2. GPCR/G Protein Immunology/Inflammation Apoptosis
  3. CCR TNF Receptor Interleukin Related
  4. RAGE406R

RAGE406R 是一种口服有效的 RAGE-DIAPH1 相互作用拮抗剂。RAGE406R 可与 ctRAGE 结合，阻止 RAGE-DIAPH1 复合物的形成，并抑制其相互作用。RAGE406R 可降低 THP1 细胞中 CCL2、TNF 和 IL-6 的表达。RAGE406R 可抑制 2 型糖尿病小鼠的迟发型超敏反应。RAGE406R 可用于糖尿病的研究。

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RAGE406R

RAGE406R Chemical Structure

CAS No. : 3034560-21-6

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RAGE406R 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RAGE406R is an orally active RAGE-DIAPH1 interaction antagonist. RAGE406R can bind to ctRAGE and prevent the formation of the RAGE-DIAPH1 complex and inhibit its interaction. RAGE406R can reduce the expression of CCL2, TNF, and IL-6 in THP1 cells. RAGE406R suppresses delayed-type hypersensitivity in T2D mice. RAGE406R can be used for the study of diabetes[1].

IC50 & Target[1]

IL-6

 

体外研究
(In Vitro)

RAGE406R (8.1 nM) 通过拮抗 ctRAGE 与 DIAPH1 之间的相互作用，抑制 ctRAGE 激活 DIAPH1 肌动蛋白聚合活性[1]。
RAGE406R (0.1-5.0 μM，1 小时) 呈剂量依赖性地降低 RAGE 和 DIAPH1 的细胞内接近程度。添加 0.1 μM RAGE406R 后，FRET 效率降至 4.7 %；在 5.0 μM 时，FRET 效率降至 1.6 %[1]。
RAGE406R (0.00006-10 μM，1.5 小时) 增强了 RAGE 配体刺激的平滑肌细胞 (SMC) 迁移的抑制作用，在小鼠主动脉 SMC 中的 IC50 为 2 nM[1]。
RAGE406R (10 μM，1.5 小时) 显著降低 THP1 细胞中 CCL2、TNF 和 IL-6 的表达[1]。

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

RAGE406R 相关抗体:

Cell Migration Assay [1]

Cell Line: Primary murine aortic SMCs
Concentration: 0.00006 μM, 0.0002 μM, 0.001 μM, 0.002 μM, 0.005 μM, 0.014 μM, 0.041 μM, 0.123 μM, 0.370 μM, 1.111 μM, 3.333 μM, 10 μM
Incubation Time: 1.5 h
Result: Increased the inhibition of RAGE ligand-stimulated SMC migration, with an IC50 of 2 nM in murine aortic SMCs.

Real Time qPCR[1]

Cell Line: THP1 cells
Concentration: 10 μM
Incubation Time: 1.5 h
Result: Significantly reduced the expression of CCL2, TNF, and IL6 in THP1 cells.
体内研究
(In Vivo)

RAGE406R (5 mg/kg，口服，每日两次，共 4 次) 可显著抑制 CF-1 小鼠体内 T 细胞介导的炎症反应[1]。
RAGE406R (5 mg/kg，局部涂抹，每日两次，连续 8 天) 可加速小鼠糖尿病伤口的愈合，且在雄性小鼠中具有更全面的抗炎作用[1]。

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

Animal Model: CF-1 mice were immunosensitized by injection of methylated bovine serum albumin (mBSA) (immunogen being mBSA + Freund's incomplete adjuvant emulsion) into the left inguinal lymph node. Three weeks later, an inflammatory response was elicited by injection of mBSA (20 μg) into the left hind paw pad[1].
Dosage: 5 mg/kg
Administration: P.o., twice daily (12-hour intervals) for a total of 4 doses
Result: Inflammation score significantly reduced.
Animal Model: Full-thickness 1 cm × 1 cm excisional wounds were created on the backs of male and female mouse models of T2D, ob/ob mice; wounds were covered with Tegaderm clear dressing[1].
Dosage: 5 mg/kg
Administration: Topical application, twice daily for 8 days
Result: Significantly promoted wound closure.
Inflammation was reduced, collagen deposition increased, and epithelial migration accelerated.
In male mice, the expression of Ccl2, TNF, and IL-6 was significantly reduced; in female mice, only Ccl2 expression was significantly decreased, while TNF and IL-6 showed no significant changes.
分子量

412.48

Formula

C25H24N4O2
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

RAGE406R 相关分类

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  • 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:

RAGE406R3034560-21-6CCRTNF ReceptorInterleukin RelatedCC chemokine receptorTumor Necrosis Factor ReceptorTNFRILActin PolymerizationDiabetesIntrinsically Disordered RegionsProtein-Protein InteractionsNMRMass SpectrometryCross-linkingReceptor for Advanced Glycation end productsmDia1DIAPH1Inhibitorinhibitorinhibit

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HY-178926
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