2. Metabolic Enzyme/Protease
  3. Cathepsin
  4. RO5461111

RO5461111 是一种高特异性、口服有效的 Cathepsin S 拮抗剂 (IC50: 0.4 nM, human Cathepsin S; 0.5 nM, murine Cathepsin S)。RO5461111 能够有效抑制抗原特异性 T 细胞和 B 细胞活化。RO5461111 对肺部炎症和狼疮性肾炎有改善作用。

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RO5461111

RO5461111 Chemical Structure

CAS No. : 1252637-46-9

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1 mg ￥2200
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5 mg ￥5480
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RO5461111 相关抗体

Top Publications Citing Use of Products

查看 Cathepsin 亚型特异性产品:

查看所有亚型
Cathepsin B Cathepsin C Cathepsin D Cathepsin E Cathepsin K Cathepsin L Cathepsin S

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RO5461111 a highly specific and orally active antagonist of Cathepsin S with IC50s of 0.4 nM (human Cathepsin S) and 0.5 nM (murine Cathepsin S), respectively. RO5461111 can effectively inhibit the activation of antigen-specific T cells and B cells. RO5461111 can improve pulmonary inflammation and lupus nephritis[1][2].

IC50 & Target[1]

human Cathepsin S

0.4 nM (IC50)

murine Cathepsin S

0.5 nM (IC50)

体外研究
(In Vitro)

RO5461111 (16 h) 在 人 (RAJI) 或鼠 (A20) 细胞系中具有细胞活性，显著降低了脾脏树突状细胞的活化以及随后 CD4 T 细胞和 CD4/CD8 双阴性 T 细胞的扩增和活化[1]。

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

RO5461111 相关抗体:
体内研究
(In Vivo)

RO5461111 (0.1-100 mg/kg; 口服; 单剂量) 可抑制 BALB/c 小鼠接种绵羊 IgG 后 T 细胞启动和抗绵羊 IgG[1]。
RO5461111 (1.31 mg/mouse 或 30 mg/kg; 口服; 8 周) 破坏 MRL-Fas(lpr) 小鼠的生发中心 (如降低 CXCL12 表达)，减少高丙种球蛋白血症和狼疮自身抗体产物 F。RO5461111 还可以减轻肺部炎症，改善狼疮性肾炎[1]。

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

Animal Model: Female MRL-Fas(lpr) mice (12-week-old; with proteinuria/serum creatinine levels up)[1]
Dosage: 262.5 mg/kg chow; or 5 mg/mouse with 1.31 mg/mouse
Administration: Oral gavage; 8 weeks
Result: Reduced the activation and expansion of spleen dendritic cells, CD4, double-negative T cells and plasma cells.
Reduced plasma levels of IL-10 and TNF-α.
分子量

614.56

Formula

C27H24F6N4O4S
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

纯度 & 产品资料
参考文献

RO5461111 相关分类

  • 摩尔计算器

  • 稀释计算器

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

质量   浓度   体积   分子量 *
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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)
× = ×
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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:

RO54611111252637-46-9RO 5461111RO-5461111CathepsinInhibitorinhibitorinhibit

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产品名称：
RO5461111
目录号：
HY-114374
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