1. Membrane Transporter/Ion Channel
  2. TRP Channel

TRPM8 Antagonist 

Cat. No.: HY-112430
Handling Instructions

TRPM8 Antagonist is a potent and selective TRPM8 antagonist, with an IC50 of 0.2 nM, used in the research of neuropathic pain syndromes.

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

TRPM8 Antagonist Chemical Structure

TRPM8 Antagonist Chemical Structure

CAS No. : 259674-19-6

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 275 In-stock
Estimated Time of Arrival: December 31
5 mg USD 250 In-stock
Estimated Time of Arrival: December 31
10 mg USD 350 In-stock
Estimated Time of Arrival: December 31
50 mg USD 950 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

TRPM8 Antagonist is a potent and selective TRPM8 antagonist, with an IC50 of 0.2 nM, used in the research of neuropathic pain syndromes.

IC50 & Target

IC50: 0.2 nM (TRPM8)[1]

In Vitro

TRPM8 Antagonist (Compound 14) is a potent and selective TRPM8 antagonist, with an IC50 of 0.2 nM, used in the research of neuropathic pain syndromes. TRPM8 Antagonist potently inhibits menthol-induced increase in intracellular Ca2+ levels in Ca2+ fluorimetric assays in HEK293 cells stably expressing the rat isoform of TRPM8 channels (IC50, 40 nM)[1].

In Vivo

TRPM8 Antagonist (1, 10, and 30 mg/kg, s.c.) shows a marked, dose-dependent antinociceptive activity, and inhibits wet-dog shakes (WDS)-like cold hypersensitivity in mice by 63% at 30 mg/kg. In addition, TRPM8 Antagonist (0.1 and 1 μg, s.c.) attenuates Oxaliplatin (OXP)-induced cold allodynia in mice[1].

Solvent & Solubility
In Vitro: 

DMSO : 160 mg/mL (401.51 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5094 mL 12.5471 mL 25.0941 mL
5 mM 0.5019 mL 2.5094 mL 5.0188 mL
10 mM 0.2509 mL 1.2547 mL 2.5094 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.67 mg/mL (6.70 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.67 mg/mL (6.70 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.67 mg/mL (6.70 mM); Clear solution

References
Animal Administration
[1]

Mice[1]
Icilin, a TRPM8 agonist, is dissolved in 20% DMSO and 1% Tween 80 in distilled water and injected intraperitoneally (i.p.) in a volume of 10 mL/kg. Each animal is acclimatized for 30 min for two consecutive days before icilin administration. TRPM8 Antagonist (compound 14) stock is prepared in DMSO and diluted in saline for injections. Gabapentin is dissolved in saline and administered s.c. at the dose of 25 mg/kg 60 min prior to icillin injection. Control animals received the vehicle injection[1].

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

References
Molecular Weight

398.50

Formula

C₂₆H₂₆N₂O₂

CAS No.

259674-19-6

SMILES

O=C([[email protected]@H](N(CC1=CC=CC=C1)CC2=CC=CC=C2)CC3=CNC4=CC=CC=C43)OC

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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  • Dilution Calculator

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This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
C1   V1   C2   V2

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Product Name:
TRPM8 Antagonist
Cat. No.:
HY-112430
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TRPM8 Antagonist

Cat. No.: HY-112430