在培养基中，menaquinone-7（0.01-10 μM；7 天）可抑制破骨细胞样细胞 [1]。在存在植物雌激素金雀异黄酮 (1, 10 μM) 的情况下，Menaquinone-7 (10 μM) 会显着增加 MC3T3E1 细胞中磷酸化的 Menaquinone-7 (1, 10 μM)，并增强对股骨钙水平的合成代谢作用 [3]。

Menaquinone-7（18.1 mg/100 g 饮食；在动物饲料中；24 天）可阻止脱色骨质流失 [5]。

细胞活力测定 [1]
细胞类型：骨髓细胞（来自 3 周大的雄性 Wistar 大鼠；经 PTH/PGE2 刺激）
测试浓度： 0.01-10 µM
孵育时间： 7 天
实验结果： PTH 或 PGE2 刺激的 TRACP 阳性 MNC 数量显着。显着降低前列腺素 E2。

Animal/Disease Models: Female Wistar rat (5 weeks old; ovariectomized (OVX) rat model)) [5].
Doses: 18.1 mg/100 g Dietary
Route of Administration: animal feed; 24-day
Experimental Results: Preventive effect on bone loss caused by OVX.

Absorption, Distribution and Excretion
Vitamin K, mainly in the form of vitamin K1, is principally absorbed from the jejunum and ileum. ... Vitamin K is delivered to the enterocytes in micelles formed from bile salts and other substances. Vitamin K is secreted by enterocytes into the lymphatics in the form of chylomicrons. It enters the circulation via the thoracic duct and is carried in the circulation to various tissues including hepatic, bone and spleen, in the form of chylomicron remnants. In the liver, some vitamin K is stored, some is oxidized to inactive end products and some is secreted with VLDL (very low density lipoprotein). Approximately 50% of vitamin K is carried in the plasma in the form of VLDL, about 25% in LDL (low-density lopoprotein) and about 25% in HDL (high-density lipoprotein). /Vitamin K/
Excretion of vitamin K and its metabolites is mainly via the feces. Some urinary excretion of vitamin K also occurs. /Vitamin K/
...Menaquinones are adequately absorbed from the GI tract only if bile salts are present. Menaquinones and its water-soluble derivatives, however, are absorbed even in the absence of bile. ... Menaquinones are absorbed almost entirely by way of the lymph. /Menaquinones/
Menaquinone forms of vitamin K are produced by bacteria in the lower bowel, where the forms appear in large amounts. However, their contributuion to the maintenance of vitamin K status has been difficult to assess. Although the content is extremely variable, the human liver contains about 10 times as much vitamin K as a mixture of menaquinones than as phylloquinone. /Menaquinones/

---

Metabolism / Metabolites
A major pathway of vitamin K metabolism is that which is involved in the reduction and recycling of the epoxide formed by the carboxylase. /Vitamin K/
Vitamin K undergoes some oxidative metabolism. /Vitamin K/

Interactions
... MK-7 induced more complete carboxylation of osteocalcin, and hematologists should be aware that preparations supplying 50 ug/d or more of MK-7 may interfere with oral anticoagulant treatment in a clinically relevant way.
Broad specturm antibiotics may sterilize the bowel and decrease the vitamin K contribution to the body by the intestinal microflora. /Vitamin K/
Cephalosporins containing side chains of N-methylthiotetrazole (cefmenoxime, cefoperazone, cefotetan, cefamandole, latamoxef) or methylthiadiazole (cefazolin) can cause vitamin K deficiency and hypoprothombinemia. These cephalosporins are inhibitors of hepatic vitamin K epoxide reductase. /Vitamin K/
Concomitant intake of cholestyramine and vitamin K may reduce the absorption of vitamin K. /Vitamin K/
For more Interactions (Complete) data for Vitamin K2 (16 total), please visit the HSDB record page.

[1]. Inhibitory effect of menaquinone-7 (vitamin K2) on osteoclast-like cell formation and osteoclastic bone resorption in rat bone tissues in vitro. Mol Cell Biochem. 2001 Dec;228(1-2):39-47.

