Piclidenoson
Based on 9 publication(s) in Google Scholar
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.
- Purity: 99.01%
- CAS No.: 152918-18-8
- Formula: C18H19IN6O4
- Molecular Weight:510.29
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Piclidenoson
More- Cell. 2025 Sep 18;188(19):5157-5174.e20. [Abstract]
- Nat Commun. 2024 Apr 16;15(1):3252. [Abstract]
- Environ Sci Technol. 2025 Mar 11;59(9):4530-4539. [Abstract]
- Cell Death Dis. 2023 Oct 28;14(10):706. [Abstract]
- J Orthop Translat. 2024 Jun 29:47:223-234. [Abstract]
- Drug Deliv Transl Res. 2025 Mar 8. [Abstract]
- Int Immunopharmacol. 2024 May 30:133:112095. [Abstract]
- Cancers (Basel). 2022 Nov 28;14(23):5854. [Abstract]
- Bone. 2022 Feb:155:116264. [Abstract]
All Adenosine Receptor Isoforms
More
Biological Activity
A3AR[2]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | IC50 |
0.78 nM
Compound: IB-MECA
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Displacement of [3H]ABMECA from human recombinant adenosine receptor A3 expressed in CHOK1 cells after 60 mins
Displacement of [3H]ABMECA from human recombinant adenosine receptor A3 expressed in CHOK1 cells after 60 mins
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[PMID: 23403082] |
| HEK293 | EC50 |
1 nM
Compound: 1
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Inhibition of isoproterenol-stimulated cAMP accumulation in HEK 293 cells expressing human Adenosine A3 receptor
Inhibition of isoproterenol-stimulated cAMP accumulation in HEK 293 cells expressing human Adenosine A3 receptor
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[PMID: 12540233] |
| HEK293 | IC50 |
1.2 nM
Compound: IB-MECA
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Inhibitory concentration against human Adenosine A3 receptor expressed in HEK293 cells using 0.1 nM [3H]AB-MECA
Inhibitory concentration against human Adenosine A3 receptor expressed in HEK293 cells using 0.1 nM [3H]AB-MECA
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[PMID: 16250647] |
| HEK293 | ED50 |
28 nM
Compound: 1, IB-MECA
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Activity at adenosine A3 receptor expressed in HEK293 cells by inhibition of isoprotenol-stimulated cAMP gated channel
Activity at adenosine A3 receptor expressed in HEK293 cells by inhibition of isoprotenol-stimulated cAMP gated channel
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[PMID: 16487705] |
| HEK293 | IC50 |
6 x 10-10 M
Compound: IB-MECA
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Displacement of [125I]ABMECA from human recombinant adenosine A3 receptor expressed in HEK293 cells
Displacement of [125I]ABMECA from human recombinant adenosine A3 receptor expressed in HEK293 cells
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[PMID: 26988801] |
| HEK293 | IC50 |
6 x 10-10 M
Compound: IB-MECA
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Displacement of [125I]AB-MECA from human recombinant adenosine receptor A3 expressed in HEK293 cells measured after 120 mins by scintillation counting method
Displacement of [125I]AB-MECA from human recombinant adenosine receptor A3 expressed in HEK293 cells measured after 120 mins by scintillation counting method
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[PMID: 27876250] |
| ScN2a | EC50 |
>25 μM
Compound: IB-MECA
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Reduction of PrPSC accumulation in ScN2a cells
Reduction of PrPSC accumulation in ScN2a cells
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[PMID: 17201410] |
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].
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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].
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Piclidenoson (0.001-100 μM; 48 hours) induces apoptosis in ovarian cancer cell line through the caspase pathway[2].
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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.
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Cell Line:OVCAR-3 cells, Caov-4 cells
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Concentration:0.0001-100 μM
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Incubation Time:48 hours
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Result:Resulted in a dose-dependent reduction in the cell viability.
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Cell Line:OVCAR-3 cells, Caov-4 cells
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Concentration:0.1 μM, 1 μM, 10 μM, 50 μM, 100 μM
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Incubation Time:48 hours
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Result:Significant increased in the percentage of apoptosis in a concentration-dependent manner.
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Cell Line:OVCAR-3 cells, Caov-4 cells
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Concentration:1 μM, 10 μM, 100 μM
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Incubation Time:48 hours
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Result:Decreased the expression of Bcl-2 was noticeably and increased the expression of Bax protein.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:B10CBAF1 male mice aged 3 months (average 30 g)[1]
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Dosage:105 μg/kg
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Administration:Intraperitoneal injection, 0.5 h after irradiation
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Result:Resulted in statistically significant increases of the mean survival time in comparison with the control irradiated mice.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 152918-18-8
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Appearance Solid
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Molecular Weight 510.29
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Formula C18H19IN6O4
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Color White to off-white
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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
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Synonyms
IB-MECA; CF-101
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (9)
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Journal Impact Factor
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Most Recent
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Cell
Deconstructing the intercellular interactome in vascular dementia with focal ischemia for therapeutic applications. [Abstract]2025 Sep 18;188(19):5157-5174.e20. PMID: 40592323 -
Nat Commun
2024 Apr 16;15(1):3252. PMID: 38627384 -
Environ Sci Technol
IodoFinder: Machine Learning-Guided Recognition of Iodinated Chemicals in Nontargeted LC-MS/MS Analysis. [Abstract]2025 Mar 11;59(9):4530-4539. PMID: 40015982 -
Cell Death Dis
Loss of adenosine A3 receptors accelerates skeletal muscle regeneration in mice following cardiotoxin-induced injury. [Abstract]2023 Oct 28;14(10):706. PMID: 37898628 -
J Orthop Translat
Pyroptosis-related crosstalk in osteoarthritis: Macrophages, fibroblast-like synoviocytes and chondrocytes. [Abstract]2024 Jun 29:47:223-234. PMID: 39040491 -
Drug Deliv Transl Res
Local delivery of an adenosine receptor agonist reduces inflammation associated with contact hypersensitivity. [Abstract]2025 Mar 8. PMID: 40057627 -
Int Immunopharmacol
Manual acupuncture ameliorates inflammatory pain by upregulating adenosine A3 receptor in complete Freund's adjuvant-induced arthritis rats. [Abstract]2024 May 30:133:112095. PMID: 38678668 -
Cancers (Basel)
Drug Repurposing Applications to Overcome Male Predominance via Targeting G2/M Checkpoint in Human Esophageal Squamous Cell Carcinoma. [Abstract]2022 Nov 28;14(23):5854. PMID: 36497337 -
Bone
CF101 alleviates OA progression and inhibits the inflammatory process via the AMP/ATP/AMPK/mTOR axis. [Abstract]2022 Feb:155:116264. PMID: 34826631
Solvent & Solubility
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 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.
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.
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.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Shin Y, et al. Activation of Phosphoinositide Breakdown and Elevation of Intracellular Calcium in a Rat RBL-2H3 Mast Cell Line by Adenosine Analogs: Involvement of A(3)-Adenosine Receptors? Drug Dev Res. 1996 Sep 1;39(1):36-46. [Content Brief]
[2]. Abedi H, et al. Mitochondrial and caspase pathways are involved in the induction of apoptosis by IB-MECA in ovarian cancer cell lines. Tumour Biol. 2014 Nov;35(11):11027-11039. [Content Brief]
[3]. Hofer M, et al. Agonist of the adenosine A3 receptor, IB-MECA, and inhibitor of cyclooxygenase-2, meloxicam, given alone or in a combination early after total body irradiation enhance survival of γ-irradiated mice. Radiat Environ Biophys. 2014 Mar;53(1):2 [Content Brief]
[4]. Chandan Sarkar, et al. Potential Therapeutic Options for COVID-19: Current Status, Challenges, and Future Perspectives. Front Pharmacol. 2020; 11: 572870. [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 |
|---|---|---|---|---|---|
| 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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