Y1271

Sigma-Aldrich

YM-202074 倍半富马酸盐 水合物

≥98% (HPLC)

别名:
YM 202074, YM202074, N-cyclohexyl-6-{[(2-methoxyethyl)(methyl)amino]methyl}-N-methylthiazolo[3,2-a]benzimidazole-2-carboxamide
Empirical Formula (Hill Notation):
C22H30N4O2S · 1.5C4H4O4 · xH2O
分子量:
588.67 (anhydrous basis)
MDL number:
PubChem Substance ID:
NACRES:
NA.77

Quality Level

assay

≥98% (HPLC)

form

powder

color

white to off-white

solubility

DMSO: >20 mg/mL
H2O: >5 mg/mL

storage temp.

room temp

SMILES string

O.OC(=O)\C=C\C(O)=O.OC(=O)\C=C\C(O)=O.COCCN(C)Cc1ccc2nc3sc(cn3c2c1)C(=O)N(C)C4CCCCC4.COCCN(C)Cc5ccc6nc7sc(cn7c6c5)C(=O)N(C)C8CCCCC8.COCCN(C)Cc9ccc%10nc%11sc(cn%11c%10c9)C(=O)N(C)C%12CCCCC%12

InChI

1S/3C22H30N4O2S.2C4H4O4.H2O/c3*1-24(11-12-28-3)14-16-9-10-18-19(13-16)26-15-20(29-22(26)23-18)21(27)25(2)17-7-5-4-6-8-17;2*5-3(6)1-2-4(7)8;/h3*9-10,13,15,17H,4-8,11-12,14H2,1-3H3;2*1-2H,(H,5,6)(H,7,8);1H2/b;;;2*2-1+;

InChI key

MCGFIZFYSARKON-RAMYONIISA-N

Packaging

5, 25 mg in glass bottle

Biochem/physiol Actions

YM-202074 is a potent and selective allosteric metabotropic glutamate receptor type 1 (mGluR1) antagonist. It bound an allosteric site of rat mGluR1 with a Ki value of 4.8 nM. It also inhibited the mGluR1-mediated inositol phosphates production in rat cerebellar granule cells with an IC50 value of 8.6 nM, while showing selectivity over mGluR(2-7).

Pictograms

Skull and crossbones

Signal Word

Danger

Hazard Statements

RIDADR

UN 2811 6.1 / PGIII

WGK Germany

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Despoina Goniotaki et al.
PLoS pathogens, 13(11), e1006733-e1006733 (2017-11-28)
Prion infections cause inexorable, progressive neurological dysfunction and neurodegeneration. Expression of the cellular prion protein PrPC is required for toxicity, suggesting the existence of deleterious PrPC-dependent signaling cascades. Because group-I metabotropic glutamate receptors (mGluR1 and mGluR5) can form complexes with...
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