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| Other Sizes |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Human studies demonstrate that calcium from calcium L-threonate is absorbed. In an open-label, single- and multiple-dose study of healthy adult Chinese subjects receiving a single oral dose of 2025 mg calcium theronate, the peak plasma concentration (Cmax) was 32.3 mg/L. The time to reach peak plasma concentration (Tmax) was approximately 2 hours. The presence of threonic acid in human urine has been identified. In a pharmacokinetic study of rats receiving 200 mg/kg bw of calcium threonate orally, approximately 30% of the calcium was excreted in the urine, around 40% was eliminated in the faeces, and about 10 -20% remained in the blood and bone, and about 10% was stored in organs after 24 hours of administration. The apparent total volume of distribution following a single oral dose of 2025 mg calcium theronate in healthy adult Chinese subjects was approximately 53.6 L. Apparent total clearance following a single oral dose of 2025 mg calcium theronate in healthy adult Chinese subjects was approximately 14.5 L/h. Biological Half-Life The terminal-phase elimination half-life following a single oral dose of 2025 mg calcium theronate in healthy adult Chinese subjects was approximately 2.7 hours. |
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| References |
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| Additional Infomation |
L-Threonic acid Calcium Salt is a L-alpha-D-Hepp-(1->7)-L-alpha-D-Hepp-(1->3)-L-alpha-D-Hepp-(1->5)-alpha-Kdo.
Calcium threonate is a calcium salt of threnoic acid and a novel drug developed for the treatment of osteoporosis and as a calcium supplement. It is found in dietary supplements as a source of L-threonate used in the treatment of calcium deficiency and prevention of osteoporosis. The most common form is calcium L-threonate, or (2R,3S)-2,3,4-trihydroxy butyric acid calcium. L-threonate is an active metabolite of vitamin C that mediates a stimulatory action on vitamin C uptake. Therapeutic efficacy of calcium threonate in reducing was studied and investigated due to the hypothesis that it may play a role in the mineralization process through its positive action on vitamin C. Drug Indication No approved therapeutic indications. Mechanism of Action Once dissociated to calcium and L-theronic acid, L-threonic acid exhibits significant stimulatory action on vitamin C uptake and prolongs the retention of vitamin C in human T-lymphoma cells. Vitamin C is a marker for osteoblast formation and has been shown to stimulate procollagen and enhance collagen synthesis. Via stimulation of vitamin C uptake, L-threonic acid acts as a metabolite that influences the mineralization process. |
| Molecular Formula |
C16H28CAO20
|
|---|---|
| Molecular Weight |
580.4595
|
| Exact Mass |
328.031
|
| CAS # |
70753-61-6
|
| PubChem CID |
13388558
|
| Appearance |
White to off-white solid powder
|
| Boiling Point |
518.9ºC at 760 mmHg
|
| Melting Point |
>300 °C(lit.)
|
| Flash Point |
281.7ºC
|
| Index of Refraction |
15 ° (C=1, H2O)
|
| Hydrogen Bond Donor Count |
6
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
19
|
| Complexity |
95.6
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
C([C@@H]([C@H](C(=O)[O-])O)O)O.C([C@@H]([C@H](C(=O)[O-])O)O)O.[Ca+2]
|
| InChi Key |
ZJXGOFZGZFVRHK-BALCVSAKSA-L
|
| InChi Code |
InChI=1S/2C4H8O5.Ca/c2*5-1-2(6)3(7)4(8)9;/h2*2-3,5-7H,1H2,(H,8,9);/q;;+2/p-2/t2*2-,3+;/m00./s1
|
| Chemical Name |
calcium;(2R,3S)-2,3,4-trihydroxybutanoate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
H2O : ~5 mg/mL (~16.01 mM)
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|---|---|
| Solubility (In Vivo) |
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.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] Oral Formulations
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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7228 mL | 8.6139 mL | 17.2277 mL | |
| 5 mM | 0.3446 mL | 1.7228 mL | 3.4455 mL | |
| 10 mM | 0.1723 mL | 0.8614 mL | 1.7228 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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