CGH 2466 dihydrochloride is a combined adenosine receptor antagonist. It is an inhibitor of phosphodiesterase type 4 and p38 mitogen-activated protein kinase. It inhibited the phosphodiesterase 4D (PDE4D) isoenzyme with an IC50 value of 22±5 nM. It inhibited the p38 mitogen-activated protein (MAP) kinases α and β with IC50 values of 187±18, 400±38 nM, respectively . There are four adenosine receptor subtypes of the G protein-coupled receptor family, designated as A1, A2A, A2B and A3 . Adenosine plays a role in the control of inflammation . Phosphodiesterases can inactivate cAMP. In inflammatory cells, phosphodiesterase-4 (PDE4) is the predominant isoenzyme . In mammalian cells, the p38 MAPK was thought to be important for regulating cellular responses during infection via its effects on the expression of proinflammatory molecules . CGS15943 is a broad spectrum adenosine antagonist, SB203580 is a prototypical inhibitor of the p38 MAP kinase, and cilomilast is a standard inhibitor of PDE4. Data showed that CGH2466 was similar to SB203580 in potency as a p38 MAP kinase inhibitor, and was similar to cilomilast in activity to inhibit PDE4D. Compared to CGS15943, CGH 2466 showed similar potency to inhibit A1, A2B and A3 adenosine receptors. In contrast to CGS15943, CGH2466 was not active at the A2A receptor. Compared with other above compounds, CGH2466 was an inhibitor of the highest potency to inhibit selected enzymes or receptors in leucocyte-based assays . 48 h after the allergen challenge, bronchoalveolar lavage recovered eosinophil numbers. In sensitized mice, aerosol challenge of ovalbumin was able to increase these eosinophil numbers. In this animal model of asthmatic inflammation, 15 min before and 24 h after the challenge, the intranasal administration of CGH2466, dose-dependently inhibited the airway eosinophilia induced by ovalbumin, reaching significant levels at doses of 3 and 10 mg.kg-1 .

Product information

CAS Number: 1177618-54-0

Molecular Weight: 322.21

Formula: C14H9Cl2N3S

Chemical Name: 4-(3,4-dichlorophenyl)-5-(pyridin-4-yl)-2,3-dihydro-1,3-thiazol-2-imine

Smiles: N=C1NC(=C(S1)C1C=CN=CC=1)C1=CC(Cl)=C(Cl)C=C1

InChiKey: BEPGKLOHQTXUHX-UHFFFAOYSA-N

InChi: InChI=1S/C14H9Cl2N3S/c15-10-2-1-9(7-11(10)16)12-13(20-14(17)19-12)8-3-5-18-6-4-8/h1-7H,(H2,17,19)

Technical Data

Appearance: Solid Power

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

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