[2]. Menaquinone-7 regulates gene expression in osteoblastic MC3T3E1 cells. Int J Mol Med. 2007 Feb;19(2):279-84.

[3]. Stimulatory effect of menaquinone-7 on bone formation in elderly female rat femoral tissues in vitro: prevention of bone deterioration with aging. Int J Mol Med. 2002 Dec;10(6):729-33.

[4]. Bicuspid Aortic Valve Stenosis and the Effect of Vitamin K2 on Calcification Using 18F-Sodium Fluoride Positron Emission Tomography/Magnetic Resonance: The BASIK2 Rationale and Trial Design. Nutrients. 2018 Mar 21;10(4):386.

[5]. Yamaguchi M, Taguchi H, Gao YH, Igarashi A, Tsukamoto Y. Effect of vitamin K2 (menaquinone-7) in fermented soybean (natto) on bone loss in ovariectomized rats. J Bone Miner Metab. 1999;17(1):23-9.

Menaquinone-7 is a menaquinone whose side-chain contains seven isoprene units in an all-trans-configutation. It has a role as a Mycoplasma genitalium metabolite, a bone density conservation agent, an Escherichia coli metabolite, a human blood serum metabolite and a cofactor.
Menaquinone 7 is under investigation in clinical trial NCT00402974 (The Effect of Vitamin K Supplementation on Osteocalcin Carboxylation in Healthy Children).
Menaquinone-7 has been reported in Brevibacillus brevis with data available.

---

Mechanism of Action
In vivo and in vitro studies have shown that vitamin K may directly act on bone metabolism. In vitro studies have demonstrated that vitamin K2 inhibits bone resorption by, in part, inhibiting the production of bone resorbing substances such as prostaglandin E2 and interleukin-6. Vitamin K2 has been reported to enhance human osteoblast-induced mineralization in vitro and to inhibit bone loss in steroid-treated rats and ovariectomized rats.
Certain naphthoquinones, in particular the synthetic vitamin K menadione, have been found to have antitumor activity in vitro and in vivo. Vitamin K2 has been found to induce the in vitro differentiation of myeloid leukemic cell lines. The mechanism of the possible anticarcinogenic activity of vitamin K is not well understood. Menadione is an oxidative stress inducer and its possible anticarcinogenic activity may, in part, be explained by induction of apoptotic cell death. One study suggested that the induction of apoptosis by menadione is mediated by the Fas/Fas ligand system. Another study reported that menadione induces cell cycle arrest and cell death by inhibiting Cda 25 phosphatase.
Vitamin K is involved as a cofactor in the posttranslational gamma-carboxylation of glutamic acid residues of certain proteins in the body. These proteins include the vitamin K-dependent coagulation factors II (prothrombin), VII (proconvertin), IX (Christmas factor), X (Stuart factor), protein C, protein S, protein Zv and a growth-arrest-specific factor (Gas6). In contrast to the other vitamin K-dependent proteins in the blood coagulation cascade, protein C and protein X serve anticoagulant roles. The two vitamin K-dependent proteins found in bone are osteocalcin, also known as bone G1a (gamma-carboxyglutamate) protein or BGP, and the matrix G1a protein or MGP. Gamma-carboxylation is catalyzed by the vitamin K-dependent gamma-carboxylases. /Vitamin K/
The primary gene product of the vitamin K-dependent proteins contains a very homologous domain between the amino terminus of the mature protein and the signal sequence that targets the polypeptide for the secretory pathway. This "propeptide" region appears to be both a "docking" or "recognition " site for the enzyme and a modulator of the activity of the enzyme by decreasing the apparent Km of the Glu site substrate. ... A key finding essential to a complete understanding of the detailed mechanism of action of this enzyme has been the identification of an intermediate chemical form of vitamin K, which could be sufficiently basic to abstract the gamma-hydrogen of the glutamyl residue. It has been proposed that the initial attack of O(2) at the naphthoquinone carbonyl carbon adjacent to the methyl group results in the formation of a dioxetane ring, which generates an alkoxide intermediate. /Vitamin K/
For more Mechanism of Action (Complete) data for Vitamin K2 (8 total), please visit the HSDB record page.

