Pricing Availability   Qty
Description: A1 and A2B antagonist. CNS stimulant
Chemical Name: 3,7-Dihydro-1,3,7-trimethyl-1H-purine-2,6-dione
Purity: ≥99% (HPLC)
Citations (2)
Reviews (3)

Biological Activity for Caffeine

Caffeine is a central nervous system stimulant. Antagonist at A1 and A2A adenosine receptors and inhibitor of cyclic nucleotide phosphodiesterases. Mobilizes calcium from intracellular stores and inhibits benzodiazepine binding to GABA receptors.

Technical Data for Caffeine

M. Wt 194.19
Formula C8H10N4O2
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 58-08-2
PubChem ID 2519
Smiles O=C1C2=C(N=CN2C)N(C)C(N1C)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Caffeine

Solvent Max Conc. mg/mL Max Conc. mM
water 19.42 100
DMSO 9.71 50

Preparing Stock Solutions for Caffeine

The following data is based on the product molecular weight 194.19. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 5.15 mL 25.75 mL 51.5 mL
5 mM 1.03 mL 5.15 mL 10.3 mL
10 mM 0.51 mL 2.57 mL 5.15 mL
50 mM 0.1 mL 0.51 mL 1.03 mL

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References for Caffeine

References are publications that support the biological activity of the product.

Nehlig et al (1992) Caffeine and the central nervous system: mechanisms of action, biochemical, metabolic and psychostimulant effects. Brain Res.Brain Res.Rev. 17 139 PMID: 1356551

Fisone et al (2004) Caffeine as a psychomotor stimulant: mechanism of action. Cell.Mol.Life Sci. 61 857 PMID: 15095008

Chen et al (2008) Caffeine blocks disruption of blood brain barrier in a rabbit model of Alzheimer's disease. J.Neuroinflammation 5 12 PMID: 18387175

If you know of a relevant reference for Caffeine, please let us know.

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Keywords: Caffeine, Caffeine supplier, A1, A2B, antagonists, CNS, stimulant, cyclic, nucleotide, PDE, inhibitors, inhibits, non-selective, adenosines, receptors, phosphodiesterases, ryanodine, Non-selective, Adenosine, Phosphodiesterases, Ryanodine, Receptors, 2793, Tocris Bioscience

2 Citations for Caffeine

Citations are publications that use Tocris products. Selected citations for Caffeine include:

Okita et al (2015) Contrasting Effects of the Cytotoxic Anticancer Drug gemcit. and the EGFR Tyrosine Kinase Inhibitor gefi. on NK Cell-Mediated Cytotoxicity via Regulation of NKG2D Ligand in Non-Small-Cell Lung Cancer Cells. PLoS One 10 e0139809 PMID: 26439264

Seto et al (2013) Acute SimV. inhibits K ATP channels of porcine coronary artery myocytes. J Cell Sci 8 e66404 PMID: 23799098

Do you know of a great paper that uses Caffeine from Tocris? Please let us know.

Reviews for Caffeine

Average Rating: 4.7 (Based on 3 Reviews.)

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Low-dose oral caffeine induces a specific form of behavioral sensitization.
By Kevin Ball on 01/28/2019
Assay Type: In Vivo
Species: Rat

Rats had free access to untreated water or water containing 0.2 mg/ml of caffeine every other day of a 14-day experiment. This dose is relevant to human caffeine intake. Rats were tested on alternated days in an open-field arena for discrete movements (horizontal and vertical) and ambulatory distance. Results showed that although caffeine intake decreased significantly across test sessions, the number of discrete horizontal movements increased significantly, that is, showed sensitization.

PMID: 22358105 Reference
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Caffeine acts on RyR2 in HL1 cells to release ER Ca2+..
By Anonymous on 12/16/2018
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: HL-1 Atrial Muscle Cell Line

HL-1 cells were loaded with cytosolic Ca2+ sensitive dye, Fura-2AM (1 µM)+F127 (0.01%) in normal tyrode solution for 40 min and excited alternately at 340 and 380 nm and fluorescence was captured at 510 nm. When the cells are perfused with 10 mM caffeine in nominally Ca2+ free tyrode solution, caffeine acts on RyR2 to release ER Ca2+, resulting in transient cytosolic peak (shown in the figure).

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Caffeine as a tool to estimate sarcoplasmic Ca2+ content in cardiomyocytes.
By Christopher Trummer on 10/15/2018
Assay Type: In Vitro
Species: Other
Cell Line/Tissue: primary ventricular cardiomyocytes

Control or saxagliptin treated primary guinea pig cardiomyocytes were loaded with FURA-2AM (1 µM) and Pluronic F 127 (1%). Ca2+ transient decay tau evoked by caffeine (30 µM) is shown in the Image. Caffeine acts as a ryanodine receptor agonist and releases Ca2+ from sarcoplasmic reticulum into the cytosol.

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