HVN74196


Catalog No. size PriceQuantity
M7006-2 2mg solid $94
M7006-10 10mg solid $360

Description

Cas:259674-19-6

Product Information

HVN74196, also known as 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. HVN74196 has CAS#259674-19-6, no formal name. For the convenience of scientific communication, we named it as HVN74196 (combined from Inchi key plus CAS#) according to Hodoodo Chemical Nomenclature (https://hodoodo.com/hodoodo-chemical-nomenclature).

 

Chemical Formula: C26H26N2O2

 

Exact Mass: 398.1994

 

Molecular Weight: 398.506

 

Elemental Analysis: C, 78.36; H, 6.58; N, 7.03; O, 8.03

 

Synonym: 

 

TRPM8 antagonist 2

HVN74196

HVN-74196

HVN 74196

Chemical Name: 

methyl Na,Na-dibenzyl-L-tryptophanate

 

InChi Key:

HHVOOJDLCVOLKI-VWLOTQADSA-N

 

InChi Code: InChI=1S/C26H26N2O2/c1-30-26(29)25(16-22-17-27-24-15-9-8-14-23(22)24)28(18-20-10-4-2-5-11-20)19-21-12-6-3-7-13-21/h2-15,17,25,27H,16,18-19H2,1H3/t25-/m0/s1

 

Smiles Code:

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

 

 

Technical Data:

 

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

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).

 

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.

 

 

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.

 

Products are for research use only. Not for human use.

 

 

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