Structure of ABT-702 2HCl
CAS No.: 1188890-28-9
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
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
4.5
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Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
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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 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
Rat astrocytes | 10 µM | 60 minutes | ABT-702 completely prevented the adenosine-accelerated ATP restoration | PMC11569012 |
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. | PMC7957171 |
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. | PMC3981016 |
C6 rat glioma cells | 0.1μM | 24 h or 48 h | 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. | PMC8155188 |
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 | PMC6750030 |
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 | PMC6750030 |
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. | PMC4302753 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
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. | PMC4302753 |
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. | PMC4285194 |
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. | PMC4285194 |
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. | PMC3386823 |
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 | PMC6750030 |
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. | PMC7957171 |
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. | PMC1572706 |
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. | PMC3427408 |
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. | PMC3200489 |
Tags: ABT-702 | ABT702 | ABT 702 | Adenosine Kinase | ADK | ABT-702 dihydrochloride | adenosine kinase inhibitor | adenosine metabolism | adenosine signaling | 1188890-28-9
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