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/ Fosaprepitant Dimeglumine/福沙匹坦二甲葡胺

Fosaprepitant Dimeglumine/福沙匹坦二甲葡胺 {[allProObj[0].p_purity_real_show]}

货号：A455841 同义名： 福沙吡坦二甲葡胺 / MK-0517; L785298

Fosaprepitant Dimeglumine是一种阿普瑞必妥的前药，阿普瑞必妥是一种选择性且高亲和力的NK1受体拮抗剂。

Fosaprepitant Dimeglumine/福沙匹坦二甲葡胺 化学结构 CAS号：265121-04-8
Fosaprepitant Dimeglumine/福沙匹坦二甲葡胺 化学结构
CAS号：265121-04-8
Fosaprepitant Dimeglumine/福沙匹坦二甲葡胺 3D分子结构
CAS号：265121-04-8
Fosaprepitant Dimeglumine/福沙匹坦二甲葡胺 化学结构 CAS号：265121-04-8
Fosaprepitant Dimeglumine/福沙匹坦二甲葡胺 3D分子结构 CAS号：265121-04-8
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Fosaprepitant Dimeglumine/福沙匹坦二甲葡胺 纯度/质量文件 产品仅供科研

货号：A455841 标准纯度： {[allProObj[0].p_purity_real_show]}
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Fosaprepitant Dimeglumine/福沙匹坦二甲葡胺 生物活性

描述 Known to induce vomiting, substance P binds to NK-1 receptors in the abdominal vagus, the NTS and the area postrema. Compounds that block NK-1 receptors lessen emesis after cisplatin, ipecac, apomorphine and radiation therapy[3]. Aprepitant is a selective NK-1 receptor antagonist approved as a therapy for the prevention of acute and delayed chemotherapy-induced nausea and vomiting (CINV). Fosaprepitant is a water-soluble phosphoryl prodrug for aprepitant, which, when administered intravenously, is converted to aprepitant within 30 min via the action of ubiquitous phosphatases[3]. Injection of the NK-1 receptor antagonists fosaprepitant directly into the vicinity of the NTS neurons inhibited cisplatin-induced emesis in the ferret, which suggested fosaprepitant may exert its main anti-emetic action centrally by depressing the neural activity of the NTS neurons, with possibly some peripheral anti-emetic effect through blockade of NK-1 receptors located on vagal terminals in the gut[3]. Preclinical toxicology studies of bolus fosaprepitant administered in seconds to dogs and rats showed that concentrations of 1 mg/ml were well tolerated. Concentrations up to 25 mg/ml at low doses (2 – 4 mg/kg/day) were well tolerated in dog[4].

Fosaprepitant Dimeglumine/福沙匹坦二甲葡胺 细胞实验

Cell Line
Concentration Treated Time Description References
SY5Y 5 µM 72 hours Evaluate cell death and proliferation capacity, showing relative resistance Oncotarget. 2017 Jan 3;8(1):430-443
SK-N-AS 0.85 µM 72 hours Determine IC50 values, showing a specific effect on malignant cells Oncotarget. 2017 Jan 3;8(1):430-443
IMR5 0–80 µM 72 hours Assess the effect of TACR1 inhibition on neuroblastoma cell viability, observed a concentration-dependent reduction in cell viability Oncotarget. 2017 Jan 3;8(1):430-443

Fosaprepitant Dimeglumine/福沙匹坦二甲葡胺 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Wistar rats Colorectal distension-induced vagal reflex model Intraperitoneal injection 30 mg/kg Single dose, colorectal distension performed 40 minutes after administration To investigate the effect of fosaprepitant on the circulatory response induced by colorectal distension. Results showed that fosaprepitant reduced the blood pressure drop caused by colorectal distension and decreased the number of c-Fos immunoreactive cells in the caudal ventrolateral medullary region. Front Pharmacol. 2022 Oct 19;13:1020685
Nude mice IMR5 xenograft model Intraperitoneal injection 60 mg/kg body weight/day Once daily for 14 days Assess the effect of fosaprepitant on tumor burden, observed significant delay in tumor growth Oncotarget. 2017 Jan 3;8(1):430-443
New Zealand White rabbits Joint contracture model Intra-articular injection 1 mL (1 mg) Injected at 3, 6, 12, and 24 hours after surgery To assess the effect of SP inhibition on pro-fibrotic gene expression in a post-traumatic joint contracture model. Results showed that fosaprepitant significantly altered the expression of pro-fibrotic genes but had no significant effect on joint contracture angles. J Cell Biochem. 2018 Feb;119(2):1326-1336

Fosaprepitant Dimeglumine/福沙匹坦二甲葡胺 动物研究

Dose Rat: 1 mg/kg, 8 mg/kg[3] (i.v.)
Administration i.v.

