1186195-59-4
Chemical Structure
Tocrifluor 1117
Synonym(s): T1117
- CAS No.: 1186195-59-4
- Formula:C56H53Cl2N7O5
- Molecular Weight:974.97
IUPAC Name: 5-(4'-(3-(3',6'-bis(dimethylamino)-3-oxo-3H-spiro[isobenzofuran-1,9'-xanthene]-5-carboxamido)propyl)-[1,1'-biphenyl]-4-yl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide
InChIKey: RNAPRXIZPJDYPH-UHFFFAOYSA-N
SMILES: O=C(C1=NN(C2=CC=C(Cl)C=C2Cl)C(C3=CC=C(C4=CC=C(CCCNC(C5=CC6=C(C7(C8=C(OC9=C7C=CC(N(C)C)=C9)C=C(N(C)C)C=C8)OC6=O)C=C5)=O)C=C4)C=C3)=C1C)NN%10CCCCC%10
Biological Activity: Tocrifluor 1117 is a selective GPR55 ligand and fluorescent probe. Tocrifluor 1117 shows extremely low affinity for mouse CB1 receptors (Ki >1000 nM) and only weakly displaces CB1 agonists. Tocrifluor 1117 specifically activates GPR55 to trigger intracellular calcium oscillations, and binds to vascular smooth muscle, endothelial and adventitial cells; all these binding effects are inhibited by pretreatment with unlabeled AM251 or O1602. Tocrifluor 1117 can clearly visualize the distribution of GPR55 in vascular tissues via confocal microscopy, while its uptake in cancer cells is completely dependent on GPR55 expression[1][2].
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Tocrifluor 1117 | Tocrifluor 1117 is a selective GPR55 ligand and fluorescent probe. Tocrifluor 1117 shows extremely low affinity for mouse CB1 receptors (Ki >1000 nM) and only weakly displaces CB1 agonists. Tocrifluor 1117 specifically activates GPR55 to trigger intracellular calcium oscillations, and binds to vascular smooth muscle, endothelial and adventitial cells; all these binding effects are inhibited by pretreatment with unlabeled AM251 or O1602. Tocrifluor 1117 can clearly visualize the distribution of GPR55 in vascular tissues via confocal microscopy, while its uptake in cancer cells is completely dependent on GPR55 expression. | |||||||||||||||||||||
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References
- [1]. Daly C J, Ross R A, Whyte J, et al. Fluorescent ligand binding reveals heterogeneous distribution of adrenoceptors and ‘cannabinoid‐like’receptors in small arteries[J]. British journal of pharmacology, 2010, 159(4): 787-796.
- [2]. Singh NS, et al. Selective GPR55 antagonism reduces chemoresistance in cancer cells. Pharmacol Res. 2016;111:757-766. [Content Brief]
