| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Vitamin K2 acts as a cofactor for the enzyme gamma-glutamyl carboxylase, which catalyzes the carboxylation of glutamic acid residues on vitamin K-dependent proteins. Its primary targets include coagulation factors II (prothrombin), VII, IX, and X in the liver, where it regulates blood coagulation. Additionally, vitamin K2 targets osteocalcin and matrix Gla protein (MGP), which are involved in bone mineralization and vascular health respectively. It also modulates signaling of certain tyrosine kinases, affecting transcription factors including c-myc and c-fos.
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| ln Vitro |
Vitamin K2 exhibits various in vitro activities including the inhibition of tumor cell growth by inducing apoptosis and cell cycle arrest. It acts as an antioxidant and anti-inflammatory agent in cellular systems. In vitro studies have shown that vitamin K2 can modulate cellular signaling pathways, affecting the expression of genes involved in cell proliferation and differentiation. It also demonstrates neuroprotective properties in neuronal cell culture models. The compound's ability to activate vitamin K-dependent proteins through carboxylation is its primary mechanism of action in vitro.
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| ln Vivo |
In vivo, Vitamin K2 promotes the synthesis of prothrombin in the liver and regulates the synthesis of coagulation factors VII, IX, and X, thereby accelerating blood coagulation. Studies have shown that Vitamin K2 supplementation helps maintain normal blood clotting, promotes wound healing, and reduces the risk of bleeding disorders. It also plays an important role in bone density conservation, preventing osteoporosis by activating osteocalcin. Additionally, Vitamin K2 exhibits antioxidant, anti-inflammatory, and neuroprotective effects in various animal models. Clinical trials have studied its use in diabetes, osteoporosis, prediabetic states, and hepatocellular carcinoma.
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| Enzyme Assay |
In vitro enzyme assays for Vitamin K2 typically measure its cofactor activity for gamma-glutamyl carboxylase. The assay involves incubating the enzyme with Vitamin K2 hydroquinone (the reduced form), CO2, and a peptide substrate containing glutamic acid residues. The carboxylation reaction is monitored by the incorporation of radioactive CO2 (14CO2) or by mass spectrometry detection of the carboxylated product. The reaction is performed in buffer containing dithiothreitol (DTT) and phosphatidylcholine at 25°C, and the enzyme activity is quantified by measuring the amount of gamma-carboxyglutamate (Gla) formed. Vitamin K epoxide reductase activity can also be assessed in parallel.
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| Cell Assay |
Cellular assays for Vitamin K2 involve culturing various cell lines including osteoblasts (e.g., MC3T3-E1), vascular smooth muscle cells, and cancer cell lines. Cells are treated with Vitamin K2 at concentrations ranging from 1-100 µM for 24-72 hours. Endpoints include assessment of cell proliferation (MTT assay), apoptosis (Annexin V staining, caspase activity), osteocalcin carboxylation (ELISA), and mineralization (Alizarin Red staining). Gene expression analysis by qPCR is used to measure markers such as osteocalcin, MGP, and cell cycle regulators. For cancer studies, cell cycle analysis by flow cytometry and assessment of tyrosine kinase signaling pathways are commonly performed.
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| Animal Protocol |
In vivo animal studies for Vitamin K2 typically use rodent models. For osteoporosis studies, ovariectomized (OVX) rats or mice are administered Vitamin K2 via oral gavage at doses of 10-50 mg/kg/day for 4-12 weeks. Bone mineral density is measured by DEXA scan, and bone turnover markers (e.g., osteocalcin, P1NP, NTX) are assessed in serum. For cancer studies, xenograft models are used, with tumor growth monitored and apoptosis markers evaluated. Coagulation studies involve measuring prothrombin time (PT) and activated partial thromboplastin time (aPTT) in plasma. For vascular calcification studies, mice fed high-fat diets are treated with Vitamin K2 and arterial calcification is assessed histologically.
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| ADME/Pharmacokinetics |
Vitamin K2 is absorbed from the gastrointestinal tract in the presence of dietary fats and bile salts. It is transported in chylomicrons and distributed to tissues, with the highest concentrations found in the liver, bone, and pancreas. The plasma half-life of Vitamin K2 is relatively short (approximately 1-2 hours), but tissue retention is longer. It is metabolized in the liver via side-chain shortening and conjugation, and excreted primarily in bile and urine. The compound is heat-resistant but sensitive to light. Pharmacokinetic studies typically measure plasma menaquinone-4 levels using HPLC or LC-MS/MS following oral administration.
