依氟鸟氨酸盐酸盐一水合物
Eflornithine hydrochloride hydrate
| 货号 | 包装规格 | 纯度/级别 | 交货周期 | 价格 | 数量 |
|---|---|---|---|---|---|
| YB00606-1g | 1g | 98% | 现货 | ||
| YB00606-5g | 5g | 98% | 现货 | ||
| YB00606-25g | 25g | 98% | 现货 |
| 中文名称 | 依氟鸟氨酸盐酸盐一水合物 |
|---|---|
| 英文名称 | Eflornithine hydrochloride hydrate |
| 别名 | 2-(Difluoromethyl)-DL-ornithine monohydrochloride monohydrate, Eflornithin monohydrochloride monohyd |
| Cas No. | 96020-91-6 |
| MDL No. | MFCD00242734 |
| 精确分子量 | 236.07393 |
| Smiles | C(CN)CC(N)(C(O)=O)C(F)F.O.Cl |
| 密度 | 1.293g/cm3 |
|---|---|
| 信号词 | Warning |
| 危险类别(旧) | R36/37/38 |
| 熔点 | 347ºC at 760mmHg |
| 化学稳定性 | 可在-20°下蒸馏水溶液保存长达3个月。 |
| 沸点 | 210ºC (dec.) |
| 运输要求 | 常温运输 |
| 海关编码 | 2922499990 |
| 特性 | * |
| 安全说明(旧) | S36/37/39-45 |
| 水溶解性 | water: 1mg/mL |
| 符号 | GHS07 |
| 存储要求 | 2-8°C |
| 闪点 | 163.7ºC |
Eflornithine (Difluoromethylornithine, DFMO, MDL-71782, RMI-71782, α-difluoromethylornithine) hydrochloride hydrate 通过对鸟氨酸脱羧酶的不可逆抑制作用，抑制多胺生物合成。它是一种化疗保护剂，可阻止血管生成。其生物半衰期为8小时。
靶点
| Target | Value |
| Orn decarboxylase |
体外研究
用α-difluoromethyl-Orn处理BY2细胞，抑制其过氧化氢的产生，但并没有发生程序性细胞死亡。
体内研究
Eflornithine is the only new molecule registered for the treatment of human African trypanosomiasis over the last 50 years. It is the drug used mainly as a back-up for melarsoprol refractory Trypanosoma brucei gambiense cases. In subjects with excessive, unwanted facial hair, eflornithine 15% cream is superior to placebo in reducing hair growth. After 24 weeks' treatment, 58% of eflornithine and 34% of placebo subjects have at least some improvement in facial hirsutism. The hair growth inhibitory activity of eflornithine is significantly enhanced when the eflornithine cream is applied onto a mouse skin area pretreated with microneedles. Treatment of coarctation hypertensive rats with eflornithine results in a normalization of the contractile intensity to KCI and norepinephrine and relaxations to acetylcholine by 14 days of hypertension.
