| CAS: | 51037-30-0 |
| MF: | C6H6N2O3 |
| MW: | 154.12 |
| EINECS: | 256-928-3 |
| Product Categories: | OLBEMOX;Pharmaceuticals;Pyrazine;Heterocycles;Intermediates & Fine Chemicals |
| Mol File: | 51037-30-0.mol |
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| Acipimox Chemical Properties |
| Melting point | 177-180 °C |
| Boiling point | 539.0±45.0 °C(Predicted) |
| density | 1.44±0.1 g/cm3(Predicted) |
| storage temp. | Inert atmosphere,2-8°C |
| solubility | Soluble in methanol, water (100 mM), DMSO (100 mM), ethanol (<1 mg/ml at 25° C), and 1 M NH4OH (1 mg/ml). |
| form | Solid |
| pka | 2.80±0.10(Predicted) |
| color | Yellow |
| Merck | 14,111 |
| InChIKey | DJQOOSBJCLSSEY-UHFFFAOYSA-N |
| CAS DataBase Reference | 51037-30-0(CAS DataBase Reference) |
| EPA Substance Registry System | Pyrazinecarboxylic acid, 5-methyl-, 4-oxide (51037-30-0) |
| Acipimox Usage And Synthesis |
| Description | Acipimox is a nicotinic acid derivate that structurally related to nicotinic acid. Like nicotinic acid, lowers lipids effectively, but unlike nicotinic acid, acipimox is longer acting and therefore much less prone to produce free fatty acid rebounding. It is usually employed in man in the therapy of hypertriglyceridemia. In addition to its lipid lowering activity, it produces a beneficial elevation of the anti-atherogenic high density lipoprotein subfraction, HDL2. Acipimox is recommended as a lipid-lowering agent to treat hyperlipidemia in patients with noninsulin dependent diabetes mellitus. |
| Chemical Properties | Yellow Solid |
| Originator | Erbamont (Italy) |
| Characteristics | The advantages of acipimox to niacin are as follows:
Longer duration of inhibition of hormone-sensitive lipase than niacin.
A lower dose (250 mg BD or TDS) of acipimox is required to lower lipid levels and better tolerability with fewer side effects than niacin.
Acipimox increases insulin sensitivity, while niacin causes insulin resistance. Thus, acipimox has a favorable role in patients with dyslipidemia and diabetes, whereas niacin is contraindicated in diabetes.
Acipimox has adjuvant role in the management of PCOD and increases tissuesensitivity to GH, whereas niacin does not. |
| Uses | Acipimox is a long-acting antilipemic agent and used for the treatment of hyperlipoproteinemias, in particular hypertriglyceridemias, and as adjunctive therapy for affecting cholesterol metabolism. |
| Definition | ChEBI: 5-methyl-4-oxido-2-pyrazin-4-iumcarboxylic acid is a pyrazinecarboxylic acid. |
| Preparation | Synthesis of acipimox: Under cooling and stirring, 78 g of maleic anhydride was dissolved in a solution of 60 ml of chloroform, and 40 ml of 30% hydrogen peroxide was added. After 2 h, 4.8 g of 5-Methyl-2-pyrazinecarboxylic acid was added, and the temperature was kept at 0-5 °C for 2 d. The maleic acid was filtered off. Concentrate to a small volume, add ethyl acetate, and filter to obtain 1.1 g of acipimox, the melting point of which is 178-180 °C. |
| Brand name | OLBETAM |
| benefits | 1. Act on the liver and adipose tissue, inhibit the lipolysis of adipose tissue, thereby reducing plasma total cholesterol, triglyceride, low-density lipoprotein, and very low-density lipoprotein.
2. Increase high-density lipoprotein in plasma, which is beneficial to the transport and clearance of cholesterol.
3. Increase liver glycogen synthesis and lower blood sugar levels. Asimimox can be used as the first-choice lipid-lowering drug for the treatment of various hyperlipidemias, especially for those with diabetes mellitus with hyperlipidemia. |
| Biological Activity | Acipimox, also known as olbemox, is a nicotinic acid analog. It functions as an anti-lipolytic drug and vasodilator. Acipimox may be used in various metabolic studies involving insulin and ghrelin. It lowers total cholesterol and total triglycerides, which helps in the treatment of hyperlipidemia. |
| Clinical Use | Acipimox was introduced in Europe to treat hyperlipidemia in 1985. Acipimox is a weak agonist of GPR109A with micromolar binding and functional activity.Like niacin, acipimox raises HDL-C and triggers vasodilation in humans.However, it remains unclear whether acipimox causes mild hyperglycemia as is observed with niacin. |
Packing &shipping&Payment
Packing:25kg/drum
Shipping:by sea or by air
Payment:T/T,western union,moneygram
Packaging Details drum
Port:Tianjin
Lead Time :
| Quantity(Kilograms) | 1 - 10000 | >10000 |
| Est. Time(days) | 5 | To be negotiated |
Company information
Hebei Mojin Biotechnology Co., Ltd, Our company is a professional in 4'-Methylacetophenone,Levamisole hydrochloride ,N-Methylformamide and other chemical reagents research and development production enterprises. Our business covers more than 30 countries, most of the big customers come from Europe, America and other countries in the world, we can guarantee the quality and price. In recent decades, with the efforts of all employees, we have established many cooperative companies in shandong, henan, guangdong and other places. Our corporate purpose is based on the market, enhance the strength, take the road of scientific and environmental sustainable development, relying on the country. Technology r & d center, increase the investment in r & d, based on the domestic market, expand the international market, manufacturing quality products, sincere service to the society, into a modern, ecological, scientific and technological enterprise world.
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