2-Furoyl-LIGRLO-amide
Based on 3 publication(s) in Google Scholar
2-Furoyl-LIGRLO-amide is a potent and selective proteinase-activated receptor 2 (PAR2) agonist with a pD2 value of 7.0..
For research use only. We do not sell to patients.
- Purity: 99.59%
- CAS No.: 729589-58-6
- Formula: C36H63N11O8
- Molecular Weight:777.95
-
Storage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
HY-P1308
SLIGRL-NH2
-
HY-P0283
Protease-Activated Receptor-2, amide
-
HY-14350
AC-55541
-
HY-112558
AZ3451
-
HY-P0078
TRAP-6
-
HY-15142
Doxorubicin hydrochloride
-
HY-100558
Bafilomycin A1
-
HY-18739
Phorbol 12-myristate 13-acetate
-
HY-A0281
4-Phenylbutyric acid
-
HY-10820
Pemetrexed
-
HY-P0226
TFLLR-NH2
-
HY-10219
Rapamycin
Publications Citing Use of MedChemExpress (MCE) 2-Furoyl-LIGRLO-amide
More
Biological Activity
|
PAR2 |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
0.43 μM
Compound: 1; 2f-LIGRLO-NH2
|
Agonist activity at PK1-tagged PAR2 (unknown origin) expressed in HEK293 cells assessed as induction of beta-arrestin recruitment incubated for 90 mins by Pathhunter chemiluminescent assay
Agonist activity at PK1-tagged PAR2 (unknown origin) expressed in HEK293 cells assessed as induction of beta-arrestin recruitment incubated for 90 mins by Pathhunter chemiluminescent assay
|
[PMID: 32551018] |
| HEK-293T | EC50 |
0.15 μM
Compound: 1; 2f-LIGRLO-NH2
|
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
|
[PMID: 32551018] |
| HT-29 | EC50 |
0.2 μM
Compound: 2
|
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
|
[PMID: 23895492] |
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[1].
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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Adult male (2/3-month-old) Trpv3-/- and WT mice[3]
-
Dosage:10 μg
-
Administration:Injected intradermally at the nape of the neck
-
Result:Was involved in PAR2- induced acute itch.
Chemical Information
-
CAS No. 729589-58-6
-
Appearance Solid
-
Molecular Weight 777.95
-
Formula C36H63N11O8
-
Color White to off-white
-
Sequence
{Fur-2-oyl}-Leu-Ile-Gly-Arg-Leu-{Orn}-NH2
-
Sequence Shortening
{Fur-2-oyl}-LIGRL-{Orn}-NH2
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (3)
-
Journal Impact Factor
-
Most Recent
-
Pharmacol Res
PAR2 deficiency impairs antitumor immunity and attenuates anti-PD1 efficacy in colorectal cancer. [Abstract]2025 May:215:107721. PMID: 40174816 -
J Immunother Cancer
Targeting PAR-2 with a negative allosteric modulator increases tumor antigen presentation and potentiates anti-PD-1 immunotherapy. [Abstract]2026 Apr 3;14(4):e013507. PMID: 41932811 -
PLoS Negl Trop Dis
A novel trypsin of Trichinella spiralis mediates larval invasion of gut epithelium via binding to PAR2 and activating ERK1/2 pathway. [Abstract]2024 Jan 2;18(1):e0011874. PMID: 38166153
Solvent & Solubility
H2O : 50 mg/mL (64.27 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (64.27 mM); Clear solution; Need ultrasonic
Purity & Documentation
-
Data Sheet (275 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[3]. Jiahui Zhao, et al. PAR2 Mediates Itch via TRPV3 Signaling in Keratinocytes. J Invest Dermatol [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 1.2854 mL | 6.4271 mL | 12.8543 mL | 32.1357 mL |
| 5 mM | 0.2571 mL | 1.2854 mL | 2.5709 mL | 6.4271 mL | |
| 10 mM | 0.1285 mL | 0.6427 mL | 1.2854 mL | 3.2136 mL | |
| 15 mM | 0.0857 mL | 0.4285 mL | 0.8570 mL | 2.1424 mL | |
| 20 mM | 0.0643 mL | 0.3214 mL | 0.6427 mL | 1.6068 mL | |
| 25 mM | 0.0514 mL | 0.2571 mL | 0.5142 mL | 1.2854 mL | |
| 30 mM | 0.0428 mL | 0.2142 mL | 0.4285 mL | 1.0712 mL | |
| 40 mM | 0.0321 mL | 0.1607 mL | 0.3214 mL | 0.8034 mL | |
| 50 mM | 0.0257 mL | 0.1285 mL | 0.2571 mL | 0.6427 mL | |
| 60 mM | 0.0214 mL | 0.1071 mL | 0.2142 mL | 0.5356 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
2-Furoyl-LIGRLO-amide Related Classifications
HY-P1314 Related Classifications
Powered by Bioz