1. Anti-infection
  2. Parasite
  3. DNDI-8219

DNDI-8219 (compound 58) 是一种有效且具有选择性和口服活性的杀锥虫剂,对克氏锥虫 (T. cruzi)IC50 为 0.4 μM。DNDI-8219 具有较低的细胞毒性 (L6 细胞 IC50 > 100 μM)。DNDI-8219 在小鼠模型中能有效研究慢性克氏锥虫感染,明显减少寄生虫负担。具有良好的溶解度、代谢稳定性和安全性。

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DNDI-8219 Chemical Structure

DNDI-8219 Chemical Structure

CAS No. : 2222660-40-2

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Other Forms of DNDI-8219:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DNDI-8219 (compound 58) is a potent selective and orally active trypanocidal agent, possessing inhibitory activity against Trypanosoma cruzi (T. cruzi) with an IC50 of 0.4 μM. DNDI-8219 has low cytotoxicity (L6 cells IC50 > 100 μM). DNDI-8219 can effectively cure chronic T. cruzi infection and markedly reduce parasite burdens in mouse model. DNDI-8219 has good solubility, metabolic stability and safety.

IC50 & Target

Trypanosoma

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
L6 IC50
> 100 μM
Compound: 58
Cytotoxicity against rat L6 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay
Cytotoxicity against rat L6 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue assay
[PMID: 33007723]
MRC5 IC50
> 64 μM
Compound: R-6
Cytotoxicity against human MRC5 cells after 72 hrs by resazurin dye based assay
Cytotoxicity against human MRC5 cells after 72 hrs by resazurin dye based assay
[PMID: 29461823]
体内研究
(In Vivo)

DNDI-8219 (50 or 100 mg/kg; PO; once daily for five days) completely cures chronic infection, as well as markedly reduces?parasite burdens?in mice[1].

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

Animal Model: Female BALB/c mice (infected with T. cruzi; n=5)[1]
Dosage: 50 or 100 mg/kg
Administration: PO; once daily for five days
Result: Completely cured one of five mice in a chronic infection mouse model, as well as markedly reduced parasite burdens in two other mice.
分子量

345.23

Formula

C13H10F3N3O5

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献

DNDI-8219 相关分类

  • 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)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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DNDI-8219
目录号:
HY-124623
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