TRPM8 antagonist 2

This product is for research use only, not for human use. We do not sell to patients.

TRPM8 antagonist 2
For small sizes, please check our retail website as below: www.invivochem.com
Size Price Stock
250mg$950Check With Us
500mg$1450Check With Us
1g$2175Check With Us

Cat #: V31167 CAS #: 259674-19-6 Purity ≥ 99%

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.

References: Bertamino A, et al. Identification of a Potent Tryptophan-Based TRPM8 Antagonist With in Vivo Analgesic Activity. J Med Chem. 2018 Jul 10. doi: 10.1021/acs.jmedchem.8b00545.

Top Publications Citing Invivochem Products
Publications Citing InvivoChem Products

Product Promise

Promise
Molecular Weight (MW)398.506
Molecular FormulaC₂₆H₂₆N₂O₂
CAS No.259674-19-6
SMILES Code O=C([C@@H](N(CC1=CC=CC=C1)CC2=CC=CC=C2)CC3=CNC4=CC=CC=C43)OC
ProtocolIn VitroTRPM8 antagonist 2 (Compound 14) is a potent selective TRPM8 antagonist, IC50 0.2 nM for neuropathic pain syndrome research. TRPM8 antagonist 2 in CA2+ Potent inhibition of menthol-induced intracellular CA in fluorescence assays2+ Elevated levels and HEK293 cells stably expressing the rat subtype (IC) of the TRPM8 channel50,40 nM)
In VivoTRPM8 antagonist 2 (1, 10, and 30 mg/kg, subcutaneously) showed significant dose-dependent analgesic activity and inhibited mouse wet-dog shakes (WDS)-like cold hypersensitivity by 30% at 63 mg/kg. In addition, TRPM8 antagonist 2 (0.1 and 1 μg, subcutaneously) reduced Oxaliplatin (OXP)-induced cold dysphonia in mice
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.5094 mL12.5469 mL25.0937 mL50.1875 mL
5mM0.5019 mL2.5094 mL5.0187 mL10.0375 mL
10mM0.2509 mL1.2547 mL2.5094 mL5.0187 mL
20mM0.1255 mL0.6273 mL1.2547 mL2.5094 mL
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.