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| Toxicity/Toxicokinetics |
Vitamin K2 has a very low toxicity profile. No known toxic effects have been reported with high doses, and it is considered safe even at levels much higher than the recommended dietary intake. The acceptable daily intake is not established due to its wide safety margin. Vitamin K2 can antagonize the effects of warfarin and other coumarin anticoagulants, which is a clinically significant drug interaction, as it promotes blood coagulation by increasing the synthesis of vitamin K-dependent clotting factors. Allergic reactions are rare. It is generally recognized as safe for use as a nutritional supplement.
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| Additional Infomation |
Menadione-4 is a menadione compound with four all-trans isoprene units in its side chain. It plays a role in maintaining bone density, acting as a metabolite, an antioxidant, an anti-inflammatory agent, and a neuroprotective agent. Menadione-4 has been used in clinical trials for the treatment of diabetes, osteoporosis, prediabetes, and hepatocellular carcinoma. Menadione-4 is a menadione compound and a form of vitamin K2, possessing potential antitumor activity. Menadione-4 may exert its effects by modulating the signaling of certain tyrosine kinases, thereby affecting multiple transcription factors, including c-myc and c-fos. This drug inhibits tumor cell growth by inducing apoptosis and cell cycle arrest.
Vitamin K2 (menatetrenone) is a form of vitamin K with important physiological roles in blood coagulation, bone metabolism, and cardiovascular health. It has been used clinically in Japan for the treatment of osteoporosis and is available as a dietary supplement worldwide. Clinical trials have explored its use in diabetes, prediabetic states, and hepatocellular carcinoma. It exhibits antineoplastic activity by modulating tyrosine kinase signaling and affecting transcription factors c-myc and c-fos. The compound is considered an endogenous metabolite and serves as both a nutrient and a pharmacological agent. |
| Molecular Formula |
C20H28O
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|---|---|
| Molecular Weight |
284.44
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| Exact Mass |
444.302
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| CAS # |
11032-49-8
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| Related CAS # |
Menaquinone-4;863-61-6
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| PubChem CID |
5282367
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.0±0.1 g/cm3
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| Boiling Point |
570.6±50.0 °C at 760 mmHg
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| Melting Point |
54 °C
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| Flash Point |
208.3±27.1 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.539
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| LogP |
10.94
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
33
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| Complexity |
855
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(C(=O)C2=CC=CC=C2C1=O)C/C=C(\C)/CC/C=C(\C)/CC/C=C(\C)/CCC=C(C)C
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| InChi Key |
DKHGMERMDICWDU-GHDNBGIDSA-N
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| InChi Code |
InChI=1S/C31H40O2/c1-22(2)12-9-13-23(3)14-10-15-24(4)16-11-17-25(5)20-21-27-26(6)30(32)28-18-7-8-19-29(28)31(27)33/h7-8,12,14,16,18-20H,9-11,13,15,17,21H2,1-6H3/b23-14+,24-16+,25-20+
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| Chemical Name |
2-methyl-3-[(2E,6E,10E)-3,7,11,15-tetramethylhexadeca-2,6,10,14-tetraenyl]naphthalene-1,4-dione
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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) |
DMSO: 50 mg/mL (175.78 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (8.79 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (8.79 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5157 mL | 17.5784 mL | 35.1568 mL | |
| 5 mM | 0.7031 mL | 3.5157 mL | 7.0314 mL | |
| 10 mM | 0.3516 mL | 1.7578 mL | 3.5157 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.
