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Chemical Structure| 1188890-28-9 Chemical Structure| 1188890-28-9

Structure of ABT-702 2HCl
CAS No.: 1188890-28-9

Chemical Structure| 1188890-28-9

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ABT702 2HCl is a potent non-nucleoside adenosine kinase inhibitor with IC50 value of 1.7 nM, displaying oral activity in animal models of pain and inflammation.

Synonyms: ABT 702 dihydrochloride; ABT-702 dihydrochloride

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Product Details of ABT-702 2HCl

CAS No. :1188890-28-9
Formula : C22H21BrCl2N6O
M.W : 536.25
SMILES Code : NC1=C(C(C2=CC=CC(Br)=C2)=CC(C3=CC=C(N4CCOCC4)N=C3)=N5)C5=NC=N1.[H]Cl.[H]Cl
Synonyms :
ABT 702 dihydrochloride; ABT-702 dihydrochloride
MDL No. :MFCD03452809
InChI Key :OOXNYFKPOPJIOT-UHFFFAOYSA-N
Pubchem ID :16760265

Safety of ABT-702 2HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
H9c2 cells 1 µM 12 hours hypoxia/4 hours reoxygenation To evaluate the effect of ABT-702 on H/R-induced apoptosis and necroptosis. Results showed that ABT-702 pre-treatment significantly reduced H/R-induced apoptosis and necroptosis in H9c2 cells. J Cell Mol Med. 2021 Mar;25(6):2931-2943.
HepG2 cells 30 µM 14-24 hours hypoxia followed by 4-24 hours re-oxygenation To evaluate the effect of ABT-702 on the protective effects of adenosine and inosine under hypoxia and re-oxygenation conditions. Results showed that ABT-702 significantly reversed the protective effects of both adenosine and inosine. Int J Mol Med. 2013 Feb;31(2):437-46.
C6 rat glioma cells 0.1 µM 24 hours or 48 hours To evaluate the inhibitory effect of ABT-702 on adenosine kinase and its impact on MTX-mediated cytotoxicity. Results showed that ABT-702 alone did not affect C6 cell viability and failed to alter the cytotoxic effect of MTX. Purinergic Signal. 2021 Jun;17(2):273-284.
Human coronary arterioles 0.1 µM 30 minutes To evaluate the effect of ABT-702 on conducted vasodilation in HFpEF patients, results showed that ABT-702 significantly augmented conducted vasodilation in HFpEF patients Circ Heart Fail. 2019 Aug;12(8):e005762.
Rat gracilis skeletal muscle arteries 0.1 µM 30 minutes To evaluate the effect of ABT-702 on conducted vasodilation, results showed that ABT-702 significantly augmented conducted vasodilation in obese ZSF1 rats Circ Heart Fail. 2019 Aug;12(8):e005762.
Human glomerular endothelial cells (HGECs) 50 µM 5 days To evaluate the effects of ABT702 on glomerular permeability, barrier function, and inflammation in human glomerular endothelial cells under high glucose conditions. ABT702 significantly reduced high glucose-induced elevation in FITC-dextran permeability and MAPK phosphorylation and restored the decrease in occludin expression. Pharmacol Res. 2014 Jul;85:45-54.
Rat astrocytes 10 µM 60 minutes ABT-702 completely prevented the adenosine-accelerated ATP restoration Neurochem Res. 2024 Nov 16;50(1):13.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Sprague-Dawley rats Spinal nerve ligation (L5/L6) and carrageenan inflammation model Subcutaneous injection 0.1, 1 and 10 mg/kg Tests every 10 min for 60 min per dose To investigate the effect of ABT-702 on spinal neurons in inflammatory and neuropathic pain models. Results showed that ABT-702 significantly inhibited postdischarge, wind-up, and C-fibre evoked responses in spinal neurons, with greater inhibition observed in the nerve injury model. Br J Pharmacol. 2001 Apr;132(7):1615-23
C57BL/6 mice Streptozotocin-induced diabetes model Intraperitoneal injection 1.5 mg/kg Twice a week for 8 weeks To evaluate the protective effects of ABT702 on renal inflammation and oxidative stress in diabetic mice. ABT702 significantly reduced blood glucose levels, albuminuria, markers of glomerular injury (nephrinuria and podocalyxin excretion), NADPH oxidase activity, TBARS excretion, renal macrophage infiltration, NF-κB activation, and MCP-1 excretion, while increasing eNOS expression and nitrate/nitrite excretion in diabetic mice. Pharmacol Res. 2014 Jul;85:45-54.
Obese ZSF1 rats HFpEF model Intraperitoneal injection 1.5 mg/kg Twice a week for eight weeks To evaluate the effect of ABT-702 on LV diastolic function, results showed that ABT-702 prevented LV diastolic dysfunction and improved conducted vasodilation and LV diastolic function Circ Heart Fail. 2019 Aug;12(8):e005762.
C57BL/6J mice Age-related hearing loss model Intraperitoneal injection 1.5 mg/kg Twice a week for 6 months or 3 months To evaluate the protective effect of ABT-702 on age-related hearing loss. Results showed that ABT-702 treatment significantly reduced ABR threshold shifts at 10 and 16 kHz and increased hair cell survival in the apical region of the cochlea. Exp Gerontol. 2011 Nov;46(11):905-14
C57BL/6 mice Myocardial ischemia/reperfusion injury model Intraperitoneal injection 2 mg/kg Single dose, sustained for 30 minutes ischemia/4 or 24 hours reperfusion To evaluate the protective effect of ABT-702 on myocardial ischemia/reperfusion injury. Results showed that ABT-702 significantly reduced myocardial infarct size, improved cardiac function, and reduced cell apoptosis and necroptosis. J Cell Mol Med. 2021 Mar;25(6):2931-2943.
Sprague-Dawley rats Cocaine sensitization model Intra-NAc microinjection 2.5 ng/side or 5 ng/side Single administration, observed for 2 hours ABT-702 dose-dependently blocked the expression of cocaine sensitization while having no effects on acute cocaine sensitivity, suggesting that upregulation of endogenous adenosine in the accumbens is sufficient to non-selectively stimulate adenosine receptors and reverse the expression of cocaine sensitization. Neuropharmacology. 2012 Nov;63(6):1172-81
Mice WT C57BL/6 mice and Adk-tg transgenic mice Intraperitoneal injection 2.5, 5, and 10 mg/kg Single administration To evaluate the antipsychotic-like activity of ABT-702 in normal mice and to reverse apomorphine-induced PPI disruption. ABT-702 enhanced basal PPI and reversed apomorphine-induced PPI disruption. J Clin Invest. 2012 Jul;122(7):2567-77
Sprague-Dawley rats Chronic constriction injury (CCI) model Intraperitoneal injection 5 mg/kg Single dose ABT-702 produces powerful analgesic effects in rodent models of experimental neuropathic pain by increasing endogenous adenosine levels through selective adenosine kinase inhibition, mediated via the A3 adenosine receptor (A3AR) signaling pathway. Brain. 2015 Jan;138(Pt 1):28-35
C57BL/6 mice Chronic constriction injury (CCI) model Intraperitoneal injection 5 mg/kg Single dose ABT-702 produces powerful analgesic effects in rodent models of experimental neuropathic pain by increasing endogenous adenosine levels through selective adenosine kinase inhibition, mediated via the A3 adenosine receptor (A3AR) signaling pathway. Brain. 2015 Jan;138(Pt 1):28-35

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.86mL

0.37mL

0.19mL

9.32mL

1.86mL

0.93mL

18.65mL

3.73mL

1.86mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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