1. Anti-infection
  2. Parasite
  3. AN7973

AN7973 

目录号: HY-128337
产品使用指南

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。

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AN7973 Chemical Structure

AN7973 Chemical Structure

CAS No. : 1620899-32-2

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Size Price Stock Quantity
10 mM * 1 mL in DMSO ¥3850 In-stock
5 mg ¥3500 In-stock
10 mg ¥5800 In-stock
25 mg ¥11000 In-stock
50 mg ¥17000 In-stock
100 mg ¥25000 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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Description

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 drug candidate for treating cryptosporidiosis.

In Vivo

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[1].
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[1].
AN7973 possesses favorable safety, stability, and PK parameters as an exciting drug candidate for treating cryptosporidiosis[1].

MCE 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[1]
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[1]
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[1]
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.
Molecular Weight

381.62

Formula

C₁₉H₁₇BClN₃O₃

CAS No.

1620899-32-2

SMILES

ClC1=CC(N2C=CC=N2)=CC=C1C(NC3=CC=C(C(C)(C)OB4O)C4=C3)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

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

Preparing
Stock Solutions
Concentration Solvent Mass 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
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 MCE 网站选购。
References
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

AN7973AN 7973AN-7973ParasiteInhibitorinhibitorinhibit

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