2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. TC-I 2014

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. TC-I 2014 exhibits antiallodynic properties in pain models.

For research use only. We do not sell to patients.

TC-I 2014 Chemical Structure

TC-I 2014 Chemical Structure

CAS No. : 1221349-53-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

TC-I 2014 Related Antibodies

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Description

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. TC-I 2014 exhibits antiallodynic properties in pain models[1].

IC50 & Target

TRPM8[1].
Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
0.413 nM
Compound: 5
Inhibition of human TRPM8 expressed in HEK293 cells assessed as inhibition of cold-induced channel current by whole cell electrophysiology
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
Compound: 5
Antagonist activity at canine TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation by FLIPR assay
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
Compound: 5
Antagonist activity at human TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation at 0.2 uM by FLIPR assay
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
Compound: 5
Antagonist activity at rat TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation at 0.2 uM by FLIPR assay
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]
In Vitro

TC-I 2014 (compound 5) potently inhibits cold-induced TRPM8 currents in HEK293 cells stably expressing canine or human TRPM8, with IC50 values of 0.413 and 1 nM, respectively[1].

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

TC-I 2014 Related Antibodies
In Vivo

TC-I 2014 (10 mg/kg, Orally once) completely prevents icilin-induced WDS[1].

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

Animal Model: TC-I 2014 (10 mg/kg, Orally once) completely prevents icilin-induced WDS[1].
Dosage: 3, 5.6, 10 mg/kg.
Administration: Orally once.
Result: Produced greater than 90% inhibition at 3, 5.6, and 10 mg/kg administered 2 h prior to icilin challenge.
Molecular Weight

467.41

Formula

C23H19F6N3O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC(C1=CC=CC=C1C2=CC(C(F)(F)F)=C3C(N=C(C4=NOC5(CCCCC5)C4)N3)=C2)(F)F
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 : 250 mg/mL (534.86 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 2.1394 mL 10.6972 mL 21.3945 mL
5 mM 0.4279 mL 2.1394 mL 4.2789 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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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation

Purity: ≥99.0%

SDS (251 KB)

COA (251 KB) Elemental Analysis Report (109 KB)

Handling Instructions (2659 KB)
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 2.1394 mL 10.6972 mL 21.3945 mL 53.4862 mL
5 mM 0.4279 mL 2.1394 mL 4.2789 mL 10.6972 mL
10 mM 0.2139 mL 1.0697 mL 2.1394 mL 5.3486 mL
15 mM 0.1426 mL 0.7131 mL 1.4263 mL 3.5657 mL
20 mM 0.1070 mL 0.5349 mL 1.0697 mL 2.6743 mL
25 mM 0.0856 mL 0.4279 mL 0.8558 mL 2.1394 mL
30 mM 0.0713 mL 0.3566 mL 0.7131 mL 1.7829 mL
40 mM 0.0535 mL 0.2674 mL 0.5349 mL 1.3372 mL
50 mM 0.0428 mL 0.2139 mL 0.4279 mL 1.0697 mL
60 mM 0.0357 mL 0.1783 mL 0.3566 mL 0.8914 mL
80 mM 0.0267 mL 0.1337 mL 0.2674 mL 0.6686 mL
100 mM 0.0214 mL 0.1070 mL 0.2139 mL 0.5349 mL
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TC-I 2014 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:

TC-I 20141221349-53-6TRP ChannelTransient receptor potential channelsInhibitorinhibitorinhibit

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