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Oxibendazole

Oxibendazole

产品编号 T6623   CAS 20559-55-1

Oxibendazole 是一种苯并咪唑驱虫药,用于防止马和一些家养宠物的蛔虫、圆线虫、线虫、蛲虫和肺虫感染。。它可诱导细胞凋亡,具有抗癌和抗炎活性。

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Oxibendazole Chemical Structure
Oxibendazole, CAS 20559-55-1
规格 价格/CNY 货期 数量
10 mg ¥ 297 现货
25 mg ¥ 469 现货
50 mg ¥ 682 现货
100 mg ¥ 1,080 现货
200 mg ¥ 1,630 现货
1 mL * 10 mM (in DMSO) ¥ 195 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
MG-132限时半价
产品目录号及名称: Oxibendazole (T6623)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Oxibendazole is a benzimidazole drug that interferes with metabolic pathways, used to protect against roundworms, strongyles, threadworms, pinworms and lungworm infestations in horses and some domestic pets.
体外活性 BRL-15572 displays high affinity and selectivity for h5-HT1D receptors. BRL-15572 has 60-fold higher affinity for h5-HT1D than 5-HT1B receptors. BRL-15572 binds to h5-HT1B and h5-HT1D receptors with pKB of less than 6 and 7.1, respectively. BRL-15572 stimulates [35S]GTP γ S binding in both cell lines, with potencies that correlated with their receptor binding affinities in both h5-HT1B and h5-HT1D receptor expressing cell lines. BRL-15572 reveals receptor binding affinities for 5-HT1A, 5-HT1B, 5-HT1E, 5-HT1F, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT6 and 5-HT7 with pKi of 7.7, 6.1, 5.2, 6.0, 6.6, 7.4, 6.2, 5.9 and 6.3, respectively. In the h5-HT1D cell line, both BRL-15572 (1 μM) shifts the 5-HT concentration response curve with pKB of 7.1, respectively. BRL-15572 does have moderately high affinity at human 5-HT1A and 5-HT2B receptors. [1] In human atrial appendages, the electrically evoked tritium overflow is inhibited by 5-HT in a manner susceptible to antagonism by BRL-15572 (300 nM; 23 times Ki at h5-HT1D receptors). [2] The inhibitory effect of 5-HT on the K+-evoked overflow of glutamate is antagonized by the h5-HT1D receptor ligand BRL-15572. BRL-15572 (1 μM) is unable to modify the effect of 5-HT at the autoreceptor regulating [3H]5-HT release. [3] The selective 5-HT1D/1B receptor antagonist BRL 15572 inhibits the effect of the agonist L-694 247. [4]
体内活性 Oxibendazole shows a significant reduction of the proportion of positive foals after treatment. Oxibendazole significantly reduces the proportion of positive horse foals on six of the seven farms (86%). [1] Oxibendazole reduces in the number of strongyle eggs/g (epg) in horse, but the reduction is only by 82% with an upper confidence limit of 89%. [2] Oxibendazole results in collapse of the lip papillae, rupture of buccal cavity cuticle, prolapse of the pharynx, degeneration of epithelial cells and erosion of microvilli in adult Ascaris suum, theses changes may lead to impaired digestion and absorption of nutrients and cause cellular autolysis, resulting in the death of the worm. [3] Oxibendazole reduces faecal worm egg counts (EPG) by 97.6% for Toxocara canis, 95.7% for Trichuris vulpis, 94.6% for Ancylostoma caninum, and 100% for Toxascaris leonine in dogs and cats. [4] Oxibendazole could only be detected in plasma at the 0.5 hours and 1.0 hours post administration sampling times and the mean maximum plasma concentration is 0.008 mg/mL in horse. Oxibendazole is detected in faeces between 12 and 72 hours after administration and the highest dry faecal concentration was detected at 24 hours. [5]
分子量 249.27
分子式 C12H15N3O3
CAS No. 20559-55-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 30 mg/ml (120.35 mM)

H2O: Insoluble

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.0117 mL 20.0586 mL 40.1171 mL 100.2929 mL
5 mM 0.8023 mL 4.0117 mL 8.0234 mL 20.0586 mL
10 mM 0.4012 mL 2.0059 mL 4.0117 mL 10.0293 mL
20 mM 0.2006 mL 1.0029 mL 2.0059 mL 5.0146 mL
50 mM 0.0802 mL 0.4012 mL 0.8023 mL 2.0059 mL
100 mM 0.0401 mL 0.2006 mL 0.4012 mL 1.0029 mL

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TargetMol Library Books参考文献

1. Lyons ET, et al. Parasitol Res,2011, 109(4), 1193-1197. 2. Slocombe JO, et al. Can Vet J,1989, 30(8), 663-665. 3. Magambo JK, et al. Afr J Health Sci,1998, 5(1), 38-41. 4. Overgaauw PA, et al. Vet Q,1998, 20(2), 69-72. 5. Gokbulut C, et al. Res Vet Sci,2002, 72(1), 11-15.

TargetMol Library Books文献引用

1. Kaduk J A, Gates-Rector S, Blanton T N.Crystal structure of oxibendazole, C12H15N3O3.Powder Diffraction.2023: 1-6.
Sophoraflavanone G CDK8-IN-13 Polyphyllin I Linderalactone Scriptaid Vanillyl Alcohol Bufotalin MMRi64

相关化合物库

该产品包含在如下化合物库中:
药物功能重定位化合物库 抗寄生虫库 抗癌活性化合物库 已知活性化合物库 人代谢物化合物库 临床期小分子药物库 经典已知活性库 FDA上市及药典收录分子库 抗癌化合物库 ReFRAME 相关化合物库

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母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

Oxibendazole 20559-55-1 Apoptosis Microbiology/Virology Parasite Inhibitor inhibit inhibitor

 

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