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CGH 2466 dihydrochloride

adenosine receptor antagonist CAS# 1177618-54-0

CGH 2466 dihydrochloride

Catalog No. BCC7338----Order now to get a substantial discount!

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Chemical structure

CGH 2466 dihydrochloride

3D structure

Chemical Properties of CGH 2466 dihydrochloride

Cas No. 1177618-54-0 SDF Download SDF
PubChem ID 16759176 Appearance Powder
Formula C14H11Cl4N3S M.Wt 395.13
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 10 mM in DMSO with gentle warming and to 5 mM in ethanol
Chemical Name 4-(3,4-dichlorophenyl)-5-pyridin-4-yl-1,3-thiazol-2-amine;dihydrochloride
SMILES C1=CC(=C(C=C1C2=C(SC(=N2)N)C3=CC=NC=C3)Cl)Cl.Cl.Cl
Standard InChIKey WHXRCTIBFLXKFD-UHFFFAOYSA-N
Standard InChI InChI=1S/C14H9Cl2N3S.2ClH/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);2*1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of CGH 2466 dihydrochloride

DescriptionAdenosine A1, A2B and A3 receptor antagonist (IC50 values are 19, 21, and 80 nM respectively). Also inhibits p38 MAPK (IC50 = 187 - 400 nM) and phosphodiesterase type 4D (IC50 = 22 nM). Displays potent anti-inflammatory effects in vitro and in vivo. Potentially useful for asthma and chronic obstructive pulmonary disease (COPD) research.

CGH 2466 dihydrochloride Dilution Calculator

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CGH 2466 dihydrochloride Molarity Calculator

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Preparing Stock Solutions of CGH 2466 dihydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.5308 mL 12.6541 mL 25.3081 mL 50.6163 mL 63.2703 mL
5 mM 0.5062 mL 2.5308 mL 5.0616 mL 10.1233 mL 12.6541 mL
10 mM 0.2531 mL 1.2654 mL 2.5308 mL 5.0616 mL 6.327 mL
50 mM 0.0506 mL 0.2531 mL 0.5062 mL 1.0123 mL 1.2654 mL
100 mM 0.0253 mL 0.1265 mL 0.2531 mL 0.5062 mL 0.6327 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on CGH 2466 dihydrochloride

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 [1].

There are four adenosine receptor subtypes of the G protein-coupled receptor family, designated as A1, A2A, A2B and A3 [2]. Adenosine plays a role in the control of inflammation [3]. Phosphodiesterases can inactivate cAMP. In inflammatory cells, phosphodiesterase-4 (PDE4) is the predominant isoenzyme [4]. 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 [5].

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 [1].

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 [1].

References:
[1].  Trifilieff A, Keller TH, Press NJ, et al. CGH2466, a combined adenosine receptor antagonist, p38 mitogen‐activated protein kinase and phosphodiesterase type 4 inhibitor with potent in vitro and in vivo anti‐inflammatory activities. British journal of pharmacology, 2005, 144(7): 1002-1010.
[2].  Klotz KN, Hessling J, Hegler J, et al. Comparative pharmacology of human adenosine receptor subtypes-characterization of stably transfected receptors in CHO cells. Naunyn-Schmiedeberg's archives of pharmacology, 1997, 357(1): 1-9.
[3].  Yang D, Zhang Y, Nguyen HG, et al. The A2B adenosine receptor protects against inflammation and excessive vascular adhesion. The Journal of clinical investigation, 2006, 116(7): 1913-1923.
[4].  Gamble E, Grootendorst DC, Brightling CE, et al. Antiinflammatory effects of the phosphodiesterase-4 inhibitor cilomilast (Ariflo) in chronic obstructive pulmonary disease. American journal of respiratory and critical care medicine, 2003, 168(8): 976-982.
[5].  Han J, Jiang Y, Li Z, et al. Activation of the transcription factor MEF2C by the MAP kinase p38 in inflammation. 1997, 386(6622):296-299.

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References on CGH 2466 dihydrochloride

CGH2466, a combined adenosine receptor antagonist, p38 mitogen-activated protein kinase and phosphodiesterase type 4 inhibitor with potent in vitro and in vivo anti-inflammatory activities.[Pubmed:15685201]

Br J Pharmacol. 2005 Apr;144(7):1002-10.

Theophylline, a phosphodiesterase inhibitor and adenosine receptor antagonist, is used in asthma and chronic obstructive pulmonary disease (COPD) treatment. However, the relatively low effectiveness of theophylline have recently led to reduced usage. The goal of the present study was to identify a theophylline-like compound with improved effectiveness. We discovered CGH2466, which not only antagonised the adenosine A1, A2b and A3 receptors with IC50 values of 19 +/- 4, 21 +/- 3 and 80 +/- 14 nM, respectively, but also inhibited the p38 mitogen-activated protein (MAP) kinases alpha and beta and the phosphodiesterase 4D (PDE4D) isoenzyme with IC50 values of 187 +/- 18, 400 +/- 38 and 22 +/- 5 nM, respectively. Despite similar potencies on individual targets, CGH2466 inhibited the production of cytokines and oxygen radicals by human peripheral blood leucocytes in vitro, more potently (IC50 values between 30 and 50 nM) than the standard p38 MAP kinase inhibitor SB203580 (30 nM to >1 microM), the PDE4 inhibitor cilomilast (120-400 nM) and the broad spectrum adenosine receptor antagonist CGS15943 (>10 microM). When given either orally or locally into the lungs, CGH2466 (3 to 10 mg kg(-1)) inhibited the ovalbumin- or lipopolysaccharide-induced airway inflammation in mice more potently than the single receptor antagonists or enzyme inhibitors used alone. In conclusion, CGH2466 through its combined activities at multiple targets exerted a powerful anti-inflammatory effect and therefore may have beneficial therapeutic value in diseases such as asthma and COPD.

Description

Anti-inflammatory agent. Inhibitor of PDE4 and p38 MAPK, also adenosine receptor antagonist

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