ABT 702 dihydrochloride |
| رقم الكتالوجGC13416 |
ثنائي هيدروكلوريد ABT 702 هو مثبط قوي لأدينوزين كيناز (AK) (IC50 \u003d 1.7 نانومتر).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1188890-28-9
Sample solution is provided at 25 µL, 10mM.
;)
_1-7.$$$37316672@70.jpg');)
;)
;)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
;)
;)
;)
_1124-1138.$$$35908550@30.jpg');)
_766-780.$$$37100057@30.jpg');)
_418-432.$$$36893736@30.jpg');)
_240-255.$$$35108512@29.jpg');)
_533-545.$$$36543525@28.jpg');)
_264-276.$$$36600053@22.jpg');)
_2214998.$$$@0.jpg');)
IC50: 1.7 nM for adenosine kinase
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].
Clinical trial: Up to now, ABT 702 is still in the preclinical development stage.
Reference:
[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.
Animal experiment: | Rats[2]Rats are fasted for 16 hours prior to use. At the beginning of the experiment, each rat is weighed, and then anesthetized using 5% isoflurane for induction and 2.5% for maintenance. A blood sample from tail vein is collected for a fasting blood glucose determination using a standard glucometer. Rats are then given an intraperitoneal (i.p.) injection of DPCPX (3 mg/kg, n=4), ABT-702 (3 mg/kg, n=4), or an equivalent volume of vehicle (15% dimethyl sulfoxide, 15% cremophor EL, 70% saline, n=4) to manipulate the effect of endogenous adenosine on neuronal activities. Ten minutes after i.p. injection, rats are administered FDG (15.4±0.7 MBq) in 0.3-0.5 mL saline by intravenous (i.v.) tail vein injection. Rats are allowed to recover from anesthesia after the FDG injection but are reanesthetized for 15-minute-static PET scan with the head in the center of the field of view. All images are reconstructed[2]. |
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 antinociceptive effects in the mouse. J Pharmacol Exp Ther. 2000 Dec;295(3):1156-64. | |
| Cas No. | 1188890-28-9 | SDF | |
| Chemical Name | 5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2,3-d]pyrimidin-4-amine dihydrochloride | ||
| Canonical SMILES | BrC1=CC=CC(C2=CC(C3=CN=C(N4CCOCC4)C=C3)=NC5=NC=NC(N)=C25)=C1.Cl.Cl | ||
| Formula | C22H19N6OBr.2HCl | M.Wt | 536.26 |
| الذوبان | ≥ 107.2 mg/mL in DMSO, ≥ 9.84 mg/mL in EtOH with ultrasonic and warming | 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 | 1.8648 mL | 9.3238 mL | 18.6477 mL |
| 5 mM | 0.373 mL | 1.8648 mL | 3.7295 mL |
| 10 mM | 0.1865 mL | 0.9324 mL | 1.8648 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 31 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *