Name | Mecobalamin |
Synonyms | Algobaz Mecobalamin MECOBALAMIN Vitamin B12 MECOBALAMINE Methylcobalamin METHYLCOBALAMIN Methyl Vitamin B12 cobalt-methylcobalamin Methyl-5,6-dimethylbenzimidazolylcobalamin cobinamide,cobalt-methylderivative,hydroxide,dihydrogenphosphate(ester), |
CAS | 13422-55-4 |
EINECS | 236-535-3 |
InChI | InChI=1/C62H90N13O14P.CH3.Co/c1-29-20-39-40(21-30(29)2)75(28-70-39)57-52(84)53(41(27-76)87-57)89-90(85,86)88-31(3)26-69-49(83)18-19-59(8)37(22-46(66)80)56-62(11)61(10,25-48(68)82)36(14-17-45(65)79)51(74-62)33(5)55-60(9,24-47(67)81)34(12-15-43(63)77)38(71-55)23-42-58(6,7)35(13-16-44(64)78)50(72-42)32(4)54(59)73-56;;/h20-21,23,28,31,34-37,41,52-53,56-57,76,84H,12-19,22,24-27H2,1-11H3,(H15,63,64,65,66,67,68,69,71,72,73,74,77,78,79,80,81,82,83,85,86);1H3;/q;-1;+3/p-2/t31?,34-,35-,36-,37+,41+,52?,53?,56?,57+,59-,60+,61+,62+;;/m1../s1 |
InChIKey | JEWJRMKHSMTXPP-WYVZQNDMSA-L |
Molecular Formula | C63H90CoN13O14P |
Molar Mass | 1343.4 |
Melting Point | >190°C (dec.) |
Water Solubility | Partially soluble in cold water, hot water. |
Solubility | DMSO (Slightly), Methanol (Sparingly), Water (Slightly) |
Appearance | Red powder |
Color | Dark Red |
pKa | pK1:7.64(+1) (25°C) |
Storage Condition | Sealed in dry,Store in freezer, under -20°C |
Stability | Light Sensitie |
Sensitive | Sensitive to light |
MDL | MFCD00082483 |
Physical and Chemical Properties | This product is a deep red crystal or crystalline powder, soluble in water, ethanol-soluble, insoluble in acetone, see light unstable |
Use | For the treatment of nervous system diseases, relieve pain and numbness, rapid relief of neuralgia, improve the pain caused by cervical spondylosis, treatment of sudden deafness |
In vitro study | Methylcobalamin (CH3-B12) is a cobalamin, a form of vitamin B12. It differs from cyanocobalamin in that the cyanide is replaced by a methyl group. Methylcobalamin (CH3-B12) features an octahedral cobalt(III) centre. Methylcobalamin (CH3-B12) can be obtained as bright red crystals. From the perspective of coordination chemistry, Methylcobalamin (CH3-B12) is notable as a rare example of a compound that contains metal-alkyl bonds. Methylcobalamin (CH3-B12) is equivalent physiologically to vitamin B12, and can be used to prevent or treat pathology arising from a lack of vitamin B12 (vitamin B12 deficiency), such as pernicious anemia. Methylcobalamin (CH3-B12) is also used in the treatment of peripheral neuropathy, diabetic neuropathy, and as a preliminary treatment for amyotrophic lateral sclerosis. From Wikipedia. |
Hazard Symbols | Xi - Irritant |
Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | S24/25 - Avoid contact with skin and eyes. S36 - Wear suitable protective clothing. S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
WGK Germany | 2 |
RTECS | GG3745000 |
HS Code | 29362600 |
Toxicity | LD50 oral in rat: > 5gm/kg |
This product is Coa-[a-( 5, 6-dimethylbenzolimyl)] -methyloleamide. The content of C63H91CoN13014P shall be between 98.0% and 102.0% calculated as anhydrous.
take this product 20mg, add water 10ml after dissolution, the solution should be clarified (General Principles 0902 The first method).
operation in the dark. Take an appropriate amount of this product, add the mobile phase to dissolve and dilute to make a solution containing about 0.5mg per lml as a test solution; Take lml for precision measurement, put it in a 100ml measuring flask, dilute it to the scale with the mobile phase, as a control solution. According to the chromatographic conditions under the content determination item, 20 u1 of each of the test solution and the control solution are accurately measured and injected into the human liquid chromatograph respectively, and the chromatogram is recorded to 3 times of the retention time of the main component peak. If there are impurity peaks in the chromatogram of the test solution, the area of a single impurity peak shall not be greater than 0.5 times (0.5%) of the area of the main peak of the control solution, the sum of each impurity peak area shall not be greater than 2 times (2.0%) of the main peak area of the control solution.
take this product, according to the moisture determination method (General 0832 first method 1), the water content shall not exceed 12.0%.
operation in the dark. Determined by high performance liquid chromatography (General 0512).
