[1]. Calcium glycerophosphate preserves transepithelial integrity in the Caco-2 model of intestinal transport. World J Gastroenterol. 2015;21(30):9055-9066.

[2]. Calcium glycerophosphate as a source of calcium and phosphorus in total parenteral nutrition solutions. JPEN J Parenter Enteral Nutr. 1991;15(2):176-180.

Calcium glycerophosphate is a [DB01373] salt of glycerophosphoric acid that forms a white, fine, slightly hygroscopic powder. The commercial product is a mixture of calcium beta-, and D-, and L -alpha-glycerophosphate. By FDA, calcium glycerophosphate is considered a generally recognized as safe (GRAS) food ingredient as a nutrient supplement (source of calcium or phosphorus), or in food products such as gelatins, puddings, and fillings. It is also present in dental or oral hygiene products due to its cariostatic effects. It is suggested that calcium glycerophosphate promotes plaque-pH buffering, elevation of plaque [DB01373] and phosphate levels and direct interaction with dental mineral.
Any salt or ester of glycerophosphoric acid.

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Drug Indication
Calcium glycerophosphate is found in OTC dental products such as toothpastes for the prevention of dental caries. As OTC products these do not have an official indication. In prescription products it is indicated as a [DB01373] or phosphate donor for replacement or supplementation in patients with insufficient [DB01373] or phosphate.

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Mechanism of Action
Calcium glycerophosphate in combination with sodium monofluorophosphate was found to reduce the acid solubility of enamel. This is thought to be due to increased uptake of fluoride in a non-alkali soluble form at the expense of a fraction remaining in the alkali-soluble form of calcium fluoride. It is also thought that calcium glycerophosphate enhances the remineralization effect of sodium monofluorophosphate leading to greater remineralization of enamel but the mechanism behind this is unknown. Calcium glycerophosphate reduces the decrease in plaque pH produced by sucrose solutions. This may be due to the buffering action of donated phosphate which acts as an acceptor to three hydrogen ions to form biphosphate, dihydrogen phosphate, and finally phosphoric acid. As bisphosphate and dihydrogen phosphate are amphoteric, these molecules can act as buffers against both acids and bases. Studies on plaque-modification by calcium glycerophosphate have been inconsistent. Redections in plaque weight and plaque area have been noted in separate studies but neither has been confirmed and no causative link has been established in regards to calcium glycerophosphate's anti-caries effect. Calcium glycerophosphate donates [DB01373] and inorganic phosphate resulting in elevated levels of the ions in plaque. These ions are important components of the mineral structure of teeth. As such, their presence supports maintenance of healthy tooth structure and mineralization. In electrolyte replacement calcium glycerophosphate again acts as a donor of [DB01373] and phosphate. See [DB11348] for pharmacological descriptions of calcium and phosphate.

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Pharmacodynamics
It is thought that calcium glycerophosphate may act through a variety of mechanisms to produce an anti-caries effect. These include increasing acid-resistance of the enamel, increasing enamel mineralization, modifying plaque, acting as a pH-buffer in plaque, and elevating [DB01373] and phosphate levels. When used as an electrolyte replacement, calcium glycerophosphate donates [DB01373] and inorganic phosphate. Calcium glycerophosphate is preferable to calcium phosphate due to its increased solubility. Compared to combination calcium gluconate and potassium phosphate, calcium glycerophosphate produces greater phosphate retention which allows for increased [DB01373] retention and ultimately greater incorporation of the ions into bone structure.

C3H7CAO6P

210.14

209.96

27214-00-2

57-03-4 (Parent);57-03-4 (Parent)

120096

White to off-white solid powder

485.5ºC at 760 mmHg

Decomposes at 170

247.4ºC

2

6

3

11

117

0

IWIRHXNCFWGFJE-UHFFFAOYSA-L

InChI=1S/C3H9O6P.Ca/c4-1-3(5)2-9-10(6,7)8;/h3-5H,1-2H2,(H2,6,7,8);/q;+2/p-2

calcium;2,3-dihydroxypropyl phosphate

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O: < 0.1 mg/mL
DMSO: < 1 mg/mL

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)