1. GPCR/G Protein Apoptosis
  2. Adenosine Receptor Apoptosis
  3. Piclidenoson

Piclidenoson  (Synonyms: IB-MECA; CF-101)

Cat. No.: HY-13591 Purity: 99.28%
COA Handling Instructions

Piclidenoson (IB-MECA) is a first-in-class, orally active and selective A3 adenosine receptor (A3AR) agonist. Piclidenoson exhibits antiproliferative effect and induces apoptosis in different cancer cell types like melanoma, leukemia. Piclidenoson can be used for the research of autoimmune inflammatory diseases and COVID-19.

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

Piclidenoson Chemical Structure

Piclidenoson Chemical Structure

CAS No. : 152918-18-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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USD 135 In-stock
Solution
10 mM * 1 mL in DMSO USD 135 In-stock
Solid
5 mg USD 120 In-stock
10 mg USD 190 In-stock
25 mg USD 400 In-stock
50 mg USD 640 In-stock
100 mg USD 990 In-stock
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Based on 4 publication(s) in Google Scholar

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Description

Piclidenoson (IB-MECA) is a first-in-class, orally active and selective A3 adenosine receptor (A3AR) agonist. Piclidenoson exhibits antiproliferative effect and induces apoptosis in different cancer cell types like melanoma, leukemia. Piclidenoson can be used for the research of autoimmune inflammatory diseases and COVID-19[1][2][3][4].

IC50 & Target

A3AR[2]

In Vitro

Piclidenoson is able to inhibit Forskolin (HY-15371)-stimulated cAMP levels with EC50s of 0.82 μM and 1.2 μM in OVCAR-3 cells and Caov-4 cells, respectively[2].
Piclidenoson (0.0001-100 μM; 48 hours) significantly reduces cell viability in a dose-dependent manner in human ovarian cancer cell lines, with IC50s of 32.14 μM and 45.37 μM for OVCAR-3 and Caov-4 cells, respectively[2].
Piclidenoson (0.001-100 μM; 48 hours) induces apoptosis in ovarian cancer cell line through the caspase pathway[2].
Piclidenoson induces apoptosis via the mitochondrial signaling pathway[2].

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

Cell Proliferation Assay[2]

Cell Line: OVCAR-3 cells, Caov-4 cells
Concentration: 0.0001-100 μM
Incubation Time: 48 hours
Result: Resulted in a dose-dependent reduction in the cell viability.

Apoptosis Analysis[2]

Cell Line: OVCAR-3 cells, Caov-4 cells
Concentration: 0.1 μM, 1 μM, 10 μM, 50 μM, 100 μM
Incubation Time: 48 hours
Result: Significant increased in the percentage of apoptosis in a concentration-dependent manner.

Western Blot Analysis[2]

Cell Line: OVCAR-3 cells, Caov-4 cells
Concentration: 1 μM, 10 μM, 100 μM
Incubation Time: 48 hours
Result: Decreased the expression of Bcl-2 was noticeably and increased the expression of Bax protein.
In Vivo

Piclidenoson (105 μg/kg; i.p.) enhances survival of γ-irradiated mice[3].

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

Animal Model: B10CBAF1 male mice aged 3 months (average 30 g)[1]
Dosage: 105 μg/kg
Administration: Intraperitoneal injection, 0.5 h after irradiation
Result: Resulted in statistically significant increases of the mean survival time in comparison with the control irradiated mice.
Clinical Trial
Molecular Weight

510.29

Formula

C18H19IN6O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@H]1[C@H](N2C=NC3=C(NCC4=CC=CC(I)=C4)N=CN=C23)O[C@H](C(NC)=O)[C@H]1O

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 : ≥ 45 mg/mL (88.19 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9597 mL 9.7983 mL 19.5967 mL
5 mM 0.3919 mL 1.9597 mL 3.9193 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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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

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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: ≥ 2.5 mg/mL (4.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (4.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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
DMSO 1 mM 1.9597 mL 9.7983 mL 19.5967 mL 48.9917 mL
5 mM 0.3919 mL 1.9597 mL 3.9193 mL 9.7983 mL
10 mM 0.1960 mL 0.9798 mL 1.9597 mL 4.8992 mL
15 mM 0.1306 mL 0.6532 mL 1.3064 mL 3.2661 mL
20 mM 0.0980 mL 0.4899 mL 0.9798 mL 2.4496 mL
25 mM 0.0784 mL 0.3919 mL 0.7839 mL 1.9597 mL
30 mM 0.0653 mL 0.3266 mL 0.6532 mL 1.6331 mL
40 mM 0.0490 mL 0.2450 mL 0.4899 mL 1.2248 mL
50 mM 0.0392 mL 0.1960 mL 0.3919 mL 0.9798 mL
60 mM 0.0327 mL 0.1633 mL 0.3266 mL 0.8165 mL
80 mM 0.0245 mL 0.1225 mL 0.2450 mL 0.6124 mL
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Piclidenoson Related Classifications

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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