1. GPCR/G Protein Apoptosis
  2. Adenosine Receptor Apoptosis
  3. N6-Cyclopentyladenosine

N6-Cyclopentyladenosine  (Synonyms: CPA; UK-80882)

Cat. No.: HY-103181 Purity: 99.59%
Handling Instructions Technical Support

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.

For research use only. We do not sell to patients.

N6-Cyclopentyladenosine Chemical Structure

N6-Cyclopentyladenosine Chemical Structure

CAS No. : 41552-82-3

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10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

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[1][2][3][4][5][6][7][8][9].

IC50 & Target

Ki: 2.3 nM (A1), 790 nM (A2A), 43 nM(A3)[1].

Cellular Effect
Cell Line Type Value Description References
Caco-2 GI50
> 250 μM
Compound: 14, CPA
Antitumor activity against human CaCo2 cells after 48 hrs by MTS assay
Antitumor activity against human CaCo2 cells after 48 hrs by MTS assay
[PMID: 18588281]
HEK-293T EC50
0.0063 μM
Compound: 5
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
[PMID: 22738238]
HT-29 GI50
> 250 μM
Compound: 14, CPA
Antitumor activity against human HT29 cells after 48 hrs by MTS assay
Antitumor activity against human HT29 cells after 48 hrs by MTS assay
[PMID: 18588281]
K562 GI50
> 250 μM
Compound: 14, CPA
Antitumor activity against human K562 cells after 48 hrs by MTS assay
Antitumor activity against human K562 cells after 48 hrs by MTS assay
[PMID: 18588281]
MCF7 GI50
> 250 μM
Compound: 14, CPA
Antitumor activity against human MCF7 cells after 48 hrs by MTS assay
Antitumor activity against human MCF7 cells after 48 hrs by MTS assay
[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.

Apoptosis Analysis[3]

Cell Line: HL-60 cells
Concentration: 100 μM
Incubation Time: 12 h、24 h
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

N6-Cyclopentyladenosine (200 nmol/kg; i.p.; single dose; 22 h before 5-fluorouracil administration) protects the hematopoietic progenitor cells (CFC-GM) in the bone marrow from the cytotoxic damage of 5-fluorouracil (HY-90006) in the 5-fluorouracil-induced hematopoietic damage model of B10CBAF1 mice[4]. N6-Cyclopentyladenosine (1 mg/kg; i.p.) suppresses rapid eye movement (REM) sleep and enhances electroencephalographic slow wave activity during non-rapid eye movement (NREM) sleep in rats[5]. N6-Cyclopentyladenosine (0.15-2.25 μmol/kg; i.p.; single dose; 30 min before training) impairs the memory retention of passive avoidance tasks in mice in a dose-dependent manner in the mouse passive avoidance behavior experiment[6]. N6-Cyclopentyladenosine (2-4 mg/kg; i.p.; single dose; 15 min before aminophylline administration) delays the onset of aminophylline-induced clonic convulsions in the mouse model of aminophylline-induced recurrent generalized seizures, but cannot prevent the death of mice within 24 h[9].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

335.36

Formula

C15H21N5O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC[C@@H]1[C@H]([C@H]([C@H](N2C=NC3=C2N=CN=C3NC4CCCC4)O1)O)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9819 mL 14.9094 mL 29.8187 mL
5 mM 0.5964 mL 2.9819 mL 5.9637 mL
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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 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 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

* 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.

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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