( pIC50 = 7.54 ); hCB1 ( pIC50 = 5.29 ); mCB1 ( pIC50 = 6.25 )
Cannabinoid Type-1 Receptor (CB1R) (allosteric modulator) [1] |
|---|---|
| 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.
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| 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].
Male Sprague-Dawley rats trained in intravenous cocaine self-administration (0.75 mg/kg/infusion) were subjected to extinction training until responding decreased to <20% of baseline. During reinstatement testing, pretreatment with RTICBM-189 (administered 30 minutes prior) dose-dependently attenuated cocaine-primed reinstatement of cocaine-seeking behavior, with significant effects observed at a dose of 10 mg/kg [1] - RTICBM-189 did not alter locomotor activity in rats at the effective dose for attenuating reinstatement, indicating the effect was not due to general sedation or motor impairment [1] |
| Animal Protocol |
Adult male Sprague-Dawley rats weighing 280-300 g
10 mg/kg IP |
| ADME/Pharmacokinetics |
RTICBM-189 has brain permeability, with a brain-to-plasma concentration ratio of approximately 0.8 (measured 1 hour after intraperitoneal injection of 10 mg/kg in rats) [1]
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| References | |
| Additional Infomation |
RTICBM-189 is a synthetic analog of 3-(4-chlorophenyl)-1-(phenethyl)urea designed as a positive allosteric modulator (PAM) of CB1R [1] - This compound is designed to target the CB1R-mediated drug addiction signaling pathway, with a focus on reducing cocaine craving behavior while avoiding the side effects associated with ortho-CB1R ligands [1] - RTICBM-189 was selected from a range of urea analogs based on its good CB1R allosteric modulatory properties, brain permeability, and in vivo efficacy in reducing cocaine relapse [1]
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| 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
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| Synonyms |
RTICBM189; RTICBM 189; RTICBM-189
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: 62~100 mg/mL (200.5~323.4 mM)
Ethanol: ~3 mg/mL |
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| 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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