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地克珠利 /Diclazuril {[allProObj[0].p_purity_real_show]}

货号:A730578 同义名: R-64433 Ambeed 开学季,买赠积分,赢豪礼

Diclazuril is a carbonic anhydrase inhibitor that is used in the treatment of glaucoma.

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Diclazuril 化学结构 CAS号:101831-37-2
Diclazuril 化学结构
CAS号:101831-37-2
Diclazuril 3D分子结构
CAS号:101831-37-2
Diclazuril 化学结构 CAS号:101831-37-2
Diclazuril 3D分子结构 CAS号:101831-37-2
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Diclazuril 纯度/质量文件 产品仅供科研

货号:A730578 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Carbonic Anhydrase Carbonic Anhydrase I Carbonic Anhydrase II Carbonic Anhydrase IV Carbonic Anhydrase IX Carbonic Anhydrase XII 其他靶点 纯度
Topiramate Calcium Channel {[allProObj[0].p_purity_real_show]}
Dichlorphenamide {[allProObj[0].p_purity_real_show]}
Mafenide Acetate {[allProObj[0].p_purity_real_show]}
Benzenesulphonamide {[allProObj[0].p_purity_real_show]}
Dorzolamide HCl +

Carbonic anhydrase I, Ki: 6000 nM

++++

Carbonic anhydrase II, Ki: 1.9 nM

+++

Carbonic anhydrase IV, Ki: 31 nM

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Methazolamide ++

hCAI, Ki: 50 nM

+++

hCAII, Ki: 14 nM

++

bCAIV, Ki: 36 nM

{[allProObj[0].p_purity_real_show]}
Tioxolone +

CAI, Ki: 91 nM

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U-104 ++

CAIX, Ki: 45.1 nM

++++

CAXII, Ki: 4.5 nM

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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Diclazuril 生物活性

描述 Diclazuril (R-64433), a benzeneacetonitrile derivative, is a potent and orally active anticoccidial agent. The good efficacy of toltrazuril administered orally to lambs in the prepatent period in subclinical natural Eimeria infections in housed lambs[3]. G4 and G5 animals immunized with 0.2% diclazuril-treated oocysts showed a significant decrease in bloody diarrhea severity, lesion scores, and oocyst counts in comparison to those immunized with untreated oocysts. Diclazuril is effective in attenuating Eimeria oocysts[4]. The mRNA and protein expression levels of EtENO were decreased by 36.3 and 40.36%, respectively, by diclazuril treatment. With diclazuril treatment, it was significantly reduced in the surface and cytoplasm and even disappeared in the nucleus of the infected/diclazuril group[5]. Diclazuril treatment significantly protected dams from hepatitis, also in tachyzoites dose (100, 300, 600) dependent manner (respectively infected-treated versus infected controls). Colonic tissues were significantly shortened in length, with infiltration of lymphocytes, and macrophages and microabscess formations in the cryptic structures, with significant improvement in diclazuril treated animals. Additionally, the number of fetuses, fetal length and fetal weight were preserved in diclazuril treated dams[6].

Diclazuril 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
NCT00001018 Cryptosporidiosis ... 展开 >> HIV Infections 收起 << Phase 1 Completed - United States, California ... 展开 >> USC School of Medicine Los Angeles, California, United States, 90033 United States, New York Dr Douglas Dieterich New York, New York, United States, 10016 Cornell Univ Med Ctr New York, New York, United States, 10021 Saint Luke's - Roosevelt Hosp Ctr New York, New York, United States, 10025 收起 <<
NCT00002027 Cryptosporidiosis ... 展开 >> HIV Infections 收起 << Not Applicable Completed - United States, New York ... 展开 >> Dr Douglas Dieterich New York, New York, United States, 10016 Cornell Univ Med Ctr New York, New York, United States, 10021 Saint Luke's - Roosevelt Hosp Ctr New York, New York, United States, 10025 收起 <<
NCT00002278 Cryptosporidiosis ... 展开 >> HIV Infections 收起 << Not Applicable Completed - United States, New York ... 展开 >> Bellevue Hosp / New York Univ Med Ctr New York, New York, United States, 10016 Cornell Univ Med Ctr New York, New York, United States, 10021 Saint Luke's - Roosevelt Hosp Ctr New York, New York, United States, 10025 收起 <<

Diclazuril 参考文献

[1]Rucquoy M, Sorel L. Diclofenamide in the treatment of therapy-resistant epilepsy. Acta Neurol Belg. 1978 May-Jun;78(3):174-82.

[2]Kanski JJ. Carbonic anhydrase inhibitors and osmotic agents in glaucoma. Carbonic anhydrase inhibitors. Br J Ophthalmol. 1968 Aug;52(8):642-3.

[3]Diaferia M, Veronesi F, Morganti G, Nisoli L, Fioretti DP. Efficacy of toltrazuril 5 % suspension (Baycox®, Bayer) and diclazuril (Vecoxan®, Janssen-Cilag) in the control of Eimeria spp. in lambs. Parasitol Res. 2013 Aug;112 Suppl 1:163-8

[4]El-Ashram S, Aboelhadid SM, Arafa WM, Gadelhaq SM, Abdel-Razik AH. Protective potential of diclazuril-treated oocysts against coccidiosis in layer chicks. Vet Parasitol. 2019 Sep;273:105-111

[5]Zhou BH, Ding HY, Yang JY, Chai J, Guo HW, Wang HW. Effects of diclazuril on the expression of enolase in second-generation merozoites of Eimeria tenella. Poult Sci. 2020 Dec;99(12):6402-6409

[6]Oz HS, Tobin T. Diclazuril Protects against Maternal Gastrointestinal Syndrome and Congenital Toxoplasmosis. Int J Clin Med. 2014 Jan 1;5(3):93-101

Diclazuril 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.45mL

0.49mL

0.25mL

12.27mL

2.45mL

1.23mL

24.53mL

4.91mL

2.45mL

Diclazuril 技术信息

CAS号101831-37-2
分子式C17H9Cl3N4O2
分子量 407.64
别名 R-64433
运输蓝冰
存储条件

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 25 mg/mL(61.33 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

动物实验配方
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