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TRPM8 Antagonist

Basic information Safety Supplier Related

TRPM8 Antagonist Basic information

Product Name:
TRPM8 Antagonist
Synonyms:
  • TRPM8 Antagonist
  • TRPM8 ANTAGONIST;259674-19-6
  • TRPM8 antagonist 2
  • L-Tryptophan, N,N-bis(phenylmethyl)-, methyl ester
  • Methyl N,N-dibenzyl-L-tryptophanate
  • Methyl Na,Na-dibenzyl-L-tryptophanate
  • TRPM8 antagonist 2,inhibit,Transient receptor potential channels,TRP Channel,Inhibitor,TRPM-8 antagonist 2
  • TRPM8 antagonist 2, 10 mM in DMSO
CAS:
259674-19-6
MF:
C26H26N2O2
MW:
398.5
Product Categories:
  • API
Mol File:
259674-19-6.mol
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TRPM8 Antagonist Chemical Properties

Boiling point:
567.5±50.0 °C(Predicted)
Density 
1.195±0.06 g/cm3(Predicted)
storage temp. 
under inert gas (nitrogen or Argon) at 2-8°C
solubility 
DMSO : 160 mg/mL (401.51 mM)
pka
17.02±0.30(Predicted)
form 
Solid
color 
Light yellow to yellow
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TRPM8 Antagonist Usage And Synthesis

Uses

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.

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].

References

[1] 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. DOI:10.1021/acs.jmedchem.8b00545

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