Fosaprepitant Dimeglumine/福沙匹坦二甲葡胺 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00090207 Nausea Vomiti... 展开 >>ng 收起 << Phase 4 Completed - -
NCT00726960 Opioid-Related Disorders ... 展开 >> Heroin Dependence Substance-Related Disorders 收起 << Phase 1 Unknown June 2010 Sweden ... 展开 >> Karolinska University Hospital, Huddinge Stockholm, Sweden, 14186 收起 <<
NCT00717054 Nausea Vomiti... 展开 >>ng 收起 << Not Applicable Completed - United States, Pennsylvania ... 展开 >> Hahnemann University Hospital Philadelphia, Pennsylvania, United States, 19102 收起 <<

Fosaprepitant Dimeglumine/福沙匹坦二甲葡胺 参考文献

[1]Grunberg S, Chua D, et al. Single-dose fosaprepitant for the prevention of chemotherapy-induced nausea and vomiting associated with cisplatin therapy: randomized, double-blind study protocol--EASE. J Clin Oncol. 2011 Apr 10;29(11):1495-501.

[2]Olver IN. Prevention of chemotherapy-induced nausea and vomiting: focus on fosaprepitant. Ther Clin Risk Manag. 2008 Apr;4(2):501-6.

[3]Navari RM. Fosaprepitant (MK-0517): a neurokinin-1 receptor antagonist for the prevention of chemotherapy-induced nausea and vomiting. Expert Opin Investig Drugs. 2007 Dec;16(12):1977-85. doi: 10.1517/13543784.16.12.1977. PMID: 18042005.

[4]Olver IN. Prevention of chemotherapy-induced nausea and vomiting: focus on fosaprepitant. Ther Clin Risk Manag. 2008 Apr;4(2):501-6. doi: 10.2147/tcrm.s2345. PMID: 18728837; PMCID: PMC2504061.

Fosaprepitant Dimeglumine/福沙匹坦二甲葡胺 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.00mL

0.20mL

0.10mL

4.98mL

1.00mL

0.50mL

9.95mL

1.99mL

1.00mL

Fosaprepitant Dimeglumine/福沙匹坦二甲葡胺 技术信息

CAS号265121-04-8
分子式C37H56F7N6O16P
分子量 1004.83
SMILES Code OC[C@H]([C@H]([C@@H]([C@H](CNC)O)O)O)O.OC[C@H]([C@H]([C@@H]([C@H](CNC)O)O)O)O.O=C1NC(CN2[C@H]([C@H](OCC2)O[C@H](C)C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)C4=CC=C(C=C4)F)=NN1P(O)(O)=O
MDL No. MFCD23102059
别名 福沙吡坦二甲葡胺 ;MK-0517; L785298; Fosaprepitant dimeglumine salt; Fosaprepitant(dimeglumine)
运输蓝冰
InChI Key VRQHBYGYXDWZDL-OOZCZQCLSA-N
Pubchem ID 135564864
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C
溶解方案

H2O: 50 mg/mL(49.76 mM)，配合低频超声助溶

配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

Tags: Fosaprepitant dimeglumine | 265121-04-8 | MK-0517 | L785298 | MK0517 | MK 0517 | L785298 | L 785298 | L-785298 | Neurokinin-1 Receptor Antagonist | GPCR/G Protein | Neuronal Signaling | Neurokinin Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Fosaprepitant Dimeglumine/福沙匹坦二甲葡胺 纯度/质量文件 | Fosaprepitant Dimeglumine/福沙匹坦二甲葡胺 生物活性 | Fosaprepitant Dimeglumine/福沙匹坦二甲葡胺 动物研究 | Fosaprepitant Dimeglumine/福沙匹坦二甲葡胺 临床数据 | Fosaprepitant Dimeglumine/福沙匹坦二甲葡胺 参考文献 | Fosaprepitant Dimeglumine/福沙匹坦二甲葡胺 实验方案 | Fosaprepitant Dimeglumine/福沙匹坦二甲葡胺 技术信息

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