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Documenti fondamentali

SML0423

Sigma-Aldrich

ML194

≥98% (HPLC)

Sinonimo/i:

1-(2,4-Difluorophenyl)-5-[[2-[[(1,1-dimethylehyl)amino]thioxomethyl]hydrazinylidene]methyl]-1H-pyrazole-4-carboxylic acid methyl ester, CID-9581011, CID9581011, Methyl 5-[(E)-(tert-butylcarbamothioylhydrazinylidene)methyl]-1-(2,4-difluorophenyl)pyrazole-4-carboxylate

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About This Item

Formula empirica (notazione di Hill):
C17H19F2N5O2S
Numero CAS:
Peso molecolare:
395.43
Numero MDL:
Codice UNSPSC:
12352200
ID PubChem:
NACRES:
NA.77

Livello qualitativo

Saggio

≥98% (HPLC)

Stato

powder

Condizioni di stoccaggio

protect from light

Colore

white to beige

Solubilità

DMSO: 15 mg/mL (clear solution)

Temperatura di conservazione

−20°C

Stringa SMILE

COC(=O)c1cnn(-c2ccc(F)cc2F)c1\C=N\NC(=S)NC(C)(C)C

InChI

1S/C17H19F2N5O2S/c1-17(2,3)22-16(27)23-20-9-14-11(15(25)26-4)8-21-24(14)13-6-5-10(18)7-12(13)19/h5-9H,1-4H3,(H2,22,23,27)/b20-9+
CYNLZIBKERMMOA-AWQFTUOYSA-N

Azioni biochim/fisiol

ML194 (CID9581011) is an antagonist of GPR35, a GPRC receptor expressed in nervous system tissue, in the GI tract particularly in pancreas and small intestine, followed by colon, spleen, and immune cells, and also expressed in gastric carcinomas. GPR35 is being investigated for potential therapeutic importance in a variety of areas including pain, hypertension, cancer, diabetes and asthma. ML194 is more membrane penetrant and more potent than earlier synthetic antagonists, with an IC50 of 160nM. ML194 was also found to rescue the cell-surface expression of mutant GPR35 receptors, likely acting as a pharmacological chaperone to alter the misfolded receptor structure.

Caratteristiche e vantaggi

This compound is a featured product for Cyclic Nucleotide research. Click here to discover more featured Cyclic Nucleotide products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound is featured on the G Proteins (Heterotrimeric) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable


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Ozayra Sharmin et al.
Scientific reports, 10(1), 9400-9400 (2020-06-12)
Pamoic acid is a potent ligand for G protein Coupled Receptor 35 (GPR35) and exhibits antinociceptive property. GPR35 activation leads to increased energy utilization and the expression of anti-inflammatory genes. However, its role in brain disorders, especially in stroke, remains
Xiao Zheng et al.
Brain, behavior, and immunity, 79, 244-255 (2019-02-23)
Psychological stress is well known to increase colitis susceptibility and promote relapse. Metabolic changes are commonly observed under psychological stress, but little is known how this relates to the progression of colitis. Here we show that kynurenic acid (KA) is

Articoli

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Contenuto correlato

Cyclic nucleotides, including cyclic AMP (cAMP), cyclic GMP (cGMP) and cyclic ADP-ribose, have been extensively studied as second messengers of intracellular events initiated by activation of GPCRs. cAMP modifies cell function in all eukaryotic cells, principally through the activation of cAMP-dependent protein kinase (PKA), but also through cAMP-gated ion channels and guanine nucleotide exchange factors directly activated by cAMP.

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