Delamanid(OPC-67683)

¥600.00

规格: 5mg

CAS 号:681492-22-8
英文名字:迪拉马尼
质量标准:>98%,BR
库存详情未设置 SKU: MB3005-1 分类: ,

Delamanid(OPC-67683)
分子式:C25H25F3N4O6分子量:534.48

简介:Delamanid是一种新型的抗肺结核药物,具有良好的胞内杀菌活性,在细胞中具有高积累率。
中文名:迪拉马尼
物理性状及指标:
外观:……………………粉末
溶解性:…………………Ethanol:2 mg/mL (3.74 mM);DMSO : 100 mg/mL (187.10 mM);Water:Insoluble
含量:……………………>98.0
储存温度:-20℃,避光防潮密闭干燥

生物活性

描述
Delamanid是一种新型的抗肺结核药物,具有良好的胞内杀菌活性,在细胞中具有高积累率。

体外

Delamanid potently inhibits the synthesis of mycolic acid, a long-chain fatty acid of the M. tuberculosis (mycobacterium tuberculosis) cell wall. Delamanid at concentrations of less than 5 μM shows no inhibitory effects on the efflux ABC transporters P-gp, BCRP, and BSEP or on the hepatic or renal SLC transporters OATPs, OCTs, and OATs. Delamanid is not metabolized by NADPH-dependent reactions, including those catalyzed by CYP enzymes, in human or animal liver microsomes. Also, delamanid has no inhibitory effects on the metabolism of exogenous CYP substrate compounds by eight CYP isoforms (CYP1A2, CYP2A6, CYP2B6, CYP2C8/9, CYP2C19, CYP2D6, CYP2E1, and CYP3A), even at a concentration of 100 μmol/liter, well above the therapeutic concentration.

体内

The water solubility of delamanid is poor and its absorption is increased more than two-fold by coadministration with food. The absolute bioavailability is unknown but estimated to be between 25% and 47%. In vivo, delamanid is more than 99% protein bound, with a high volume of distribution (Vz/F of 2100 L) and a half-life of 30-38 hours. Delamanid is excreted primarily in the stool, with less than 5% excretion in the urine. It is thought to be primarily metabolized by albumin, with secondary contributions from P450 enzymes, primarily CYP3A4. Animal studies indicate that delamanid is excreted in breast milk.

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储液配置及储存:按表中溶解性配置;如溶解困难,可以通过快速搅拌,超声或温和加热(在45-60°C下水浴)。液体稳定性报道的很少,建议现配现用,如需储存,建议:-20℃1-3月;-80℃ 3-6月。

运输条件:常温运输

1 mg

5 mg

10 mg

1 mM 1.8710 mL 9.3549 mL 18.7098 mL
5 mM 0.3742 mL 1.8710 mL 3.7420 mL
10 mM 0.1871 mL 0.9355 mL 1.8710 mL
50 mM 0.0374 mL 0.1871 mL 0.3742 mL

【注意】
●我司产品为非无菌包装,若用于细胞培养,请提前做预处理,除去热原细菌,否则会导致染菌。

●部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,以上数据仅供参考交流研究之用。

规格

5mg

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