2. Anti-infection
  3. Parasite
  4. NPD-2975

NPD-2975 (compound 30) 是一种口服有效抗锥虫药，可对抗非洲人类锥虫病 (HAT)。 NPD-2975 在人 MRC-5 肺成纤维细胞和急性感染布氏锥虫 (T. b. brucei) 的小鼠模型中具有低毒性。NPD-2975 显示出可接受的代谢稳定性，体外抑制 T. b. brucei 的 IC500 为 70 nM。NPD-2975 抑制 CYP450 酶，对 CYP1A2 和 CYP2C19 的 IC50 分别为 0.16 和 0.42 μM。

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NPD-2975 Chemical Structure

NPD-2975 Chemical Structure

CAS No. : 3032452-65-3

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NPD-2975 相关抗体

Top Publications Citing Use of Products

查看 Parasite 亚型特异性产品:

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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NPD-2975 (compound 30) is an orally active antitrypanosomal agent, against Human African Trypanosomiasis (HAT). NPD-2975 has low toxicity potential against human MRC-5 lung fibroblasts, and acute mouse model of T. b. brucei infection. NPD-2975 shows acceptable metabolic stability, inhibits T. b. brucei with IC500 of 70 nM in vitro. NPD-2975 also inhibits CYP enzymes resulted in IC50 values of 0.16 and 0.42 μM against CYP1A2 and CYP2C19, respectively[1].

IC50 & Target

IC50: 70 nM (Trypanosoma brucei), 0.16 μM (CYP1A2), 0.42 μM (CYP2C19)[1]
体内研究
(In Vivo)

NPD-2975 (25 mg/kg，每日2次，连用5天；灌胃) 提高了 HAT 感染小鼠模型中 i 期的存活率[1]。

NPD-2975 在小鼠中的药代动力学分析[1]

Route Dose (mg/kg) Tmax (h) Cmax (μM) T1/2 (h) AUC0-6 h (ng·h/mL) Cl (mL/min)
PO 50 1 5.25 3.46 6064.75 58.5
IP 10 13.18 1.06 3928.37 171

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

272.28

Formula

C14H13FN4O
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

NPD-2975 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.

Keywords:

NPD-29753032452-65-3NPD2975NPD 2975ParasiteInhibitorinhibitorinhibit

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