腺苷受体激动剂，NECA-CAS 35920-39-9-Calbiochem

C₁₂H₁₆N₆O₄

308.29

MFCD00069195

A cell-permeable adenosine analog that acts a potent non-selective agonist of adenosine receptors (K_i = 14 nM, 20 nM, 2.4 µM and 6.2 nM for A₁, A_2A, A_2B, A₃, respectively). Increases intracellular cAMP production (EC₅₀ = 3.1 µM in A_2B expressing CHO cells). Shown to increase glucagon release in a dose-dependent manner and inhibit insulin release at low concentrations. Although at higher concentration some insulin release is observed. Also, displays a wide range adenosine-dependent effects, such as blocking platelet aggregation and inhibiting DNA synthesis. When administered at reperfusion, it is shown reduce infarction and block the formation of the mitochondrial permeability transition pore by activating p70S6 kinase.

Reversible: yes

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Forster, K., et al. 2006. Basic Res. Cardiol.101, 319.
de Zwart, M., et al. 1998. Nucleosides Nucleotides.17, 969.
Phillis, J. et al. 1986, Pharm. Biochem. Behavior.24, 263
Durcan, M. J., et al. 1989. Pharmacol Biochem Behav.32, 487.
Bacher, S., et al. 1982. Naunyn Schmiedebergs Arch Pharmacol.329, 67.
Cusack, N., et al. 1981. Br J Pharm.72, 443.
Londos, C., et al. 1980. Proc Natl Acad Sci.77, 2551.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

100

≥99% (HPLC)

solid

14 nM K_i

Calbiochem^®

OK to freeze
protect from light

white

DMSO: 50 mM

wet ice

2-8℃

1S/C12H16N6O4/c1-2-14-11(21)8-6(19)7(20)12(22-8)18-4-17-5-9(13)15-3-16-10(5)18/h3-4,6-8,12,19-20H,2H2,1H3,(H,14,21)(H2,13,15,16)/t6-,7+,8-,12?/m0/s1

JADDQZYHOWSFJD-QQIVLSGASA-N

10 mg in Glass bottle
Packaged under inert gas

GHS06

Danger

H300

P264 - P270 - P301 + P310 - P405 - P501

Acute Tox. 2 Oral

6.1A - Combustible, acute toxic Cat. 1 and 2 / very toxic hazardous materials

WGK 3