N6-Cyclopentyladenosine
Based on 1 Customer Validation
N6-Cyclopentyladenosine (CPA) is a selective Adenosine A1 receptor agonist, with Ki values of 2.3 nM, 790 nM and 43 nM for human A1, A2A and A3 receptors, respectively. N6-cyclopentyladenosine increases Apoptosis. N6-Cyclopentyladenosine has antitumor activity against leukemia. N6-cyclopentyladenosine improves 5-fluorouracil (HY-90006)-induced hematopoietic damage, regulates sleep, and delays Aminophylline-induced clonic epileptic seizures.
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- Pureté : 99.95%
- CAS No.: 41552-82-3
- Formule: C15H21N5O4
- Masse moléculaire:335.36
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
Ki: 2.3 nM (A1), 790 nM (A2A), 43 nM(A3)[1].
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Caco-2 | GI50 |
>250 μM
Compound: 14, CPA
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Antitumor activity against human CaCo2 cells after 48 hrs by MTS assay
Antitumor activity against human CaCo2 cells after 48 hrs by MTS assay
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[PMID: 18588281] |
| HEK-293T | EC50 |
0.0063 μM
Compound: 5
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Agonist activity at human A1AR expressed in HEK293T/17 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 10 mins by luciferase reporter assay
Agonist activity at human A1AR expressed in HEK293T/17 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 10 mins by luciferase reporter assay
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[PMID: 22738238] |
| HT-29 | GI50 |
>250 μM
Compound: 14, CPA
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Antitumor activity against human HT29 cells after 48 hrs by MTS assay
Antitumor activity against human HT29 cells after 48 hrs by MTS assay
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[PMID: 18588281] |
| K562 | GI50 |
>250 μM
Compound: 14, CPA
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Antitumor activity against human K562 cells after 48 hrs by MTS assay
Antitumor activity against human K562 cells after 48 hrs by MTS assay
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[PMID: 18588281] |
| MCF7 | GI50 |
>250 μM
Compound: 14, CPA
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Antitumor activity against human MCF7 cells after 48 hrs by MTS assay
Antitumor activity against human MCF7 cells after 48 hrs by MTS assay
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[PMID: 18588281] |
In Vitro
N6-Cyclopentyladenosine (100 μM, 12-24 h) decreases viability of HL-60 cells and increases the number of apoptotic HL-60 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HL-60 cells
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Concentration:100 μM
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Incubation Time:12 h、24 h
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Result:Increased the number of apoptotic cells, with approximately 10-13% of cells undergoing apoptosis at a concentration of 100 μM within 24 h.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 41552-82-3
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Appearance Solid
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Masse moléculaire 335.36
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Formule C15H21N5O4
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Color White to off-white
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SMILES
OC[C@@H]1[C@H]([C@H]([C@H](N2C=NC3=C2N=CN=C3NC4CCCC4)O1)O)O
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Synonyms
CPA; UK-80882
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvant et solubilité
In Vitro:
1 M HCl : 100 mg/mL (298.19 mM; Need ultrasonic)
DMSO : 12.5 mg/mL (37.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 2.5 mg/mL (7.45 mM; ultrasonic and warming and heat to 60°C)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (3.73 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (3.73 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
Pureté et documentation
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Fiche technique (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Klotz KN, et al. Adenosine receptors and their ligands. Naunyn Schmiedebergs Arch Pharmacol. 2000 Nov;362(4-5):382-91. [Content Brief]
[2]. Soliño M, et al. Adenosine A1 receptor: A neuroprotective target in light induced retinal degeneration. PLoS One. 2018 Jun 18;13(6):e0198838. [Content Brief]
[3]. Mlejnek P, et al. Apoptosis induced by N6-substituted derivatives of adenosine is related to intracellular accumulation of corresponding mononucleotides in HL-60 cells. Toxicol In Vitro. 2005 Oct;19(7):985-90. [Content Brief]
[4]. Pospísil M, et al. N6-cyclopentyladenosine inhibits proliferation of murine haematopoietic progenitor cells in vivo. Eur J Pharmacol. 2005 Jan 10;507(1-3):1-6. [Content Brief]
[5]. Schwierin B, et al. Effects of N6-cyclopentyladenosine and caffeine on sleep regulation in the rat. Eur J Pharmacol. 1996 Apr 11;300(3):163-71. [Content Brief]
[6]. Normile HJ, et al. N6-cyclopentyladenosine impairs passive avoidance retention by selective action at A1 receptors. Brain Res Bull. 1991 Jul;27(1):101-4. [Content Brief]
[7]. Mathôt RA, et al. Pharmacokinetic-pharmacodynamic relationship of the cardiovascular effects of adenosine A1 receptor agonist N6-cyclopentyladenosine in the rat. J Pharmacol Exp Ther. 1994 Feb;268(2):616-24. [Content Brief]
[8]. Mathôt RA, et al. Deoxyribose analogues of N6-cyclopentyladenosine (CPA): partial agonists at the adenosine A1 receptor in vivo. Br J Pharmacol. 1995 Oct;116(3):1957-64. [Content Brief]
[9]. Jaishree J, et al. Individual and combined effects of N6-cyclopentyladenosine, flunarizine and diazepam on aminophylline-induced recurrent generalized seizures in mice. Pol J Pharmacol. 2003 Jul-Aug;55(4):559-64. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO / 1 M HCl | 1 mM | 2.9819 mL | 14.9094 mL | 29.8187 mL | 74.5468 mL |
| 5 mM | 0.5964 mL | 2.9819 mL | 5.9637 mL | 14.9094 mL | |
| DMSO / 1 M HCl | 10 mM | 0.2982 mL | 1.4909 mL | 2.9819 mL | 7.4547 mL |
| 15 mM | 0.1988 mL | 0.9940 mL | 1.9879 mL | 4.9698 mL | |
| 20 mM | 0.1491 mL | 0.7455 mL | 1.4909 mL | 3.7273 mL | |
| 25 mM | 0.1193 mL | 0.5964 mL | 1.1927 mL | 2.9819 mL | |
| 30 mM | 0.0994 mL | 0.4970 mL | 0.9940 mL | 2.4849 mL | |
| 1 M HCl | 40 mM | 0.0745 mL | 0.3727 mL | 0.7455 mL | 1.8637 mL |
| 50 mM | 0.0596 mL | 0.2982 mL | 0.5964 mL | 1.4909 mL | |
| 60 mM | 0.0497 mL | 0.2485 mL | 0.4970 mL | 1.2424 mL | |
| 80 mM | 0.0373 mL | 0.1864 mL | 0.3727 mL | 0.9318 mL | |
| 100 mM | 0.0298 mL | 0.1491 mL | 0.2982 mL | 0.7455 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
N6-Cyclopentyladenosine Related Classifications
HY-103181 Related Classifications
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