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ChemicalBook Optimization Suppliers |
| 名前: |
Alfa Aesar |
| 電話番号: |
400-6106006 |
| 電子メール: |
saleschina@alfa-asia.com |
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| 融点 | 102-106 °C (lit.) | | 沸点 | 192-193 °C (lit.) | | 比重(密度) | 1,37 g/cm3 | | 蒸気圧 | 5 hPa (25 °C) | | 屈折率 | 1.4062 (estimate) | | 闪点 | 192-193°C | | 貯蔵温度 | Store below +30°C. | | 溶解性 | 1.6g/l | | 外見 | Liquid | | 色 | Clear colorless to faintly yellow | | PH | 4.0-6.0 (10g/l, H2O, 20℃)suspension | | 水溶解度 | Soluble in water (1.6 mg/ml at 20°C), methanol (30-36 mg/ml), ethanol (10 mg/ml at 25°C), DMSO (29 mg/ml at 25°C), and DMF (~12 mg/ml). | | Merck | 14,4287 | | BRN | 774590 | | 安定性： | Stable. Incompatible with acids, bases, oxidizing agents, reducing agents. | | CAS データベース | 624-49-7(CAS DataBase Reference) | | NISTの化学物質情報 | 2-Butenedioic acid (E)-, dimethyl ester(624-49-7) | | EPAの化学物質情報 | 2-Butenedioic acid (2E)-, 1,4-dimethyl ester (624-49-7) |
| | フマル酸ジメチル Usage And Synthesis |
| 外観 | 白色, 結晶〜結晶性粉末 | | 溶解性 | エタノール及びアセトンに溶け、水にほとんど溶けない。 | | 用途 | 有機合成原料。 | | 効能 | 免疫調節薬 | | 商品名 | テクフィデラ (バイオジェン・ジャパン) | | 説明 | In March 2013, the US FDA approved dimethyl fumarate for the treatment of relapsing forms of multiple sclerosis (MS). Dimethyl fumarate is the newest oral therapeutic for MS. While its mechanism is not completely understood, dimethyl fumarate increases anti-inflammatory cytokines (IL-10, IL-4, and IL-6), decreases proinflammatory cytokines (IL-1β, IL-6, and TNF-α), and activates the Nrf2 pathway to protect neuronal cells. Nrf2 is activated by covalent bond-forming electrophiles such as dimethyl fumarate, a Michael acceptor. Dimethyl fumarate has been used for the treatment of psoriasis in Europe since 1994 and has a favorable long-term safety profile. An exploratory study in patients with relapsing remitting MS showed significant reductions in MS lesions after 18 weeks of treatment with 720 mg/day of dimethyl fumarate. Evaluation of dimethyl fumarate in a mouse experimental autoimmune encephalomyelitis model of MS resulted in reduced spinal cord macrophage inflammation. Dimethyl fumarate is obtained in high purity by esterification of fumaric acid with methanol and catalytic sulfuric acid. | | 化学的特性 | fine white crystalline powder | | Originator | Biogen Idec (United States) | | 使用 | Dimethyl fumarate acts as an immunomodulator. It is also used in cycloaddition reactions involving ylides, benzenes and amino acids. It is added to food grains,tobacco,leather and preservation. Clothing | | 定義 | ChEBI: Dimethyl fumarate is an enoate ester resulting from the formal condensation of both carboxy groups of fumaric acid with methanol. Used for treatment of adults with relapsing forms of multiple sclerosis. It has a role as an immunomodulator and an antipsoriatic. It is an enoate ester, a methyl ester and a diester. It is functionally related to a methanol and a fumaric acid. | | brand name | Tecfidera | | Synthesis Reference(s) | Synthetic Communications, 21, p. 223, 1991 DOI: 10.1080/00397919108020815
The Journal of Organic Chemistry, 55, p. 329, 1990 DOI: 10.1021/jo00288a056 | | 一般的な説明 | Dimethyl fumarate is a novel oral therapeutic agent, which can be used for patients suffering from relapsing-remitting multiple sclerosis. It shows an effective inhibition of mould in bread and can also serve as a potential candidate for the treatment of psoriasis, a chronic autoimmune condition. | | 接触アレルゲン | Dimethylfumarate, a strong irritant, is used as an industrial wide spectrum biocide in Asia and mainly in China, for textiles, leather, seeds, food, and cosmetic ingredients. It provoked a worldwide epidemic of severe contact dermatitis, initially from Chinese sofas sold in Finland, Great Britain, and France. It also induced severe burning and contact allergy due to shoes, and to contaminated clothing as well. This chemical, presents as is (white powder) or as tablets contained in little bags disposed in/or around the materials to protect, progressively evaporates and contaminates the environment. It is forbidden in the European Union since 2008 | | 臨床応用 | Treatment of relapsing-remitting multiple sclerosis
Treatment of moderate to severe plaque psoriasis | | 薬物相互作用 | Potentially hazardous interactions with other drugs
Aminophylline and theophylline: enhanced effect of
aminophylline and theophylline.
Anaesthetics: enhanced hypotensive effect.
Anti-arrhythmics: increased risk of bradycardia, AV
block and myocardial depression with amiodarone;
increased risk of bradycardia and myocardial
depression with dronedarone.
Antibacterials: metabolism increased by rifampicin;
metabolism possibly inhibited by clarithromycin,
erythromycin and telithromycin.
Antidepressants: enhanced hypotensive effect with
MAOIs; concentration of imipramine and possibly
other trycyclics increased
Antiepileptics: effect probably reduced by
barbiturates, fosphenytoin, phenytoin, and
primidone; enhanced effect of carbamazepine;
increased levels of fosphenytoin and phenytoin.
Antifungals: negative inotropic effect possibly
increased with itraconazole.
Antihypertensives: enhanced hypotensive effect;
increased risk of first dose hypotensive effect of postsynaptic alpha-blockers
Antipsychotics: concentration of lurasidone
increased.
Antivirals: concentration increased by atazanavir and
ritonavir - reduce dose of diltiazem with atazanavir;
concentration reduced by efavirenz; use telaprevir
with caution.
Avanafil: possibly increases avanafil concentration.
Beta-blockers: risk of bradycardia and AV block if
co-prescribed with beta-blockers.
Cardiac glycosides: increased digoxin concentration.
Ciclosporin: increased ciclosporin concentrations.
Cilostazol: increased cilostazol concentration -
avoid.
Colchicine: possibly increased risk of colchicine
toxicity - suspend or reduce colchicine, avoid
concomitant use in renal or hepatic failure.
Cytotoxics: concentration of bosutinib, ibrutinib and
olaparib possibly increased - avoid or reduce dose;
possibly increased risk of bradycardia with crizotinib.
Fingolimod: increased risk of bradycardia.
Ivabradine: concentration of ivabradine increased -
avoid.
Lipid lowering drugs: concentration of lomitapide
possibly increased - avoid.
Sirolimus: sirolimus concentration increased. | | 代謝 | Diltiazem is almost completely absorbed from the
gastrointestinal tract after oral doses, but undergoes
extensive first-pass hepatic metabolism resulting in a
bioavailability of about 40%. It is extensively metabolised
in the liver, mainly by the cytochrome P450 isoenzyme
CYP3A4; one of the metabolites, desacetyldiltiazem,
has been reported to have 25-50% of the activity of the
parent compound.
About 2-4% of a dose is excreted in urine as unchanged
diltiazem with the remainder excreted as metabolites in
bile and urine. |
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