Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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Targets |
PAR2
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ln Vitro |
In cultured human and rat cells, 2-Furoyl-LIGRLO-amide (2-Furoyl-LIGRLO-NH2) enhances PAR2-expressing cells [1]. Two to three hundred times more potent than SLIGRL-NH2 is 2-Furoyl-LIGRLO-amide (2-Furoyl-LIGRLO-NH2) in bioassays of tissue PAR2 activity, as determined by arterial vasodilation and hyperpolarization. 2-Furoyl-LIGRLO-amide does not significantly cause non-PAR2-mediated contraction of mouse femoral arteries, in contrast to trans-cinnamoyl-LIGRLO-NH2 [1].
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ln Vivo |
When given intradermally in the nape of the neck at a dose of 10 μg prior to the reaction, Furoyl-LIGRLO-amide (but not histamine) causes less scratches in Trpv3-/-mice. However, it dramatically decreased the quantity of scratches in WT mice[1].
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Animal Protocol |
Animal/Disease Models: Adult male (2/3-month-old) Trpv3-/- and WT mice[3]
Doses: 10 μg Route of Administration: Injected intradermally at the nape of the neck Experimental Results: Was involved in PAR2- induced acute itch. |
References |
[1]. McGuire JJ, et al. 2-furoyl-LIGRLO-amide: a potent and selective proteinase-activated receptor 2 agonist. J Pharmacol Exp Ther. 2004 Jun;309(3):1124-31.
[2]. Lohman RJ, et al. An antagonist of human protease activated receptor-2 attenuates PAR2 signaling, macrophage activation, mast cell degranulation, and collagen-induced arthritis in rats. FASEB J. 2012 Jul;26(7):2877-87. [3]. Jiahui Zhao, et al. PAR2 Mediates Itch via TRPV3 Signaling in Keratinocytes. J Invest Dermatol |
Molecular Formula |
C36H63N11O8
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Molecular Weight |
777.95
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CAS # |
729589-58-6
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Related CAS # |
2-Furoyl-LIGRLO-amide TFA;2468029-34-5
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SMILES |
CC[C@@H]([C@H](NC([C@@H](NC(C1=CC=CO1)=O)CC(C)C)=O)C(NCC(N[C@H](C(N[C@H](C(N[C@H](C(N)=O)CCCN)=O)CC(C)C)=O)CCCNC(N)=N)=O)=O)C
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Solubility (In Vitro) |
H2O: 50 mg/mL (64.27 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (64.27 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
 (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.2854 mL | 6.4271 mL | 12.8543 mL | |
5 mM | 0.2571 mL | 1.2854 mL | 2.5709 mL | |
10 mM | 0.1285 mL | 0.6427 mL | 1.2854 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.