ABT 702 Dihydrochloride Property

storage temp. 

Inert atmosphere,Store in freezer, under -20°C

solubility 

insoluble in H2O; ≥107.2 mg/mL in DMSO; ≥9.84 mg/mL in EtOH with gentle warming and ultrasonic

form 

solid

color 

Orange

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

ABT 702 Dihydrochloride Chemical Properties,Usage,Production

Biological Activity

adenosine (ado) is an endogenous homeostatic inhibitory neuromodulator that reduces cellular excitability at sites of tissue injury and inflammation. inhibition of adenosine kinase (ak), the primary metabolic enzyme for ado, selectively increases ado concentrations at sites of tissue trauma and enhances the analgesic and antiinflammatory actions of ado. abt 702 is a novel, potent nonnucleoside ak inhibitor.

in vitro

abt 702 was active both in inhibiting ak (ic50 ) 1.7 nm) and ado phosphorylation in the intact cells (ic50 ) 50 nm). abt 702 was also highly selective for ak inhibition as compared to other sites of ado action including ada, ado receptors, and ado transport sites [1].

in vivo

abt 702 had dose-dependent antinociceptive and antiinflammatory actions in a variety of animal models of nociceptive, inflammatory, and neuropathic pain. abt 702 is the first of a novel class of potent, selective, non-nucleoside, orally active ak inhibitors that have potent antinociceptive effects in animal models [1].

IC 50

1.7 nm for adenosine kinase

References

[1] lee ch, jiang m, cowart m, gfesser g, perner r, kim kh, gu yg, williams m, jarvis mf, kowaluk ea, stewart ao, bhagwat ss. discovery of 4-amino-5-(3-bromophenyl)-7-(6-morpholino-pyridin-3-yl)pyrido[2,3-d]pyrimidine, an orally active, non-nucleoside adenosine kinase inhibitor.. j med chem. 2001 jun 21;44(13):2133-8.