1. Apoptosis
  2. Apoptosis TNF Receptor
  3. RP-832c

RP-832c 是一种宿主防御肽 (HDP) 的合成类似物,靶向 M2 极化巨噬细胞表面的甘露糖受体 CD206 (Kd = 3.5 μM)。RP-832c 结合 CD206 后会引起受体构象的显著变化,激活信号通路,导致 CD206 阳性 M2 巨噬细胞快速凋亡 (apoptosis),并重新极化为 M1 表型。RP-832c 处理可显著降低 M2 巨噬细胞中 CD206 基因表达,同时暂时性增加 M1 巨噬细胞标志物 TNF-α 的表达。RP-832c 可用于研究 T 细胞淋巴瘤 (CTCL) 和特发性肺纤维化 (IPF)。

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RP-832c

RP-832c Chemical Structure

CAS No. : 2375823-45-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RP-832c is a synthetic analogue of host defense peptides (HDP), targeting the mannose receptor CD206 on the surface of M2 polarized macrophages (Kd = 3.5 μM). RP-832c binding to CD206 induces a significant conformational change in the receptor, activating signaling pathways that lead to rapid apoptosis and repolarization of CD206-positive M2 macrophages to an M1 phenotype. RP-832c treatment significantly reduces CD206 gene expression in M2 macrophages while transiently increasing expression of TNF-α, a marker for M1 macrophages. RP-832c is used for the studies of T-cell lymphoma (CTCL) and idiopathic pulmonary fibrosis (IPF)[1][2].

体外研究
(In Vitro)

RP-832c (0-100 μM) 对 M2 极化的骨髓来源巨噬细胞 (BMDM) 表现出剂量依赖性抑制,IC50 值为 6.184 μM,对 M1 极化的巨噬细胞产生极小的细胞毒性,并且对两种不同的人胎儿肺成纤维细胞系 MRC5 和 IMR9 无细胞毒性[2]
RP-832c (10 μM, 24 h) 显著降低 M2 巨噬细胞中 CD206 的表达,并短暂增加 TNF-α 的表达[2]

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

RT-PCR[2]

Cell Line: M2 macrophages
Concentration: 10 μM
Incubation Time: 0, 2, 8 and 24 h
Result: Decreased CD206 gene expression.
Resulted in an initial increase in TNF-α gene expression.
体内研究
(In Vivo)

RP-832c (腹腔注射,每日一次,持续 10 天) 在皮肤 T 细胞淋巴瘤肿瘤微环境中通过促使免疫抑制的 M2 型巨噬细胞向抗肿瘤的 M1 型巨噬细胞转变来抑制肿瘤生长[1]
RP-832c (5-10 mg/kg,皮下注射,每日一次,持续 21 天) 在肺纤维化小鼠模型中显示出显著的预防和治疗效果[2]

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

Animal Model: Bleomycin (HY-108345) induced lung fibrosis model models established in 6-8-week-old C57BL/6 mice[2]
Dosage: 5 and 10 mg/kg for prevention group and 10 mg/kg for treatment group
Administration: Subcutaneous injection (s.c.), once daily for 21 days
Result: significantly reduced collagen deposition in a dose-dependent manner with the alveolar structure well-preserved and the degree of fibrosis mild in prevention group.
Significantly reduces the degree of already formed fibrosis , reduced TNF-α, IL-6, IL-10, IFN-γ, CXCL1/2, etc and the expression of TGF-β1 and MMP-13 in treatment group.
Observed no significant toxicity at a dose of up to 50 mg/kg.
分子量

1367.60

Formula

C68H94N20O11

CAS 号
Sequence

Arg-Trp-Lys-Phe-Gly-Gly-Phe-Lys-Trp-Arg

Sequence Shortening

RWKFGGFKWR

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
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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.

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产品名称:
RP-832c
目录号:
HY-P11107
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