DPCPX |
| رقم الكتالوجGC16099 |
DPCPX (PD 116948) ، أحد مشتقات الزانثين ، هو أحد مضادات مستقبلات الأدينوزين A1 شديدة القوة والانتقائية ، مع Ki 0.46 نانومتر في 3H-CHA المرتبطة بمستقبلات A1 في أغشية الدماغ الكاملة للفئران
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 102146-07-6
Sample solution is provided at 25 µL, 10mM.
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DPCPX is a potent and selective high affinity A1 adenosine receptor antagonist with a Ki value of 0.45nM for adenylate cyclase in rat fat cell membranes [1]. The A1 adenosine receptor is an important G protein-coupled receptor whose activation inhibits adenylyl cyclase activity, regulates calcium ion channels, and inhibits potassium ion channels, thereby modulating cardiac function, neurotransmission, and various physiological processes[2]. DPCPX is a xanthine analog that competitively binds to the adenosine binding site on the A1 adenosine receptor, inhibiting its activation. It is commonly used to study the function of A1 adenosine receptors and their roles in cardiovascular, neurological, metabolic systems, and certain cancers[1,3].
DPCPX is used to evaluate pharmacological differences in A1 adenosine receptors from different sources. [3H]-DPCPX was used to treat the membranes of human, guinea pig, rat, and mouse brains (treatment concentrations and times were: human: 0.7nM, 120min; guinea pig: 0.2nM, 60min; rat and mouse: 0.1nM, 20min). DPCPX exhibited significant differences in binding properties to membranes from different species, while maintaining relatively consistent binding affinity across different brain regions within the same species[4]. Treatment of MCF-7 cells with DPCPX (87nM) for 24, 48, and 72h resulted in increased expression of p53, caspase 3, 8, and 9, and a decrease in cell viability, indicating that DPCPX promotes apoptosis in MCF-7 cells[5].
DPCPX (1mg/kg) administered intraperitoneally to mice significantly reduced renal damage caused by the radiocontrast agent iohexol[6]. DPCPX (0.25mg/kg) administered subcutaneously to rats significantly increased the mortality rate, neurological deficit scores, and brain infarction volume in middle cerebral artery occlusion (MCAO) rats, while reducing the neuroprotective effects of tetramethylpyrazine (TSG) [7].
References:
[1] Lohse M, Klotz K N, Lindenborn-Fotinos J, et al., 8-Cyclopentyl-1,3-dipropylxanthine (DPCPX) — a selective high affinity antagonist radioligand for A1 adenosine receptors, Naunyn-Schmiedeberg's archives of pharmacology[J]. 1987, 336: 204-210.
[2] Linden J, Structure and function of A1 adenosine receptors, FASEB journal : official publication of the Federation of American Societies for Experimental Biology[J]. 1991,12: 2668-76.
[3] Moro S, Gao Z G, Jacobson K A, et al., Progress in the pursuit of therapeutic adenosine receptor antagonists, Medicinal Research Reviews[J]. 2005, 26: 131-159.
[4] Maemoto T, Finlayson K, Olverman H J, Akahane A, et al., Species differences in brain adenosine A1 receptor pharmacology revealed by use of xanthine and pyrazolopyridine based antagonists, British Journal of Pharmacology[J]. 1997, 122: 1202-1208.
[5] Dastjerdi M N, Rarani M Z, Valiani A, et al., The effect of adenosine A1 receptor agonist and antagonist on p53 and caspase 3, 8, and 9 expression and apoptosis rate in MCF-7 breast cancer cell line, Research in Pharmaceutical Sciences[J]. 2016, 11: 303-310.
[6] Lee H T, Jan M, Bae S C, et al., A1 adenosine receptor knockout mice are protected against acute radiocontrast nephropathy in vivo, American Journal of Physiology-Renal Physiology[J]. 2006, 290: F1367-F1375.
[7] Ruan L, Li G, Zhao W, et al., Activation of Adenosine A1 Receptor in Ischemic Stroke: Neuroprotection by Tetrahydroxy Stilbene Glycoside as an Agonist, Antioxidants[J]. 2021, 10: 1112.
| Cell experiment [1]: | |
Cell lines | MCF-7 cells |
Preparation Method | MCF-7 cells were seeded into 24-well plates with 104 cells per well and cultured for 24h. They were treated with different concentrations (0, 87nM) of DPCPX.DMSO was added at 24, 48, 72, and 96h, and 100µl aliquot of the soluble fraction was transferred into 96-well plates, and the optical density (OD) was measured by a plate reader. |
Reaction Conditions | 0, 87nM; 24, 48, 72h |
Applications | DPCPX significantly inhibited the survival rate of MCF-7 cells in a time-dependent manner. |
| Animal experiment [2]: | |
Animal models | kidney injury model mice |
Preparation Method | Mice were injected with a nitric oxide synthase inhibitor (NG-nitro-L-arginine methyl ester, 10mg/kg) and an inhibitor of prostaglandin synthesis (indomethacin, 10mg/kg) intraperitoneally (ip) to inhibit the protective mechanisms in the kidneys. Part of them were pretreated with 1 mg/kg DPCPX ip. After 15min, the mice were injected with iohexol (350mg iodine/ml) ip. Renal function was assessed by measuring plasma Cr 24h after radiocontrast injection by a colorimetric method. |
Dosage form | 1mg/kg for 15min; i.p. |
Applications | Treatment of DPCPX significantly protected against radiocontrast nephropathy. |
References: | |
| Cas No. | 102146-07-6 | SDF | |
| Chemical Name | 8-cyclopentyl-1,3-dipropyl-1H-purine-2,6(3H,7H)-dione | ||
| Canonical SMILES | O=C1N(CCC)C(N(CCC)C2=C1NC(C3CCCC3)=N2)=O | ||
| Formula | C16H24N4O2 | M.Wt | 304.39 |
| الذوبان | <1.52mg/ml in DMSO; <3.04mg/ml in ethanol | 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 | 3.2853 mL | 16.4263 mL | 32.8526 mL |
| 5 mM | 657.1 μL | 3.2853 mL | 6.5705 mL |
| 10 mM | 328.5 μL | 1.6426 mL | 3.2853 mL |
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)
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