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SML0893

Sigma-Aldrich

M8-B hydrochloride

≥98% (HPLC)

Synonym(s):

N-(2-Aminoethyl)-N-(4-(benzyloxy)-3-methoxybenzyl)thiophene-2-carboxamide hydrochloride, N-(2-Aminoethyl)-N-[[3-methoxy-4-(phenylmethoxy)phenyl]methyl]-2-thiophenecarboxamide hydrochloride

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About This Item

Empirical Formula (Hill Notation):
C22H24N2O3S · HCl
CAS Number:
Molecular Weight:
432.96
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

Assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

H2O: 2 mg/mL, clear (warmed)

storage temp.

2-8°C

InChI

1S/C22H24N2O3S.ClH/c1-26-20-14-18(9-10-19(20)27-16-17-6-3-2-4-7-17)15-24(12-11-23)22(25)21-8-5-13-28-21;/h2-10,13-14H,11-12,15-16,23H2,1H3;1H

InChI key

FMQJBHACRTZLME-UHFFFAOYSA-N

Application

M8-B hydrochloride has been used as a transient receptor potential melastatin-8 (TRPM8) channel antagonist to study its therapeutic efficiency on a mouse model of severe dry eye disease (DED) induced by the excision of extra-orbital lacrimal and Harderian glands.

Biochem/physiol Actions

M8-B is a selective and potent antagonist of the transient receptor potential melastatin-8 (TRPM8) channel. M8-B blocked cold-induced and icilin or methol-induced activation of rat, human, and murine TRPM8 channels with IC50 values in rat ranging from 7.8 nM to 64.3 nM, and it did not block other TRP channels (IC50 values > 20 mM). M8-B decreased deep body temperature in both mice and rats, showing that blockade of TRPM8 receptor might be used to induce therapeutic hypothermia, an effective treatment in cardiac arrest.

Features and Benefits

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Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

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Darine Fakih et al.
International journal of molecular sciences, 21(22) (2020-11-25)
Dry eye disease (DED) is commonly associated with ocular surface inflammation and pain. In this study, we evaluated the effectiveness of repeated instillations of transient receptor potential melastatin 8 (TRPM8) ion channel antagonist M8-B on a mouse model of severe

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