2. Anti-infection Metabolic Enzyme/Protease
  3. Parasite Cytochrome P450
  4. DNDI-VL-2098

DNDI-VL-2098 是一种口服有效的抗利什曼原虫试剂。DNDI-VL-2098 具有高渗透性、体外代谢稳定性以及对 CYP2C19 的选择性抑制 (IC50=0.47 μM)。DNDI-VL-2098 在高达 12.5 μM 浓度下不影响其他主要 CYP 酶 (CYP1A2、CYP2C9、CYP2D6 和 CYP3A4) 活性。其在小鼠、仓鼠、大鼠和犬等多种动物模型中均展现出良好的药代动力学性质。DNDI-VL-2098 存在中高水平血浆蛋白结合的特点，可用于内脏利什曼病的研究。

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DNDI-VL-2098

DNDI-VL-2098 Chemical Structure

CAS No. : 681492-17-1

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DNDI-VL-2098 相关抗体

Top Publications Citing Use of Products

查看 Parasite 亚型特异性产品:

查看所有亚型
Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

查看 Cytochrome P450 亚型特异性产品:

查看所有亚型
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DNDI-VL-2098 is an orally active antileishmanial agent. DNDI-VL-2098 exhibits high permeability, in vitro metabolic stability, and selective inhibition of CYP2C19 (IC50=0.47 μM). DNDI-VL-2098 does not affect the activities of other major CYP enzymes (CYP1A2, CYP2C9, CYP2D6 and CYP3A4) at concentrations up to 12.5 μM. It shows favorable pharmacokinetic properties in multiple animal models including mice, hamsters, rats and dogs. DNDI-VL-2098 is characterized by moderate to high plasma protein binding and can be used for the research of visceral leishmaniasis[1].

IC50 & Target

Leishmania

 

CYP2C19

0.47 μM (IC50)

体外研究
(In Vitro)

DNDI-VL-2098 (0.3-30 μg/mL; 4 h) 在小鼠、大鼠、犬和人源样本中表现出中等到高度的血浆蛋白结合率 (94-98%)，游离分数为 3-6%[1]。
DNDI-VL-2098 在巨噬细胞无鞭毛体模型中具有强效活性，针对锑抗性 Leishmania donovani DD8 株的 IC50 为 0.025 μM，针对非洲临床分离株的 IC50 为 0.7-2.6 μM[1]。

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

DNDI-VL-2098 相关抗体:

Cell Viability AssayWestern Blot AnalysisCell Proliferation AssayApoptosis AnalysisCell Cytotoxicity AssayCell Cycle AnalysisRT-PCRCell Autophagy AssayImmunofluorescenceCell Differentiation AssayCell Invasion AssayCell Migration Assay Real Time qPCRELISA Assay[1]

Cell Line: Macrophage amastigote model
Concentration: IC50 assay
Incubation Time: 24-48 h
Result: Against the antimony-resistant Leishmania donovani DD8 strain with an IC50 of 0.025 μM, and against African clinical strains with IC50 values of 0.7-2.6 μM.
药代动力学
(Parmacokinetics)
Species Dose Route C0 AUClast CLblood Vss T1/2 Tmax Cmax Bioavailability
Golden hamster[1] 1 mg/kg i.v. 1.14 μg/mL 0.63 μg·h/mL 25.98 mL/min/kg 2.00 L/kg 1.19 h / / /
Golden hamster[1] 6.25 mg/kg p.o. / 4.49 μg·h/mL / / / 0.25 h 1.17 μg/mL 115 %
Golden hamster[1] 12.5 mg/kg p.o. / 17.13 μg·h/mL / / / 0.50 h 2.36 μg/mL /
Golden hamster[1] 25 mg/kg p.o. / 29.80 μg·h/mL / / / 4.00 h 3.13 μg/mL /
Golden hamster[1] 50 mg/kg p.o. / 53.00 μg·h/mL / / / 4.00 h 4.93 μg/mL /
Mice[1] 1 mg/kg i.v. 0.74 μg/mL 1.65 μg·h/mL 9.37 mL/min/kg 1.98 L/kg 2.94 h / / /
Mice[1] 6.25 mg/kg p.o. / 13.10 μg·h/mL / / / 2.00 h 1.08 μg/mL 127 %
Mice[1] 12.5 mg/kg p.o. / 29.76 μg·h/mL / / / 4.00 h 2.43 μg/mL /
Mice[1] 25 mg/kg p.o. / 77.23 μg·h/mL / / / 4.00 h 5.39 μg/mL /
Mice[1] 50 mg/kg p.o. / 145.08 μg·h/mL / / / 6.00 h 8.39 μg/mL /
Rat[1] 1 mg/kg i.v. 0.56 μg/mL 1.84 μg·h/mL 8.18 mL/min/kg 2.24 L/kg 3.44 h / / /
Rat[1] 5 mg/kg p.o. / 10.96 μg·h/mL / / / 1.81 h 0.86 μg/mL 119 %
Rat[1] 5 mg/kg p.o. / 6.64 μg·h/mL / / / 4.50 h 0.57 μg/mL 72 %
Rat[1] 50 mg/kg p.o. / 76.22 μg·h/mL / / / 5.00 h 7.13 μg/mL /
Rat[1] 100 mg/kg p.o. / 187.14 μg·h/mL / / / 6.50 h 9.99 μg/mL /
Rat[1] 200 mg/kg p.o. / 351.77 μg·h/mL / / / 7.50 h 12.75 μg/mL /
体内研究
(In Vivo)

DNDI-VL-2098 (50 mg/kg；口服；每日 1 次；连续 5 天) 在内脏利什曼病急性小鼠模型中实现了超过 99% 的寄生虫抑制率[1]。
DNDI-VL-2098 (25 mg/kg) 在慢性内脏利什曼病仓鼠模型中可实现超过 85% 的寄生虫抑制率，效力优于其外消旋体和 (S)-对映体[1]。

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

Animal Model: Swiss Albino mice with Visceral Leishmaniasis[1]
Dosage: 50 mg/kg
Administration: once daily; 5 days; p.o.
Result: Achieved greater than 99% parasite inhibition.
分子量

359.26

Formula

C14H12F3N3O5
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-VL-2098 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

DNDI-VL-2098681492-17-1ParasiteCytochrome P450CYPsliver microsomesCYP1A2CYP2C9Caco-2 cell monolayersLeishmania donovani DD8 strainCYP2C19visceral leishmaniasisCYP3A4hepatocytesCYP2D6Inhibitorinhibitorinhibit

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