SLIGRL-NH2 TFA  (Synonyms: Protease-Activated Receptor-2 Activating Peptide TFA)

SLIGRL-NH2 TFA (Protease-Activated Receptor-2 Activating Peptide TFA) is an agonist of Protease-Activated Receptor-2 (PAR-2)^[1].

SLIGRL-NH2 is an agonist of PAR-2 and MrgprC11^[1]. SLIGRL-NH2 causes an L-NAME-inhibited relaxation. Based on SLIGRL-NH₂ causing a concentration-dependent relaxation with an EC₅₀ of 10 µM in endothelium-free preparations in the presence of perivascular adipose tissue (PVAT) , 20 µM is used as a suitable ‘test’ concentration of peptide in subsequent experiments designed to evaluate the effects of potential inhibitors of ADRF release/action. In the endothelium-free aorta preparations, SLIGRL-NH2 causes a concentration-dependent relaxation in preparations only in the presence of PVAT [+PVAT, -ENDO (endothelium)]^[2].

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

770.84

C₃₁H₅₇F₃N₁₀O₉

2828432-39-7

Ser-Leu-Ile-Gly-Arg-Leu-NH2

SLIGRL-NH2

OC[C@H](N)C(N[C@@H](CC(C)C)C(N[C@@H]([C@@H](C)CC)C(NCC(N[C@@H](CCCNC(N)=N)C(N[C@H](C(N)=O)CC(C)C)=O)=O)=O)=O)=O.OC(C(F)(F)F)=O

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• [1]. Akiyama T, et al. Behavioral model of itch, alloknesis, pain and allodynia in the lower hindlimb and correlativeresponses of lumbar dorsal horn neurons in the mouse. Neuroscience. 2014 Apr 25;266:38-46.  [Content Brief]

  [2]. Li Y, et al. Perivascular adipose tissue-derived relaxing factors: release by peptide agonists via proteinase-activated receptor-2 (PAR2) and non-PAR2 mechanisms. Br J Pharmacol. 2011 Dec;164(8):1990-2002.  [Content Brief]