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RP-182

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Catalog No. TP3893Cas No. 1895883-60-9

RP-182 is a synthetic immunomodulatory peptide that exerts antitumor effects by targeting the mannose receptor CD206 on the surface of tumor-associated macrophages (TAM) with a binding affinity (Kd) of 8 μM. It induces a conformational change in the CD206 receptor, which activates NF-κB signaling and phagocytosis in TAM with high CD206 expression. RP-182 serves a dual function by activating the canonical NF-κB signaling pathway, leading to TNFα secretion and autocrine activation of TNF receptor 1 (TNFR1), which subsequently results in caspase 8 activation and apoptosis. This compound is studied in the contexts of pancreatic cancer and melanoma.

RP-182

RP-182

😃Good
Catalog No. TP3893Cas No. 1895883-60-9
RP-182 is a synthetic immunomodulatory peptide that exerts antitumor effects by targeting the mannose receptor CD206 on the surface of tumor-associated macrophages (TAM) with a binding affinity (Kd) of 8 μM. It induces a conformational change in the CD206 receptor, which activates NF-κB signaling and phagocytosis in TAM with high CD206 expression. RP-182 serves a dual function by activating the canonical NF-κB signaling pathway, leading to TNFα secretion and autocrine activation of TNF receptor 1 (TNFR1), which subsequently results in caspase 8 activation and apoptosis. This compound is studied in the contexts of pancreatic cancer and melanoma.
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Product Introduction

Bioactivity
Description
RP-182 is a synthetic immunomodulatory peptide that exerts antitumor effects by targeting the mannose receptor CD206 on the surface of tumor-associated macrophages (TAM) with a binding affinity (Kd) of 8 μM. It induces a conformational change in the CD206 receptor, which activates NF-κB signaling and phagocytosis in TAM with high CD206 expression. RP-182 serves a dual function by activating the canonical NF-κB signaling pathway, leading to TNFα secretion and autocrine activation of TNF receptor 1 (TNFR1), which subsequently results in caspase 8 activation and apoptosis. This compound is studied in the contexts of pancreatic cancer and melanoma.
In vitro
RP-182 is a compound that enhances its cytotoxic effect against CD206 high M2-like macrophages through the MyD88/NF-κB pathway, with an IC50 of 17.6 μM, when used in concentrations ranging from 1 nM to 1 mM over 48 hours. Additionally, at a concentration of 0.1 μM for 2 to 24 hours, RP-182 internalizes CD206, activates NF-κB, and increases IRF7 phosphorylation in M2 bone marrow-derived macrophages polarized with IL-4. Furthermore, RP-182 at concentrations of 3-30 μM for 24 hours raises the levels of inflammatory factors secreted by macrophages, indicating an immune reprogramming effect.
In vivo
Administered intraperitoneally at 20 mg/kg every other day for 2 weeks, RP-182 significantly inhibits tumor growth in B16 melanoma and KP16 pancreatic models while enhancing immunogenicity in mice. Moreover, a daily intraperitoneal injection of RP-182 at 20 mg/kg over 18 days markedly alleviates pulmonary fibrosis in mice.
Chemical Properties
Molecular Weight1374.68
FormulaC69H103N19O11
Cas No.1895883-60-9
Smiles[C@@H](CC1=CC=CC=C1)(NC([C@@H](NC([C@@H](NC([C@H](CC2=CC=CC=C2)NC([C@@H](NC([C@@H](NC([C@@H](NC([C@H](CC3=CC=CC=C3)NC([C@H](CCCCN)N)=O)=O)CCCNC(=N)N)=O)CCCCN)=O)C)=O)=O)CCCCN)=O)CCCNC(=N)N)=O)C(N[C@@H](CC4=CC=CC=C4)C(O)=O)=O
Storage & Solubility Information
Storagekeep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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