Bioactivity | 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]. |
Invitro | 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]. |
Name | CB1R Allosteric modulator 3 |
CAS | 2633686-36-7 |
Formula | C22H17ClN2O2 |
Molar Mass | 376.84 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Peter C Schaffer, et al. Focused structure-activity relationship profiling around the 2-phenylindole scaffold of a cannabinoid type-1 receptor agonist-positive allosteric modulator: site-III aromatic-ring congeners with enhanced activity and solubility. Bioorg Med Chem. 2020 Nov 1;28(21):115727. |