2. Membrane Transporter/Ion Channel
    Neuronal Signaling
  3. TRP Channel
  4. TRPM8 antagonist 2

TRPM8 antagonist 2 

Cat. No.: HY-112430 Purity: 98.33%
COA Handling Instructions

TRPM8 antagonist 2 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 2 Chemical Structure

TRPM8 antagonist 2 Chemical Structure

CAS No. : 259674-19-6

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Solution
10 mM * 1 mL in DMSO USD 109 In-stock
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10 mM * 1 mL
ready for reconstitution
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Solid
5 mg USD 99 In-stock
10 mg USD 165 In-stock
50 mg USD 462 In-stock
100 mg USD 770 In-stock
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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

TRPM8 antagonist 2 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 2 (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 2 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].

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

TRPM8 antagonist 2 (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 2 (0.1 and 1 μg, s.c.) attenuates Oxaliplatin (OXP)-induced cold allodynia in mice[1].

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

398.50

Appearance

Solid

Formula

C26H26N2O2
CAS No.
SMILES

O=C([[email protected]@H](N(CC1=CC=CC=C1)CC2=CC=CC=C2)CC3=CNC4=CC=CC=C43)OC
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 : 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    40% PEG300    5% Tween-80    45% saline

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

  • 2.

    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

  • 3.

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

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

*All of the co-solvents are available by MCE.
Purity & Documentation
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 2 (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 receive the vehicle injection[1].

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

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This equation is commonly abbreviated as: C1V1 = C2V2

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Keywords:

TRPM8 antagonist 2259674-19-6TRP ChannelTransient receptor potential channelsInhibitorinhibitorinhibit

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