Description
2-Furoyl-LIGRLO-amide is a potent and selective proteinase-activated receptor 2 (PAR2) agonist with a pD2 value of 7.0..
Product information
CAS Number: 729589-58-6
Molecular Weight: 777.95
Formula: C36H63N11O8
Chemical Name: (Z,2S,3S)-N-{[(Z)-[(1S)-1-[(Z)-[(1S)-1-[(Z)-[(1S)-4-amino-1-(C-hydroxycarbonimidoyl)butyl]-C-hydroxycarbonimidoyl]-3-methylbutyl]-C-hydroxycarbonimidoyl]-4-carbamimidamidobutyl]-C-hydroxycarbonimidoyl]methyl}-2-[(Z)-[(2S)-2-[(furan-2-yl)formamido]-1-hydroxy-4-methylpentylidene]amino]-3-methylpentanimidic acid
Smiles: C[C@@H](CC)[C@H](/N=C(\O)/[C@H](CC(C)C)NC(=O)C1=CC=CO1)/C(/O)=N/C/C(/O)=N/[C@@H](CCCNC(N)=N)/C(/O)=N/[C@@H](CC(C)C)/C(/O)=N/[C@@H](CCCN)C(=N)O
InChiKey: OSKIRYSKGDEIOG-WTWMNNMUSA-N
InChi: InChI=1S/C36H63N11O8/c1-7-22(6)29(47-33(52)26(18-21(4)5)46-34(53)27-13-10-16-55-27)35(54)42-19-28(48)43-24(12-9-15-41-36(39)40)31(50)45-25(17-20(2)3)32(51)44-23(30(38)49)11-8-14-37/h10,13,16,20-26,29H,7-9,11-12,14-15,17-19,37H2,1-6H3,(H2,38,49)(H,42,54)(H,43,48)(H,44,51)(H,45,50)(H,46,53)(H,47,52)(H4,39,40,41)/t22-,23-,24-,25-,26-,29-/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
2-Furoyl-LIGRLO-amide (2-Furoyl-LIGRLO-NH2) is equally effective to and 10 to 25 times more potent than SLIGRLNH2 for increasing intracellular calcium in cultured human and rat PAR2-expressing cells, respectively. In bioassays of tissue PAR2 activity, measured as arterial vasodilation and hyperpolarization, 2-Furoyl-LIGRLO-amide (2-Furoyl-LIGRLO-NH2) is 10 to 300 times more potent than SLIGRL-NH2. Unlike trans-cinnamoyl-LIGRLO-NH2, 2-Furoyl-LIGRLO-amide do not cause a prominent non-PAR2-mediated contraction of murine femoral arteries.
In Vivo:
Furoyl-LIGRLO-amide (injected intradermally at the nape of the neck; 10 μg; pre-injected) exhibits fewer scratches in response to 2-Furoyl-LIGRLO-amide but not to histamine in Trpv3-/- mice. But it decreases significantly the number of scratches in WT mice.
Products are for research use only. Not for human use.
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