Adenosine Kinase Inhibitor (hydrate) (Synonyms: ABT-702) |
| Katalog-Nr.GC16930 |
inhibitor of adenosine kinase
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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IC50: 1.7 nM in cell-free assays
Adenosine Kinase Inhibitor is an inhibitor of adenosine kinase.
Adenosine kinase is the key metabolizing enzyme regulating cellular adenosine concentrations. Inhibition of adenosine kinase can selectively enhance the protective actions of adenosine during tissue trauma without producing the nonspecific effects associated with the systemic administration of adenosine receptor agonists.
In vitro: Adenosine Kinase Inhibitor was found to be a potent non-nucleoside adenosine kinase inhibitor with several folds of magnitude selectivity over other sites of adenosine interaction. Adenosine Kinase Inhibitor was 1300- to 7700-fold selective for adenosine kinase compared with other neurotransmitter and peptide receptors, neurotransmitter/nucleoside reuptake sites, and enzymes. Adenosine Kinase Inhibitor was equipotent in inhibiting native human adenosine kinase, human recombinant isoforms, as well as adenosine kinase from dog, rat, monkey, and mouse brain [1].
In vivo: Adenosine Kinase Inhibitor was orally active and efficacious in reducing acute somatic nociception in the mouse hot-plate assay. Adenosine Kinase Inhibitor could dose-dependently reduce nociception in the phenyl-p-quinone-induced abdominal constriction assay. The antinociceptive effects of Adenosine Kinase Inhibitor in the hotplate assay were stop by the nonselective adenosine receptor antagonist theophylline, but not by a peripherally selective adenosine receptor antagonist [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Jarvis, M. F.,Yu, H.,Kohlhaas, K., et al. ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholino-pyridin-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 antinociceptive effects in the mouse. Journal of Pharmacology and Experimental Therapeutics 295(3), 1156-1164 (2000).
| Cas No. | SDF | ||
| Überlieferungen | ABT-702 | ||
| Chemical Name | 5-(3-bromophenyl)-7-[6-(4-morpholinyl)-3-pyridinyl]-pyrido[2,3-d]pyrimidin-4-amine, hydrate (5:2) | ||
| Canonical SMILES | BrC1=CC=CC(C2=CC(C3=CN=C(N4CCOCC4)C=C3)=NC5=C2C(N)=NC=N5)=C1.O | ||
| Formula | C22H19BrN6O • 0.4H2O | M.Wt | 470.5 |
| Löslichkeit | ≤30mg/ml in DMSO;20mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1254 mL | 10.627 mL | 21.254 mL |
| 5 mM | 0.4251 mL | 2.1254 mL | 4.2508 mL |
| 10 mM | 0.2125 mL | 1.0627 mL | 2.1254 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)
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