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Mebendazole/甲苯咪唑 {[allProObj[0].p_purity_real_show]}

货号:A162607 同义名: 甲苯达唑 / NSC 184849; Vermox

Mebendazole是一种hedgehog信号通路抑制剂,并且是治疗线虫感染的广谱抗蠕虫药。

Mebendazole/甲苯咪唑 化学结构 CAS号:31431-39-7
Mebendazole/甲苯咪唑 化学结构
CAS号:31431-39-7
Mebendazole/甲苯咪唑 3D分子结构
CAS号:31431-39-7
Mebendazole/甲苯咪唑 化学结构 CAS号:31431-39-7
Mebendazole/甲苯咪唑 3D分子结构 CAS号:31431-39-7
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Mebendazole/甲苯咪唑 纯度/质量文件 产品仅供科研

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Mebendazole/甲苯咪唑 生物活性

描述 Mebendazole is an antiparasitic which can bind nematode tubulin and cause inhibition of intestinal microtubule synthesis. It also inhibits Hh signaling, targeting SMO. Mebendazole was sufficient to reduce ShhN-induced expression of endogenous GLI1 and PTCH1 to basal levels at 0.1μM in the immortalized human retinal pigment epithelial cell line hTERT-RPE1. Similarly, there was partial reduction in GLI1 and PTCH1 transcripts at 0.1μM mebendazole and almost complete suppression at 1μM mebendazole, on the human medulloblastoma cell line DAOY. This inhibition of Hh signaling by Mebendazole led decrease of cell proliferation and survival, and increase apoptosis. Daily gavage of Mebendazole at dose of 50mg/kg for 38 days extended the median survival of DAOY orthotopic tumor xenograft mice. Mebendazole at 1μM decreased activation of SMO shown by the Gli-luc and Renilla reporter in NIH3T3 fibroblasts maintained in low-serum conditions for 48 hours. Mebendazole suppressed the formation of the primary cilium, a microtubule based organelle that functions as a signaling hub for Hh pathway activation. Combination of vismodegib and mebendazole resulted in additive Hh signaling inhibition[5].

Mebendazole/甲苯咪唑 动物研究

Dose Mice: 1 mg/kg - 50 mg/kg[2] (p.o.), 10 mg/kg- 100 mg/kg[3] (p.o.) Rat: 10 mg/kg[2] (p.o.)
Administration p.o.
Pharmacokinetics
Animal Dogs[4]
Dose 500 mg tablet
Administration Current hewable tablet
AUC0→24h 221 ng·h/ml
T1/2 2.072 h
Tmax 9.90 h
AUC0→31h 258 ng·h/ml
Cmax 23.4 ng/ml
AUC0→∞ 228 ng·h/ml

Mebendazole/甲苯咪唑 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
NCT00000314 Cocaine-Related Disorders Phase 2 Completed - United States, New York ... 展开 >> VA Medical Center Brooklyn, New York, United States, 11209 收起 <<
NCT00080444 Vomiting Phase 3 Completed - -
NCT03472573 Recurrent B Acute Lymphoblasti... 展开 >>c Leukemia Refractory B Acute Lymphoblastic Leukemia 收起 << Phase 1 Recruiting November 2020 United States, Pennsylvania ... 展开 >> Sidney Kimmel Cancer Center at Thomas Jefferson University Recruiting Philadelphia, Pennsylvania, United States, 19107 Contact: Margaret Kasner, MD    215-955-8874    margaret.kasner@jefferson.edu    Principal Investigator: Margaret Kasner, MD 收起 <<

Mebendazole/甲苯咪唑 参考文献

[1]Larsen AR, Bai RY, et al. Repurposing the antihelmintic mebendazole as a hedgehog inhibitor. Mol Cancer Ther. 2015 Jan;14(1):3-13.

[2]Maki J, Yanagisawa T, et al. Studies on anthelmintic effects of flubendazole and mebendazole on the rat lungworm Angiostrongylus cantonensis in mice and rats. J Parasitol. 1986 Aug;72(4):512-6.

[3]Maki J, Yanagisawa T, et al. Anthelmintic effects of bithionol, paromomycin sulphate, flubendazole and mebendazole on mature and immature Hymenolepis nana in mice. J Helminthol. 1985 Sep;59(3):211-6.

[4]Mebendazole

[5]Larsen AR, Bai RY, Chung JH, Borodovsky A, Rudin CM, Riggins GJ, Bunz F. Repurposing the antihelmintic mebendazole as a hedgehog inhibitor. Mol Cancer Ther. 2015 Jan;14(1):3-13. doi: 10.1158/1535-7163.MCT-14-0755-T. Epub 2014 Nov 5. PMID: 25376612; PMCID: PMC4297232.

Mebendazole/甲苯咪唑 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.39mL

0.68mL

0.34mL

16.93mL

3.39mL

1.69mL

33.87mL

6.77mL

3.39mL

Mebendazole/甲苯咪唑 技术信息

CAS号31431-39-7
分子式C16H13N3O3
分子量 295.29
SMILES Code COC(=O)NC1=NC2=C(N1)C=CC(=C2)C(=O)C1=CC=CC=C1
MDL No. MFCD00057872
别名 甲苯达唑 ;NSC 184849; Vermox; Wormkuur; Vermin; Vermidil; Vermicol; R 17635; Mebenvet; Pantelmin; Telmin
运输蓝冰
InChI Key OPXLLQIJSORQAM-UHFFFAOYSA-N
Pubchem ID 4030
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, room temperature

溶解方案

DMSO: 3 mg/mL(10.16 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

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