2. GPCR/G Protein Neuronal Signaling
  3. Cannabinoid Receptor
  4. RTICBM-189

RTICBM-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.

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RTICBM-189 Chemical Structure

RTICBM-189 Chemical Structure

CAS No. : 551909-15-0

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Based on 1 publication(s) in Google Scholar

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Description

RTICBM-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].

IC50 & Target[1]

CB1

7.54 (pIC50)

hCB1

5.29 (pIC50)

mCB1

6.25 (pIC50)

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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).
Molecular Weight

309.19

Formula

C15H14Cl2N2O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NCCC1=CC(Cl)=CC=C1)NC2=CC=C(C=C2)Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (323.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (8.09 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (6.73 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2343 mL 16.1713 mL 32.3426 mL 80.8564 mL
5 mM 0.6469 mL 3.2343 mL 6.4685 mL 16.1713 mL
10 mM 0.3234 mL 1.6171 mL 3.2343 mL 8.0856 mL
15 mM 0.2156 mL 1.0781 mL 2.1562 mL 5.3904 mL
20 mM 0.1617 mL 0.8086 mL 1.6171 mL 4.0428 mL
25 mM 0.1294 mL 0.6469 mL 1.2937 mL 3.2343 mL
30 mM 0.1078 mL 0.5390 mL 1.0781 mL 2.6952 mL
40 mM 0.0809 mL 0.4043 mL 0.8086 mL 2.0214 mL
50 mM 0.0647 mL 0.3234 mL 0.6469 mL 1.6171 mL
60 mM 0.0539 mL 0.2695 mL 0.5390 mL 1.3476 mL
80 mM 0.0404 mL 0.2021 mL 0.4043 mL 1.0107 mL
100 mM 0.0323 mL 0.1617 mL 0.3234 mL 0.8086 mL
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RTICBM-189 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RTICBM-189551909-15-0RTICBM189RTICBM 189Cannabinoid ReceptorCB1BrainPenetrantAllostericSeekingBehaviorInhibitorinhibitorinhibit

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