| CAS: | 129299-72-5 | |
| 英文名称: |
|
| 货号 | 品牌 | 产品名称 | 规格 | 包装、参考价格 | |||
| HY-101638A | MCE | (±)-Fabesetron,129299-72-5_MCE(MedChemExpress) | 咨询 | ||||
MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。 (±)-FabesetronMCE 国际站：(±)-Fabesetron 品牌：MedChemExpress (MCE) 货号：HY-101638A CAS 号：129299-72-5 生物活性： (±)-法贝司琼（(±)-FK1052 游离碱）是法贝司琼的外消旋体，法贝司琼是一种强效的 5-HT3 和 5-HT4 受体双重拮抗剂[1]。 体内研究(In Vivo)：In conscious rats, both 5-HT and 5-methoxytryptamine significantly increase fecal pellet output and accelerate colonic transit. In contrast, the effect of 2-methyl-5-HT is slight. Although Ondansetron and Granisetron slightly reduce 5-HT (1 mg/kg s.c.) stimulated colonic transit, FK1052, at 0.1 mg/kg p.o., inhibits completely the increases in the colonic transit. Furthermore, FK1052, Ondansetron and Granisetron significantly depress the increase in fecal pellet output caused by wrap-restraint stress, with ED50 values of 0.21, 3.0 and 1.1 mg/kg p.o., respectively. Intraperitoneal administration of 5-HT and 5-methoxytryptamine, but not 2-methyl-5-HT, produces a dose-related increase in the incidence of diarrhea in fasted mice. 5-HT (0.32 mg/kg i.p.)-induced diarrhea is also inhibited by FK1052, Ondansetron and Granisetron, with ED50 values of 0.09, 2.3 and 0.88 mg/kg p.o., respectively[1]. FK1052 (1 mg/kg i.v. ×4) apparently reduces delayed emesis caused by Methotrexate (MTX) and increases, but not significantly, the time for onset of emesis. Furthermore, increasing the dose to 3.2 mg/kg of FK1052 also significantly inhibits the number of the emetic episodes induced by MTX, of which the action is more effective than the treatment with FK1052 at 1 mg/kg[2]. MCE尚未独立确认这些方法的准确性。 仅供参考。 分子量：293.36 Formula：C18H19N3O 运输条件：美国大陆地区的室温；其他地区可能有所不同。 储存方式：请按照分析证书中推荐的条件储存产品。 Animal Administration [1]：Mice and Rats[1] Male Sprague-Dawley rats weighing 220 to 330 g and male ddy mice weighing 25 to 35 g are used. FK1052, Ondansetron, Granisetron, Methysergide, Ketanserin and Atropine are dissolved in distilled water. 5-HT, 2-methyl-5-HT, 1-phenylbiguanide and 5-MeOT are dissolved in physiological saline. Diazepam is suspended with 0.5% methylcellulose solution. The drugs are administered to rats at a volume of 2 mL/ kg and to mice at a volume of 5 mL/kg. Dogs[2] Beagle dogs of either sex weighting 8.0 to18.5 kg are used in the study. Dogs are injected i.v. with MTX (2.5 mg/kg/mL) at 7:30 AM. The animal behavior is recorded using a video camera with an automatic night photographing system for up to 72 h and analyzed at the end of the experiment. FK1052 (1 and 3.2 mg/kg), Ondansetron (1 mg/kg), Tropisetron (1 mg/kg), CP-122,721 (0.1 mg/kg), or vehicle (0.5 mL/kg) is administered i.v. at 24, 36, 48, and 60 h after MTX treatment. Episodes of emesis occurring within a few minutes are defined as a single emetic episode. A 12 h artificial light cycle (lights on between 7:30 AM and 7:30 PM) is used throughout the study. Dogs are given a standard laboratory dog chow (300 g/day) and water ad libitum. The animals are retested with MTX at least 6 weeks later. MCE尚未独立确认这些方法的准确性。 仅供参考。 提供质量检测报告：Data Sheet、产品使用指南 产品活性：(±)-Fabesetron ((±)-FK1052 free base) 是 Fabesetron 的消旋体。Fabesetron 是一种有效的 5-HT3 和 5-HT4 受体双重拮抗剂。 IC50 & Target：5-HT3 and 5-HT4 receptor[1] 相关产品：BW-723C86 | PCPA methyl ester hydrochloride | CP 93129 dihydrochloride | RS-102221 hydrochloride | Deramciclane | Lesopitron dihydrochloride | GR 55562 dihydrochloride | BW-723C86 (Standard) | PCPA methyl ester hydrochloride (Standard) | RS-102221 hydrochloride (Standard) | Xylamidine | CP 93129 dihydrochloride (Standard) 热门产品线：抑制剂 | 稳定性同位素标记物 | 脂质 | 糖类 Trending products：Inhibitors | Isotope-Labeled Compounds | Lipids | Saccharides MCE 抑制剂: MedChemExpress 信号通路产品覆盖细胞凋亡、自噬、细胞周期与 DNA 损伤、表观遗传、GPCR/G 蛋白、免疫与炎症、JAK/STAT、MAPK/ERK、膜转运体与离子通道、代谢酶与蛋白酶、神经信号、NF-κB、PI3K/Akt/mTOR、PROTAC、蛋白酪氨酸激酶/受体酪氨酸激酶、干细胞/Wnt、TGF-β/Smad 及维生素 D/核受体等研究方向，为肿瘤、感染、炎症与免疫、神经系统疾病、代谢性疾病、心血管疾病和内分泌研究提供多维度的产品选择，助力客户发表文献超 80,000 篇。 相关产品可根据具体情况提供化学结构、作用靶点、生物活性、纯度、溶解度、体内外研究信息、参考文献及质量分析报告 (COA)等资料。 客户发表文献： 参考文献： 品牌介绍:
 | |||||||
m.cnreagent.com
