AN7973,99.70%

产品编号:Bellancom-128337| CAS NO:1620899-32-2| 分子式:C19H17BClN3O3| 分子量:381.62

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用,

货号 包装 价格 库存与货期 购买量 操作
Bellancom-128337
3500.00 杭州 北京(现货)
Bellancom-128337
5800.00 杭州 北京(现货)
Bellancom-128337
11000.00 杭州 北京(现货)
Bellancom-128337
17000.00 杭州 北京(现货)
Bellancom-128337
25000.00 杭州 北京(现货)

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AN7973

产品介绍 AN7973 是 6-甲酰胺苯并氧杂硼杂环戊烯,阻止细胞内寄生虫 (parasite) 发育并抑制隐孢子虫生长。 AN7973 具有良好的安全性,稳定性和 PK 参数,可用于隐孢子虫病的研究。
生物活性

AN7973 is the 6-carboxamide benzoxaborole, blocks intracellular parasite development and inhibits Cryptosporidium growth. AN7973 is orally active, possesses favorable safety, stability, and PK parameters, and is an exciting agent candidate for treating cryptosporidiosis.

体外研究
体内研究

AN7973 (oral gavage; 5-25 mg/kg; once daily) is efficacious in murine models of both acute and chronic infection by rapidly eliminating C.parvum in vivo.
AN7973 (oral gavage; 5 mg/kg, 10 mg/kg, 6.67 mg/kg; once daily, twice daily, three times daily) reduces C.parvum fecal shedding, diarrhea, and dehydration in a neonatal calf model (closely mimics that seen in infants) of cryptosporidiosis.
AN7973 possesses favorable safety, stability, and PK parameters as an exciting drug candidate for treating cryptosporidiosis.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Four to five weeks NOD scid gamma mice (NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ)(NSG) with chronic Cryptosporidium infection
Dosage: 10 mg/kg, 20 mg/kg
Administration: Oral gavage; 10 mg/kg, 20 mg/kg; once daily
Result: Reduced parasite shedding by >99% at a dose of 25 mg/kg and by >90% at a dose of 10 mg/kg administration.
Animal Model: Four-week-old female C57BL/6 IFN-γ−/− mice with acute Cryptosporidium infection
Dosage: 5 mg/kg, 10 mg/kg, 25 mg/kg
Administration: Oral gavage; 5 mg/kg, 10 mg/kg, 25 mg/kg; once dairy
Result: Eliminated C.parvums at a dose-dependent efficacy.
Animal Model: One-day-old to two-day-old Holstein bull Neonatal calf model of cryptosporidiosis
Dosage: 5 mg/kg, 10 mg/kg, 6.67 mg/kg
Administration: Oral gavage; 5 mg/kg, 10 mg/kg, 6.67 mg/kg; once daily, twice daily, three times daily
Result: Curtailed parasite shedding and completely eliminated diarrhea.
体内研究

AN7973 (oral gavage; 5-25 mg/kg; once daily) is efficacious in murine models of both acute and chronic infection by rapidly eliminating C.parvum in vivo.
AN7973 (oral gavage; 5 mg/kg, 10 mg/kg, 6.67 mg/kg; once daily, twice daily, three times daily) reduces C.parvum fecal shedding, diarrhea, and dehydration in a neonatal calf model (closely mimics that seen in infants) of cryptosporidiosis.
AN7973 possesses favorable safety, stability, and PK parameters as an exciting drug candidate for treating cryptosporidiosis.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Four to five weeks NOD scid gamma mice (NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ)(NSG) with chronic Cryptosporidium infection
Dosage: 10 mg/kg, 20 mg/kg
Administration: Oral gavage; 10 mg/kg, 20 mg/kg; once daily
Result: Reduced parasite shedding by >99% at a dose of 25 mg/kg and by >90% at a dose of 10 mg/kg administration.
Animal Model: Four-week-old female C57BL/6 IFN-γ−/− mice with acute Cryptosporidium infection
Dosage: 5 mg/kg, 10 mg/kg, 25 mg/kg
Administration: Oral gavage; 5 mg/kg, 10 mg/kg, 25 mg/kg; once dairy
Result: Eliminated C.parvums at a dose-dependent efficacy.
Animal Model: One-day-old to two-day-old Holstein bull Neonatal calf model of cryptosporidiosis
Dosage: 5 mg/kg, 10 mg/kg, 6.67 mg/kg
Administration: Oral gavage; 5 mg/kg, 10 mg/kg, 6.67 mg/kg; once daily, twice daily, three times daily
Result: Curtailed parasite shedding and completely eliminated diarrhea.
性状Solid
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (327.55 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6204 mL 13.1020 mL 26.2041 mL
5 mM 0.5241 mL 2.6204 mL 5.2408 mL
10 mM 0.2620 mL 1.3102 mL 2.6204 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制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

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.45 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.45 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.45 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.45 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.45 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.45 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 西域 网站选购。
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

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