---

Therapeutic Uses
There is no typical dosage for vitamin K. Some multivitamin preparations contain vitamin K as vitamin K1 (phylloquinone or phytonadione) or vitamin K2 (menaquinones) at doses of 25 to 100 ug.
Vitamin K is used to treat anticoagulant-induced prothrombin deficiency caused by warfarin, hyporprothrombinemia secondary to antibiotic therapy and hypoprothrombinemia secondary to vitamin C deficiency from various causes, including malabsorption syndromes. /Vitamin K/
Because hemorrhagic disease of the newborn can be effectively prevented by administrating vitamin K, infants born in the US and Canada routinely receive 0.5-1 mg pf phylloquinone intramuscularly or 2.0 mg orally within 6 hours of birth. This practice is supported by both US and Canadian pediatric societies. /Phylloquinone/
The current recommendations of the American Academy of Pediatrics advise that "vitamin K (phylloquinone) should be given to all newborns as a single, intramuscular dose of 0.5-1 mg" and if this advice is followed, the disease /Vitamin K deficiency bleeding/ is effectively prevented. /Vitamin K/
For more Therapeutic Uses (Complete) data for Vitamin K2 (8 total), please visit the HSDB record page.

---

Drug Warnings
... MK-7 induced more complete carboxylation of osteocalcin, and hematologists should be aware that preparations supplying 50 ug/d or more of MK-7 may interfere with oral anticoagulant treatment in a clinically relevant way.
It has been suggested that vitamin K may have roles in osteoporosis and vascular health. However, this is difficult to establish on the basis of the studies performed thus far. /Vitamin K/
Pregnant women and nursing mothers should avoid supplemental intakes of vitamin K greater than RDA amounts (65 ug daily) unless higher amounts are prescribed by their physicians. /Vitamin K/
Individuals on chronic warfarin therapy may require dietary counseling on how to maintain steady vitamin K intake levels. Because habitual vitamin K intake may modulate warfarin dosage in patients using this anticoagulant, these individuals should maintain their normal dietary and supplementation patterns once an effective dose of warfarin has been established. /Vitamin K/
For more Drug Warnings (Complete) data for Vitamin K2 (6 total), please visit the HSDB record page.

C46H64O2

649.00

648.49

2124-57-4

Menaquinone-7-13C6;Menaquinone-7-d7;1233937-31-9

5287554

Light yellow to yellow solid powder

0.961

720.1±60.0 °C at 760 mmHg

54ºC

254.9±29.9 °C

0.0±2.3 mmHg at 25°C

1.532

17.05

34.14

0

2

20

48

1310

0

CC1=C(C(=O)C2=CC=CC=C2C1=O)C/C=C(\C)/CC/C=C(\C)/CC/C=C(\C)/CC/C=C(\C)/CC/C=C(\C)/CC/C=C(\C)/CCC=C(C)C

RAKQPZMEYJZGPI-LJWNYQGCSA-N

InChI=1S/C46H64O2/c1-34(2)18-12-19-35(3)20-13-21-36(4)22-14-23-37(5)24-15-25-38(6)26-16-27-39(7)28-17-29-40(8)32-33-42-41(9)45(47)43-30-10-11-31-44(43)46(42)48/h10-11,18,20,22,24,26,28,30-32H,12-17,19,21,23,25,27,29,33H2,1-9H3/b35-20+,36-22+,37-24+,38-26+,39-28+,40-32+

2-[(2E,6E,10E,14E,18E,22E)-3,7,11,15,19,23,27-heptamethyloctacosa-2,6,10,14,18,22,26-heptaenyl]-3-methylnaphthalene-1,4-dione

Vitamin K2-7; Vitamin K2(35); Vitamin MK-7

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)

DMSO : ~5 mg/mL (~7.70 mM)

配方 1 中的溶解度: 0.54 mg/mL (0.83 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 悬浮液；超声助溶。
例如，若需制备1 mL的工作液，可将100 μL 5.4 mg/mL澄清DMSO储备液加入400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

---

配方 2 中的溶解度: ≥ 0.54 mg/mL (0.83 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 5.4 mg/mL澄清DMSO储备液加入900 μL玉米油中，混合均匀。

---

请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。