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| Targets |
PAR2
PAR2 (proteinase-activated receptor 2). 2-Furoyl-LIGRLO-amide is a potent and selective agonist of PAR2. It has a pD2 value of 7.0. By activating PAR2, it triggers downstream signaling pathways involved in inflammation, pain, and vascular responses. Its selectivity for PAR2 over other PAR subtypes makes it a useful tool for studying PAR2-specific functions. |
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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].
2-Furoyl-LIGRLO-amide is a potent and selective PAR2 agonist with a pD2 of 7.0. It causes dose-dependent relaxation of murine femoral arteries. This demonstrates its ability to activate PAR2-mediated vasodilatory responses. The compound's potent and selective activity makes it a valuable tool for studying PAR2 signaling in various tissues. |
| 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].
In vivo, 2-Furoyl-LIGRLO-amide would be expected to exert PAR2-mediated effects, including vasodilation, inflammation, and pain modulation. Its ability to cause relaxation of murine femoral arteries in vitro suggests potential vascular effects in vivo. Its effects in vivo would be assessed in animal models of inflammation, pain, and cardiovascular disease. |
| Enzyme Assay |
In vitro binding and functional assays are used to characterize 2-Furoyl-LIGRLO-amide as a PAR2 agonist. Functional assays measuring PAR2-mediated signaling, such as calcium mobilization or ERK phosphorylation, are performed using PAR2-expressing cells to determine its potency and confirm its agonistic activity, with a pD2 of 7.0.
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| Cell Assay |
Cellular assays for 2-Furoyl-LIGRLO-amide involve treating PAR2-expressing cells with the compound and measuring receptor activation. Functional readouts include intracellular calcium mobilization, a key downstream signal following PAR2 activation. These assays confirm the compound's agonistic activity and potency at PAR2.
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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. In vivo studies with 2-Furoyl-LIGRLO-amide would be performed in animal models to investigate PAR2 function. The compound could be administered via injection, and its effects on vascular tone, inflammation, and pain responses would be assessed. Its ability to cause relaxation of murine femoral arteries in vitro suggests potential vascular effects in vivo. |
| ADME/Pharmacokinetics |
2-Furoyl-LIGRLO-amide is a peptide with molecular formula C36H63N11O8 and molecular weight of 777.95. It is soluble in water (50 mg/mL). As a peptide agonist, its pharmacokinetic properties would be characteristic of this class, with potential for rapid degradation. The compound should be stored under recommended conditions.
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| Toxicity/Toxicokinetics |
No specific toxicity data is available for 2-Furoyl-LIGRLO-amide. As a PAR2 agonist, its safety profile would be an important consideration. Potential toxicities could be related to its effects on PAR2-mediated inflammation and pain signaling. Standard preclinical safety studies would be required to evaluate its safety for potential therapeutic applications.
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| References | |
| Additional Infomation |
2-Furoyl-LIGRLO-amide (CAS#: 729589-58-6) is a potent and selective PAR2 agonist with a pD2 of 7.0. It causes dose-dependent relaxation of murine femoral arteries. It has a molecular formula of C36H63N11O8 and a molecular weight of 777.95. It is a research tool for studying PAR2-mediated signaling in inflammation, pain, and vascular function.
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| Molecular Formula |
C36H63N11O8
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|---|---|
| Molecular Weight |
777.95
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| Exact Mass |
777.486
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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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| PubChem CID |
10395438
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.605
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| LogP |
1.17
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
26
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| Heavy Atom Count |
55
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| Complexity |
1310
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| Defined Atom Stereocenter Count |
6
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| SMILES |
CC[C@H](C)[C@@H](C(=O)NCC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(=O)N)NC(=O)[C@H](CC(C)C)NC(=O)C1=CC=CO1
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| InChi Key |
OSKIRYSKGDEIOG-WTWMNNMUSA-N
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| InChi Code |
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
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| Chemical Name |
N-[(2S)-1-[[(2S,3S)-1-[[2-[[(2S)-5-(diaminomethylideneamino)-1-[[(2S)-1-[[(2S)-1,5-diamino-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]furan-2-carboxamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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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.
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