This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
Adenosine receptor inhibitor 1
Catalog No. T61850 CAS
2550400-52-5
Adenosine receptor inhibitor 1 is a highly potent and selective antagonist of adenosine receptor (AR). It exhibits exceptional affinity for A1 AR, A2A AR, A2B AR, and A3 AR, with respective Ki values of <1000, 68.5, <1000, <1000 nM. This compound demonstrates notable antinociceptive, anti-inflammatory, and peripheral analgesic properties. Therefore, Adenosine receptor inhibitor 1 holds great promise for investigating cancer and neurodegenerative diseases [1].
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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
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Biological Description
Chemical Properties
Storage
& Solubility Information
Description
Adenosine receptor inhibitor 1 is a highly potent and selective antagonist of adenosine receptor (AR). It exhibits exceptional affinity for A1 AR, A2A AR, A2B AR, and A3 AR, with respective Ki values of >1000, 68.5, >1000, >1000 nM. This compound demonstrates notable antinociceptive, anti-inflammatory, and peripheral analgesic properties. Therefore, Adenosine receptor inhibitor 1 holds great promise for investigating cancer and neurodegenerative diseases [1].
In vitro
Compound 12d, an adenosine receptor inhibitor, demonstrates metabolic stability with 96.56% and 97.97% of the parent compound remaining after a 120-minute incubation with mouse liver microsomes (MLMs) and rat liver microsomes (RLMs), respectively [1].
In vivo
Adenosine receptor inhibitor 1 administered intraperitoneally (i.p.) at doses of 20, 30, 40 mg/kg demonstrated concentration-dependent antinociceptive effects, reducing the pain response in animal models. Specifically, at a 20 mg/kg dose, it exhibited an anti-inflammatory effect, reducing edema in a carrageenan-induced model, and at doses of 5, 10, 20 mg/kg, it showed significant analgesic effects in mice, reducing pain from peripheral sources. In an 18-26 g male albino Swiss mouse model with chronic pain induced by 5% formalin, doses of 20, 30, 40 mg/kg decreased the licking/biting time of the irritated paw. In 150-180 g male Wistar rats experiencing carrageenan-induced edema, a 20 mg/kg dose inhibited edema by 23.3%, 54.2%, and 66.0% over 1, 2, and 3 hours, respectively. Furthermore, in mice injected with irritants such as phenylbenzoquinone or acetic acid to induce pain, doses of 5, 10, 20 mg/kg led to a decrease in pain manifestations by 32.9%, 54.9%, and 82.0%, respectively.
Molecular Weight
395.82
Formula
C17H19ClFN5O3
CAS No.
2550400-52-5
Storage
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Dose Conversion
You can also refer to dose conversion for different animals.
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Method for preparing DMSO master liquid: mg
drug pre-dissolved in μL DMSO (Master liquid concentration
mg/mL),
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL PEG300, mix and clarify, next add μL
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:
Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.