Fig. 1 · Structure

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TC-I 2014

Cat. No. A19793 CAS 1221349-53-6

TRPM8 antagonist

TC-I 2014 (compound 5) is a potent and orally active Benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonist, with IC50 values of 0.8 nM, 3.0 nM and 4.4 nM for canine, human and rat channels respectively.

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Biological Activity

Cellular Effect

Cell Line Activity Value Description Reference
HEK293 IC50 0.413 nM Inhibition of human TRPM8 expressed in HEK293 cells assessed as inhibition of cold-induced channel current by whole cell electrophysiology [PMID: 21128593]
HEK293 IC50 0.8 nM Antagonist activity at canine TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation by FLIPR assay [PMID: 21128593]
HEK293 IC50 3 nM Antagonist activity at human TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation at 0.2 uM by FLIPR assay [PMID: 21128593]
HEK293 IC50 4 nM Antagonist activity at rat TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation at 0.2 uM by FLIPR assay [PMID: 21128593]

Specifications

Manufacturer Adooq Bioscience
Actions Antagonist
CAS Number 1221349-53-6
Applications TRPM8 antagonist
Formula C23H19F6N3O
Molecular Weight 467.41
SMILES
FC(C1=CC=CC=C1C2=CC(C(F)(F)F)=C3C(N=C(C4=NOC5(CCCCC5)C4)N3)=C2)(F)F

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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