LIH383

£85.00 1mg

Atypical chemokine receptor (ACKR3) agonist.

LIH383 is a highly selective agonist of the atypical chemokine receptor, ACKR3 (formerly known as CXCR7). Functionally, ACKR3 is a scavenger receptor for a wide variety of opioid peptides, especially enkephalins and dynorphins, reducing their availability for the classical opioid receptors. LIH383 competes directly with CXCL12-AF647 for ACKR3 binding at low nanomolar concentrations and is more potent in inducing ?-arrestin recruitment to ACKR3 than the full-length chemokine ligands CXCL12 and CXCL11, with EC50 values of 1.2 nM and 2.2 nM respectively, and no effect on of any other opioid or chemokine receptor at concentrations up to 3 M. LIH383 can restrain the negative regulatory function of ACKR3 on opioid peptides and potentiate their activity in rat brain.

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SKU: PN-220 Categories: ,

Additional information

Three Letter Sequence

H-Phe-Gly-Gly-Phe-Met-Arg-Arg-Lys-NH2

Molecular Weight

997.23

Molecular Formula

C45H72N16O8S

Sequence

FGGFMRRK-NH2

Solubility

Soluble in water

Appearance

Freeze dried solid

Storage

Store desiccated, frozen and in the dark

Purity

>95% by HPLC

Modifications

Amide at C terminal lysine

Searchable Words

LIH383, pain, atypical chemokine receptor, ACKR3, CXCR7, opioid, PN-220, PN220