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[CAS NO. 1188890-28-9] ABT-702 dihydrochloride
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-103161 |
| Brand: | MCE |
| CAS: | 1188890-28-9 |
Overview
| MDL | MFCD03452809 |
|---|---|
| Molecular Weight | 536.25 |
| Molecular Formula | C22H21BrCl2N6O |
| SMILES | NC1=C(C(C2=CC=CC(Br)=C2)=CC(C3=CC=C(N4CCOCC4)N=C3)=N5)C5=NC=N1.[H]Cl.[H]Cl |
Summary
ABT-702 dihydrochloride is a potent adenosine kinase ( AK ) inhibitor ( IC 50 =1.7 nM).
IC50 & Target
IC50: 1.7 nM (Adenosine kinase, AK) [1]
In Vitro
ABT-702 is an orally effective adenosine kinase inhibitor that has several orders of magnitude selectivity over other sites of adenosine (ADO) interaction (A 1 , A 2A , A 3 receptors, ADO transporter, and ADO deaminase). ABT-702 is equipotent (IC 50 =1.5±0.3 nM) in inhibiting native human AK (placenta), two human recombinant isoforms (AK long and AK short ), and AK from monkey, dog, rat, and mouse brain. ABT-702 potently inhibits the activity of rat brain cytosolic AK in a concentration-dependent manner with an IC 50 value of 1.7 nM. ABT-702 also potently inhibits AK activity in intact cultured IMR-32 human neuroblastoma cells (IC 50 =51 nM), indicating that ABT-702 can penetrate the cell membrane and potently inhibit AK at its intracellular site [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
ABT-702 significantly reduces acute thermal nociception in a dose-dependent manner after both intraperitoneal (ED 50 =8 μmol/kg i.p.) and oral (ED 50 =65 μmol/kg p.o.) administration in the mouse hot-plate test. Consistent with its antinociceptive effects in the hot-plate assay, ABT-702 also produces dose-dependent antinociceptive effects (ED 50 =2 μmol/kg i.p.) in the abdominal constriction assay. Like Morphine (21 μmol/kg i.p.), ABT-702 exhibits full efficacy in this model of persistent chemical pain [1] . Rats are given an intraperitoneal injection of the adenosine A 1 receptor antagonist DPCPX (3 mg/kg), ABT-702 (3 mg/kg), or vehicle 10 minutes prior to an intravenous injection of 2- 18 F-fluorodeoxy-D-glucose (FDG) (FDG, 15.4±0.7 MBq per rat). Rats are then subjected to a 15 minute static positron emission tomography (PET) scan. Reconstructed images are normalized to FDG PET template for rats and standard uptake values (SUVs) are calculated. To examine the regional effect of active treatment compared to vehicle, statistical parametric mapping analysis is performed. Whole-brain FDG uptake is not affected by drug treatment. Significant regional hypometabolism is detected, particularly in cerebellum, of DPCPX and ABT-702 treated rats, relative to vehicle-treated rats. Thus, endogenous adenosine can affect FDG accumulation although this effect is modest in quiescent rats. Body weight (316.8±28.4 g; mean±SD) and blood glucose (5.5±1.7 mM) are not significantly different among three groups. Whole-brain PET SUV values are 1.6±0.4, 1.6±0.6, and 1.8±0.6 for vehicle, ABT-702, and DPCPX-treated rats, respectively (F(2,9)=0.298, P=0.75). statistical parametric mapping (SPM) analysis reveals significant regional hypometabolism in the cerebellum, mesencephalic region, and medulla in the ABT-702-treated rats compared to the vehicle-treated rats [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : ≥ 33.33 mg/mL ( 62.15 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.8648 mL | 9.3240 mL | 18.6480 mL |
| 5 mM | 0.3730 mL | 1.8648 mL | 3.7296 mL |
| 10 mM | 0.1865 mL | 0.9324 mL | 1.8648 mL |
References
- [1] Jarvis MF, et al. ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinoc
- [2] Parkinson FE, et al. The Effect of Endogenous Adenosine on Neuronal Activity in Rats: An FDG PET Study. J Neuroimaging. 2016 Jul;26(4):403-5.
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