Chemical Structure : RAP-103
Catalog No.: 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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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.
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Appearance | Solid | |
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Solubility |
10 mM in DMSO |
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