RAP-103 | CCR2 antagonist | Probechem Biochemicals

Chemical Structure : RAP-103

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RAP-103 (all-D-TTNYT)

货号: PC-21102Not For Human Use, Lab Use Only.

RAP-103 is an orally active, stabilized pentapeptide analog of DAPTA (D-ala-peptide T-amide), and multi-chemokine receptor antagonist.

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生物&药学活性

RAP-103 is an orally active, stabilized pentapeptide analog of DAPTA (D-ala-peptide T-amide), and multi-chemokine receptor antagonist.
RAP-103 inhibits chemokine ligands from binding to four specific chemokine receptors: CCR2, CCR5, CCR8, and CXCR4.
RAP-103 exhibits potent antagonism for both CCR2 (IC50 = 4.2 pM) and CCR5 (IC50 = 0.18 pM) in monocyte chemotaxis assays and CCR8 (IC50 = 7.7 fM).
RAP-103 attenuates behavioral hallmarks of neuropathic pain, such as mechanical allodynia and thermal hyperalgesia.
RAP-103 also downregulates corresponding molecular hallmarks of neuropathic pain such as phagocytosis, immune cell migration, and cell membrane ruffling.
RAP-103 inhibits opioid-derived respiratory depression, reduces opioid reinforcement and physical dependence, and normalizes opioid-induced dysregulation of mesolimbic chemokine receptors in rats.

物理化学性质&存储条件

分子量
分子式
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES

参考文献

1. Mami Noda, et al. Neurochem Int. 2018 Oct;119:184-189.

RAP-103 (all-D-TTNYT)

生物&药学活性

物理化学性质&存储条件

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RAP-103 (all-D-TTNYT)

生物&药学活性

物理化学性质&存储条件

参考文献

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