1. GPCR/G Protein Neuronal Signaling
  2. Cannabinoid Receptor Arrestin
  3. CB1R Allosteric modulator 3

CB1R Allosteric modulator 3 is a CB1R positive allosteric modulator. CB1R Allosteric modulator 3 has potent inhibition of cAMP and β-Arrestin with EC50 values of 0.018 μM and 1.241 μM, respectively.

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CB1R Allosteric modulator 3 Chemical Structure

CB1R Allosteric modulator 3 Chemical Structure

CAS No. : 2633686-36-7

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Description

CB1R Allosteric modulator 3 is a CB1R positive allosteric modulator. CB1R Allosteric modulator 3 has potent inhibition of cAMP and β-Arrestin with EC50 values of 0.018 μM and 1.241 μM, respectively[1].

IC50 & Target

CB1

 

In Vitro

CB1R Allosteric modulator 3 (compound 44) (0.10 nM-10 μM, 30 min) has potent inhibition of cAMP and β-Arrestin with EC50 values of 0.018 μM and 1.241 μM, respectively[1].
CB1R Allosteric modulator 3 can enhance CB1R ago-PAM activity because of small lipophilic functional groups on the ortho-position of the GAT211 site-III phenyl ring[1].

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

Molecular Weight

376.84

Formula

C22H17ClN2O2

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

ClC1=C(C=CC=C1)C(C2=C(C3=CC=CC=C3)NC4=C2C=CC=C4)C[N+]([O-])=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (265.36 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 2.6536 mL 13.2682 mL 26.5365 mL
5 mM 0.5307 mL 2.6536 mL 5.3073 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
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. 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 2.6536 mL 13.2682 mL 26.5365 mL 66.3412 mL
5 mM 0.5307 mL 2.6536 mL 5.3073 mL 13.2682 mL
10 mM 0.2654 mL 1.3268 mL 2.6536 mL 6.6341 mL
15 mM 0.1769 mL 0.8845 mL 1.7691 mL 4.4227 mL
20 mM 0.1327 mL 0.6634 mL 1.3268 mL 3.3171 mL
25 mM 0.1061 mL 0.5307 mL 1.0615 mL 2.6536 mL
30 mM 0.0885 mL 0.4423 mL 0.8845 mL 2.2114 mL
40 mM 0.0663 mL 0.3317 mL 0.6634 mL 1.6585 mL
50 mM 0.0531 mL 0.2654 mL 0.5307 mL 1.3268 mL
60 mM 0.0442 mL 0.2211 mL 0.4423 mL 1.1057 mL
80 mM 0.0332 mL 0.1659 mL 0.3317 mL 0.8293 mL
100 mM 0.0265 mL 0.1327 mL 0.2654 mL 0.6634 mL
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  • 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.

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CB1R Allosteric modulator 3
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