96 products were found matching "K04265"!

Recombinant CHO-K1 cells stably overexpress human adenosine A1 receptor (ADORA1) on the surface and contain high levels of G protein Galphai to couple with the receptor in downstream signaling pathways.

An adenosine A1 receptor positive allosteric modulator, inhibits TNF-a and cycloheximide-induced apoptosis in HK-2 kidney epithelial cells at 10 µM, increases right atrial heart rate in combination with ADA in isolated rat right atria (EC50 = 0.83 nM), reduces plasma creatinine levels and infarct area in a mouse...

5'-N-Ethylcarboxamidoadenosine (NECA) is an adenosine analog that acts as an agonist of adenosine receptors (Kis = 1,880, 6,660, and 3.5 nM for human adenosine subtypes A1, A2A, and A3, respectively). NECA is reported to act as a potent vasodilator and can inhibit platelet aggregation by increasing cAMP (EC50 = 3.1...

5'-Deoxy-5'-methylthioadenosine (MTA) is an intermediate in the generation of adenine and methionine that is produced by the decarboxylation of S-adenosylmethionine. This nucleoside is a potent agonist of adenosine receptors (Kis = 0.15, 1.13, 13.9, and 0.68 µM for A1, A2A, A2B, and A3, respectively). At higher...

2-Chloroadenosine (CADO) is a metabolically stable analog of adenosine that binds to adenosine A1, A2A, and A3 receptors with Ki values of 300, 80, and 1,900 nM, respectively. CADO has been used to activate adenosine receptors in the thalamus, generating anticonvulsive activity in a rat model of generalized...

5'-Deoxy-5'-methylthioadenosine-d3 (MTA-d3) is intended for use as an internal standard for the quantification of MTA (Cay-15593) by GC- or LC-MS. MTA is an intermediate in the generation of adenine and methionine that is produced by the decarboxylation of S-adenosylmethionine. This nucleoside is a potent agonist of...

Theobromine is a methylxanthine alkaloid and derivative of caffeine (Cay-14118) that has been found in cocoa beans and has diverse biological activities. It is an adenosine A1 receptor antagonist (IC50s = 200-280 µM in radioligand binding assays using rat brain membranes). Theobromine (150 µg/ml) increases AMPK...

7-Methylxanthine is an adenosine A1 receptor antagonist and active metabolite of theobromine (Cay-21745) and caffeine (Cay-14118). It inhibits binding of the adenosine A1 receptor agonist cyclohexyladenosine in rat cerebral cortical membranes in a concentration-dependent manner. 7-Methylxanthine (300 mg/kg) inhibits...

Description: 4-Methyl-2-oxopentanoic acid is an abnormal metabolite, a neurotoxin and a metabolic toxin. Target: Endogenous Metabolite. Smiles: CSC[C@H]1O[C@H]([C@H](O)[C@@H]1O)n1cnc2c(N)ncnc12. References: Avila MA, et al. Methylthioadenosine. Int J Biochem Cell Biol. 2004 Nov,36(11):2125-30.

KW 3902 is an antagonist of the adenosine A1 receptor (Ki = 0.19 nM). It displays 890-fold selectivity for A1 receptors over A2A receptors and has no activity at A3 receptors. KW 3902 less potently inhibits human organic anion transporter 1 (OAT1, Ki = 7.82 µM). KW 3902 exhibits renal protective effects during...

N6-Cyclopentyladenosine is a selective agonist at adenosine 1 receptors (A1Rs) (Kis = 2.3, 790, and 43 nM for A1R, A2R, and A3R receptors, respectively, in transfected CHO cells). When microinjected into the rat brainstem, it increases blood pressure and heart rate. It is effective for pain in normal and...