Link: https://clinicaltrials.gov/ct2/show/NCT06817512
Conditions:Ischemic StrokeLink: https://clinicaltrials.gov/ct2/show/NCT05500443
Conditions:Coronary Artery DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT05547750
Conditions:Nocturnal Leg Cramps
Title:Pilot Study of Vitamin K2 (MK-7) and Vitamin D3 Supplementation and the Effects on PASC Symptomatology and Inflammatory Biomarkers
Status:Completed
updateDate:2024-09-27
Ctid:NCT05356936
Link: https://clinicaltrials.gov/ct2/show/NCT05356936
Conditions:Post-acute COVID-19 SyndromeLink: https://clinicaltrials.gov/ct2/show/NCT05995522
Conditions:Overweight and Obesity|Cardiometabolic Risk FactorsLink: https://clinicaltrials.gov/ct2/show/NCT04676958
Conditions:Inflammation|Oxidative Stress|Vitamin K|Exercise|Strength|RecoveryLink: https://clinicaltrials.gov/ct2/show/NCT05375630
Conditions:Diabete Type 2Link: https://clinicaltrials.gov/ct2/show/NCT05675163
Conditions:Oxidative Stress|InflammationLink: https://clinicaltrials.gov/ct2/show/NCT05161975
Conditions:Muscle Atrophy|CachexiaLink: https://clinicaltrials.gov/ct2/show/NCT04429035
Conditions:Aortic Valve Stenosis|Aortic Valve Calcification|Mitral Annular Calcification|Mitral Valve Calcification|Mitral Valve StenosisLink: https://clinicaltrials.gov/ct2/show/NCT04477811
Conditions:End Stage Renal Disease on DialysisLink: https://clinicaltrials.gov/ct2/show/NCT03897660
Conditions:HealthyLink: https://clinicaltrials.gov/ct2/show/NCT02976246
Conditions:Vitamin K Supplementation|Endstage Renal Disease|Cardiovascular Disease|Bone DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT04382027
Conditions:HealthyLink: https://clinicaltrials.gov/ct2/show/NCT01232647
Conditions:Post-menopausal OsteoporosisLink: https://clinicaltrials.gov/ct2/show/NCT03311321
Conditions:Cardiovascular Diseases|Chronic Kidney Disease Stage 3|Chronic Kidney Disease Stage 4|Chronic Kidney Disease Stage 5|Vitamin K Deficiency|HemodialysisLink: https://clinicaltrials.gov/ct2/show/NCT02959762
Conditions:Obesity|Insulin Resistance|Obesity in Diabetes|Nutritional and Metabolic Diseases|Hyperlipidemia|Hyperglycemia|Cardiovascular DiseasesLink: https://clinicaltrials.gov/ct2/show/NCT01972113
Conditions:Obesity|Insulin Resistance|Insulin Sensitivity|Prediabetes|Dyslipidemia|DiabetesLink: https://clinicaltrials.gov/ct2/show/NCT04145492
Conditions:End Stage Renal DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT02610933
Conditions:Vascular CalcificationLink: https://clinicaltrials.gov/ct2/show/NCT00548509
Conditions:OsteoporosisLink: https://clinicaltrials.gov/ct2/show/NCT02917525
Conditions:Aortic Valve Stenosis|Bicuspid Aortic ValveLink: https://clinicaltrials.gov/ct2/show/NCT02517580
Conditions:Arterial Stiffness|Vitamin K2 DeficiencyLink: https://clinicaltrials.gov/ct2/show/NCT00062595
Conditions:OsteoporosisLink: https://clinicaltrials.gov/ct2/show/NCT00165698
Conditions:Postmenopausal OsteoporosisLink: https://clinicaltrials.gov/ct2/show/NCT01923012
Conditions:Carotid Disease|AtherosclerosisLink: https://clinicaltrials.gov/ct2/show/NCT01533441
Conditions:ThrombosisLink: https://clinicaltrials.gov/ct2/show/NCT01638182
Conditions:Bone Health|Vascular HealthLink: https://clinicaltrials.gov/ct2/show/NCT00960973
Conditions:Diabetes|Prediabetic StateLink: https://clinicaltrials.gov/ct2/show/NCT01194778
Conditions:Carboxylation Level|Vitamin K-dependent ProteinsLink: https://clinicaltrials.gov/ct2/show/NCT01101698
Conditions:Kidney Diseases|Coronary Artery CalcificationLink: https://clinicaltrials.gov/ct2/show/NCT00165607
Conditions:OsteoporosisLink: https://clinicaltrials.gov/ct2/show/NCT00165633
Conditions:Hepatocellular CarcinomaProducts are for research use only; We do not sell to patients
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