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| 1mg |
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| Other Sizes |
| Targets |
Cav3.2 voltage-gated calcium channels (T-type calcium channels) in addition to various reactive oxygen species (ROS). L-Ascorbic acid (vitamin C) is an endogenous antioxidant and essential cofactor. It has been shown to selectively inhibit Cav3.2 channels with an IC50 of 6.5 microM. It also acts as an electron donor, scavenging free radicals and protecting cells from oxidative damage. The 13C6-labeled version has identical biological properties but is used as an analytical standard.
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| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as tracers that influence measurement during the drug development process. It's possible that the pharmacokinetics and functional range of medications contribute to the concern over mutagenesis [1].
In vitro, L-ascorbic acid (vitamin C) demonstrates multiple biological activities. It selectively inhibits Cav3.2 T-type calcium channels with an IC50 of 6.5 microM. As an electron donor, it is a potent endogenous antioxidant, scavenging reactive oxygen and nitrogen species. It serves as an essential cofactor for various hydroxylation enzymes, including prolyl hydroxylase (required for collagen synthesis) and dopamine beta-hydroxylase. It also enhances iron absorption and supports immune cell function. The 13C6-labeled version has identical activity but is used as an internal standard. |
| ln Vivo |
In vivo, L-ascorbic acid is an essential nutrient for humans, who cannot synthesize it due to the lack of L-gulonolactone oxidase. It is required for collagen synthesis, wound healing, bone formation, and maintenance of cartilage, teeth, and gums. Severe deficiency leads to scurvy, characterized by bleeding gums, easy bruising, and poor wound healing. Vitamin C also enhances immune function, promotes iron absorption from plant sources, and reduces the risk of chronic diseases by acting as an antioxidant. The 13C6-labeled version is used as an analytical standard.
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| Enzyme Assay |
A standard in vitro biochemical assay for ascorbic acid is an antioxidant (radical scavenging) assay, such as the DPPH (2,2-diphenyl-1-picrylhydrazyl) or ABTS (2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)) assay. The test compound (ascorbic acid or its labeled analog) at varying concentrations is incubated with the stable radical DPPH or ABTS•+. The decrease in absorbance at 515 nm (DPPH) or 734 nm (ABTS) is measured spectrophotometrically to determine the half-maximal scavenging concentration (SC50) or Trolox equivalent antioxidant capacity (TEAC).
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| Cell Assay |
In vitro cellular assays for L-ascorbic acid include cell viability and oxidative stress assays. For example, cells (e.g., human fibroblasts or neuronal cell lines) are treated with varying concentrations of ascorbic acid (or the 13C6-labeled analog) for 24-72 hours, followed by an MTT or resazurin assay to assess cytotoxicity and cytoprotection. Oxidative stress models involve pre-treating cells with ascorbic acid, then exposing them to hydrogen peroxide or other oxidants, and measuring cell death or reactive oxygen species (ROS) levels using fluorescent dyes such as DCFH-DA.
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| Animal Protocol |
In vivo animal studies for L-ascorbic acid are often conducted in guinea pigs or mice lacking gulonolactone oxidase. Animals are placed on a vitamin C-deficient diet to induce scurvy-like symptoms (weight loss, reduced collagen synthesis, impaired wound healing). The test compound (ascorbic acid or its labeled analog) is then administered at varying doses via oral gavage or in drinking water. Endpoints include body weight, tissue ascorbate levels (measured by LC-MS/MS using the 13C6-labeled internal standard), collagen content, and survival.
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| ADME/Pharmacokinetics |
L-Ascorbic acid (vitamin C) has a short half-life and rapid renal clearance at high doses. Oral bioavailability is dose-dependent, with absorption decreasing as dose increases (>200 mg). The compound is primarily excreted unchanged in urine at high doses; at lower doses, it is metabolized to oxalate and other metabolites. The 13C6-labeled version has identical pharmacokinetics. The unlabeled compound is widely available as an over-the-counter dietary supplement and is administered orally or intravenously for various indications.
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| Toxicity/Toxicokinetics |
L-Ascorbic acid (vitamin C) is generally recognized as safe (GRAS) with very low toxicity. The tolerable upper intake level in adults is 2,000 mg/day. Adverse effects at high doses include gastrointestinal disturbances (diarrhea, nausea, abdominal cramps) due to osmotic effects. In individuals with predisposing conditions, high doses can increase the risk of kidney stones (calcium oxalate). The 13C6-labeled version has an identical safety profile. Standard laboratory safety precautions should be followed when handling the labeled material.
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| References |
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-246.
[2]. Sebastian J Padayatty, et al. Vitamin C as an antioxidant: evaluation of its role in disease prevention. J Am Coll Nutr. 2003 Feb;22(1):18-35. [3]. Sungrae Cho, et al. Hormetic dose response to L-ascorbic acid as an anti-cancer drug in colorectal cancer cell lines according to SVCT-2 expression. Sci Rep. 2018 Jul 27;8(1):11372. [4]. Satyanarayana Sreemantula, et al. Influence of antioxidant (L- ascorbic acid) on tolbutamide induced hypoglycaemia/antihyperglycaemia in normal and diabetic rats. BMC Endocr Disord. 2005 Mar 3;5(1):2. [5]. Michael T Nelson, et al. Molecular mechanisms of subtype-specific inhibition of neuronal T-type calcium channels by ascorbate. J Neurosci. 2007 Nov 14;27(46):12577-83. [6]. Aleksander Hinek, et al. Sodium L-ascorbate enhances elastic fibers deposition by fibroblasts from normal and pathologic human skin. J Dermatol Sci. 2014 Sep;75(3):173-82. |
| Additional Infomation |
L-Ascorbic acid-13C6-1 is a stable isotope-labeled internal standard for LC-MS/MS quantification of vitamin C in biological matrices such as plasma, serum, urine, and tissue homogenates. It is also used in metabolic tracer studies to track ascorbate absorption, distribution, metabolism, and excretion (ADME). The unlabeled L-ascorbic acid (vitamin C) is an essential nutrient, a potent antioxidant, and is used therapeutically to treat and prevent vitamin C deficiency (scurvy). It is also investigated as an adjunctive therapy in cancer, sepsis, and viral infections. The 13C6-labeled version is strictly an analytical standard for research use.
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| Molecular Formula |
13C6H8O6
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|---|---|
| Molecular Weight |
182.08
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| Exact Mass |
182.052
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| CAS # |
1331939-77-5
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| Related CAS # |
L-Ascorbic acid;50-81-7
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| PubChem CID |
57369508
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| Appearance |
White to off-white solid powder
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| Melting Point |
187-189°C
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| LogP |
-1.6
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
12
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| Complexity |
232
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O[13CH2][13CH]([13C@H]1O[13C](=O)[13C](O)=[13C]1O)O
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| InChi Key |
CIWBSHSKHKDKBQ-HFEVONBRSA-N
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| InChi Code |
InChI=1S/C6H8O6/c7-1-2(8)5-3(9)4(10)6(11)12-5/h2,5,7-10H,1H2/t2?,5-/m1/s1/i1+1,2+1,3+1,4+1,5+1,6+1
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| Chemical Name |
(2R)-2-(1,2-dihydroxy(1,2-13C2)ethyl)-3,4-dihydroxy-(2,3,4,5-13C4)2H-furan-5-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 5.4921 mL | 27.4605 mL | 54.9209 mL | |
| 5 mM | 1.0984 mL | 5.4921 mL | 10.9842 mL | |
| 10 mM | 0.5492 mL | 2.7460 mL | 5.4921 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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