Tecadenoson-CVT-510-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETecadenosonCat. No.: HY-19661CAS No.: 204512-90-3Synonyms: CVT-510分式: CHNO分量: 337.33作靶点: Adenosine Receptor作通路: GPCR/G Protein储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 155 mg/mL (459.

2、49 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.9645 mL 14.8223 mL 29.6446 mL5 mM 0.5929 mL 2.9645 mL 5.9289 mL10 mM 0.2964 mL 1.4822 mL 2.9645 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Tecadenoson (CVT-510)选择性的腺苷受体 (A1 ad

3、enosine receptor) 激动剂。IC50 & Target Target: A1 adenosine receptor 1体外研究In the atrial-paced isolated heart, Tecadenoson is approximately 5 fold more potent to prolong the stimulus-1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEto-His bundle (S-H interval), a measure of slowing AV nodal conduction (

4、EC50=41nM) than to increasecoronary conductance (EC50=200nM). At concentrations of Tecadenoson (40nM) and diltiazem (1M) thatcauses equal prolongation of S-H interval (-10ms), diltiazem, but not Tecadenoson, significantly reduces leftventricular developed pressure (LVP) and markedly increases corona

5、ry conductance. Tecadenoson shortensatrial (EC50=73nM) but not the ventricular monophasic action potentials (MAP) 1.体内研究 In atrial-paced anaesthetized guinea-pigs, intravenous infusions of Tecadenoson and diltiazem causes nearlyequal prolongations of P-R interval 1. Tecadenoson (2, 5, 20 g/kg i.p.)

6、causes a rapid and sustained dose-dependent decrease in NEFA at doses that do not cause bradycardia. Tecadenoson given at 50 g/kgcauses a significant bradycardia (50% decrease in heart rate at 25 min 2.PROTOCOLKinase Assay 1 The effect of Tecadenoson on binding to A1 and A2A-adenosine receptors of p

7、orcine forebrain and striatummembranes, respectively, are determined. Assays for A1 and A2A receptors are carried out by using the A1receptor antagonist 3HCPX and the A2A receptor agonist 3HCGS21680. Membranes are treated withadenosine deaminase (2U/mL) for 20min at room temperature prior to and dur

8、ing radioligand bindingassays. Membranes (0.2-0.7mg), adenosine deaminase, and the indicated radioligand are incubated for 3hin a 300L volume of Tris-HCl buffer (50mM) (pH7.4). Assays are carried out in triplicate at roomtemperature. After the incubation period, bound and free radioligand are dilute

9、d by the addition of ice-coldTris-HCl buffer (5mL), and immediately separated by vacuum filtration of assay contents onto WhatmanGF/C filters and ishing of trapped membranes with Tris-HCl buffer (20 mL). Filter disks containingmembrane-bound radioactivity are placed in 4 mL Scintiverse, and the radi

10、oactivity is quantified by a liquidscintillation counter. Specific binding of 3HCPX and 3HCGS21680 is defined as membrane bindingdisplaced in the presence of CPT (10M) and R-PIA (10M), respectively 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Anima

11、l Rat: The effects of Tecadenoson on heart rate and to reduce serum NEFA concentration are determined inAdministration 2 separate groups of rats to avoid the effects of animal handling and blood sampling on heart rate. Three daysbefore an experiment, a catheter (0.025-mm outer diameter) is implanted

12、 in the left common carotid artery ofeach rat using aseptic conditions and sterile technique. The catheter is tunneled subcutaneously to the dorsalsurface. After recovery from anesthesia, rats are placed in metabolic cages to facilitate handling and bloodsampling. Blood samples (0.2 mL) are drawn be

13、fore and at various time points after i.p. injection of eitherTecadenoson or vehicle (DMSO in saline). A 0.4-mL volume of 1% sodium citrate in saline is administeredafter withdrawal of each blood sample to replace blood volume and prevent clotting in the carotid arterycatheter. Serum is collected fr

14、om each sample after centrifugation of the clotted blood. Serum samples arestored at 80C until analysis. Serum NEFA concentration is determined using an enzymatic colorimetricassay kit 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES2/3 Mast

15、er of Small Molecules 您边的抑制剂师www.MedChemE1. Snowdy S, et al. A comparison of an A1 adenosine receptor agonist (CVT-510) with diltiazem for slowing of AVnodal conduction inguinea-pig. Br J Pharmacol. 1999 Jan;126(1):137-46.2. Fraser H, et al. N-3-(R)-tetrahydrofuranyl-6-aminopurine riboside, an A1 adenosine receptor agonist, antagonizes catecholamine-induced lipolysis without cardiovascular effects in awake rats. J Pharmacol Ex