2. Anti-infection
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  4. Ro 13-3978

Ro 13-3978 是一种具有口服活性的抗血吸虫剂。Ro 13-3978 对幼年和成年曼氏血吸虫感染具有优异的体内抗血吸虫活性。Ro 13-3978 在体内对 E. caproni 和 F. hepatica 无活性。Ro 13-3978 可阻断双氢睾酮诱导的雄激素依赖型细胞增殖，在。Ro 13-3978 可用于血吸虫病的相关研究。

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Ro 13-3978

Ro 13-3978 Chemical Structure

CAS No. : 70842-04-5

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Ro 13-3978 相关抗体

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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

Ro 13-3978 is an orally active antischistosomal agent. Ro 13-3978 exhibits excellent in vivo antischistosomal activity against juvenile and adult Schistosoma mansoni infections. Ro 13-3978 shows no in vivo activity against E. caproni and F. hepatica. Ro 13-3978 blocks dihydrotestosterone-induced proliferation of androgen-dependent cells. Ro 13-3978 can be used in research related to schistosomiasis[1][2].

IC50 & Target[1]

Schistosome

 

体外研究
(In Vitro)

Ro 13-3978 (100 μg/mL; 72 h) 可在体外适度降低新生转化的 S. mansoni 血吸虫童虫的运动能力，且不会造成体被损伤[1]。
Ro 13-3978 (0.12-90 μM; 70 h) 在孵育 70 h 后，对大鼠骨骼肌成肌细胞 L6 的最高浓度达 90 μM 时仍无细胞毒性，其 IC50 大于 90 μM[1]。
Ro 13-3978 (25-100 μg/mL; 72 h) 会在体外实验中使成年曼氏血吸虫 (S. mansoni) 虫体出现轻微的体被变化，包括雄虫体被皱缩以及部分雌虫体被脱落[1]。

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

Ro 13-3978 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Cmax AUC0-last
Mice[2] 100 mg/kg p.o. 124 μM 2740 μM·h
体内研究
(In Vivo)

Ro 13-3978 (12.5-200 mg/kg；口服；单次) 在 NMRI 小鼠中表现出剂量依赖性的抗血吸虫活性，其针对成年 S. mansoni 的 ED50 为 14.6 mg/kg，针对幼年 S. mansoni 的 ED50 为 138.9 mg/kg[1]。
Ro 13-3978 (100 mg/kg；口服；单次) 在 NMRI 小鼠中表现出阶段特异性抗血吸虫活性：对感染后 22 天及以后的曼氏血吸虫 (S. mansoni) 具有高疗效 (总虫体减少率 64.3-94.6%)，对 7-14 日龄的虫体无活性，而在感染前给药时仅具有中等效果[1]。

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

Animal Model: NMRI mice (female, weight ~20-22 g, orally infected with Schistosoma mansoni cercariae)[1]
Dosage: 12.5-100 mg/kg (adult infections); 50-200 mg/kg (juvenile infections)
Administration: p.o.; single dose
Result: Reduced total adult S.
mansoni worm burden by 37.1%, 82.6%, 78.2%, and 94.6% at 12.5 mg/kg, 25 mg/kg, 50 mg/kg, and 100 mg/kg respectively.
Reduced female adult S.
mansoni worm burden by 33.8%, 84.5%, 57.3%, and 88.0% at 12.5 mg/kg, 25 mg/kg, 50 mg/kg, and 100 mg/kg respectively.
Calculated an ED50 of 14.6 mg/kg for 49 day-old S. mansoni infections.
Reduced total juvenile S.
mansoni worm burden by 0%, 63.8%, and 88.1% at 50 mg/kg, 100 mg/kg, and 200 mg/kg respectively.
Reduced female juvenile S.
mansoni worm burden by 0%, 57.3%, and 85.4% at 50 mg/kg, 100 mg/kg, and 200 mg/kg respectively.
Calculated an ED50 of 138.9 mg/kg for 22 day-old S. mansoni infections.
分子量

290.22

Formula

C12H10F4N2O2
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

Ro 13-3978 相关分类

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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:

Ro 13-397870842-04-5Parasiteschistosomiasisandrogen receptormouse liver S9 fractionsLAPC4 cellsNMRI micerat skeletal myoblast cellsdihydrotestosteroneandrogen-dependent cellshuman liver S9 fractionsSchistosoma mansoniInhibitorinhibitorinhibit

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