silica gel bonded with octa-alkyl silane was used as a filler (4.6mm X 250mm , 5um or equivalent performance column); the mobile phase was 0.03mol / L potassium dihydrogen phosphate solution (adjusted to pH 0.2 with 4.5 mol / L sodium hydroxide solution or phosphoric acid)-acetonitrile (84:16); The detection wavelength was 342nm. Take about 10mg of mecobalamin reference substance, put it in a 20ml measuring flask, add water to dissolve and dilute to the scale, shake well, place it under natural light for 5-10 minutes, and inject 20u1 into the liquid chromatograph, adjust the flow rate so that the retention time of mecobalamin peak is about 12 minutes, record the chromatogram, the separation degree of mecobalamin peak and hydroxycobalamin peak (relative retention time is about 0.2) should be greater than 20, the degree of separation between the mecobalamin peak and the adjacent impurity peak shall meet the requirements.
take an appropriate amount of this product, accurately weigh it, add the mobile phase to dissolve and quantitatively dilute it to make a solution containing about 50ug per lml, which is used as the test solution, the chromatogram was recorded by injection of 20u1 into human Liquid Chromatograph. Another reference substance of mecobalamin was taken and determined by the same method. According to the external standard method to calculate the peak area, that is.
treatment of peripheral neuropathy drugs.
light shielding, sealed storage.
protection from light is not more than 5lx.
This product contains mecobalamin (C63H91CoN13014P) should be the label amount of 90.0% ~ 110.0%.
The content of this product is white to pink granules or powder.
Same as mecobalamin.
0.5mg
light shielding, sealed storage.
protection from light is not more than 5lx.
Physiological function | Mecobalamin is a therapeutic drug for peripheral neurological disorders. Compared with other vitamin B12 preparations, it has good transmissibility to nerve tissue. It can promote nucleic acid-protein-lipid metabolism and repair damaged nerve tissue through methyl conversion reaction. It plays a coenzyme role in the synthesis of methionine from homocysteine, especially in the synthesis of thymidine from deoxyuridine, and promotes the synthesis of DNA and RNA. In addition, in the experiment of glial cells, this drug increases the activity of methionine synthase and promotes the synthesis of myelin lipid lecithin. Improving the metabolic disorders of nerve tissue can promote the synthesis of axons and their proteins, make the delivery speed of bone proteins close to normal, and maintain the function of axons. mecobalamin injection can also inhibit the abnormal excitation conduction of nerve tissue, promote the maturation and division of red blood mother cells, and improve anemia. Mecobalamin can quickly restore the red blood cell count, hemoglobin and hematocrit values of rats reduced by B12 deficiency. It is applied to megaloblastic anemia and peripheral nerve disorders caused by vitamin B12 deficiency. |
pharmacological action | mecobalamin is a vitamin B12 derivative, named by chemical structure, it should be called "methyl vitamin B12", its methylated functional group can participate in the body's biochemical process Methyl transfer activity has a promoting effect on the metabolism of nucleic acid, protein and fat in nerve tissue, can stimulate the synthesis of lecithin in Schwann cells, repair damaged myelin, improve nerve conduction velocity; it can directly enter nerve cells and stimulate axon damaged areas to regenerate; stimulate the protein synthesis of nerve cells, strengthen axon anabolism, and prevent axon degeneration; participate in nucleic acid synthesis and promote hematopoietic function. Clinically, it is often used in the treatment of diabetic neuropathy, and long-term use also has a certain effect on the macrovascular complications of diabetes. Mecobalamin is mainly used for peripheral nerve diseases caused by diabetes and megaloblastic anemia caused by vitamin B12 deficiency. It is widely used clinically with few side effects. |
preparation | the existing synthesis methods of mecobalamin are two steps of cyanocobalamin reduction and methylation. the actual operation is a one-pot reaction. the common synthesis methods mainly include: the preparation method of mecobalamin by sodium borohydride reduction and methyl iodide methylation using cyanocobalamin as raw material; The preparation method of mecobalamin by sodium borohydride reduction and dimethyl sulfate methylation using cyanocobalamin as raw material; using cyanocobalamin as a raw material to reduce by sodium borohydride and methylate methyl toluenesulfonate to prepare mecobalamin; in the presence of cobalt salt or iron salt, sodium borohydride reduces cyanocobalamin, and then use trimethyl iodide The method of methylation of sulfoxide or trimethyl bromide to prepare mecobalamin; the method of reducing cyanocobalamin with sodium borohydride and methylation of dimethyl carbonate to prepare cyanocobalamin. |
biological activity | Methylcobalamin (Mecobalamin, Vancomin, Methycobal, Cobametin) is one of the active forms of vitamin B12, which can directly participate in homocysteine metabolism. It is used to treat some nutritional diseases and other clinical diseases such as Alzheimer's disease and rheumatoid arthritis. |
use | used to treat neurological diseases, relieve pain and numbness, quickly relieve neuralgia, improve pain caused by cervical spondylosis, and treat sudden deafness. mecobalamin is an endogenous coenzyme B12, which participates in a one-carbon unit cycle and plays an important role in the transmethylation reaction of methionine from homocysteine. |