2-Furoyl-LIGRLO-amide

Name: 2-Furoyl-LIGRLO-amide
Brand: MedChemExpress
SKU: HY-P1314
Rating: 4.5 (1 reviews)

Cat. No.: HY-P1314 Purity: 99.87%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

Custom Peptide Synthesis

2-Furoyl-LIGRLO-amide Chemical Structure

CAS No. : 729589-58-6

Size	Price	Stock	Quantity
1 mg	USD 105	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 314	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 534	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of 2-Furoyl-LIGRLO-amide:

2-Furoyl-LIGRLO-amide TFA Get quote

1 Publications Citing Use of MCE 2-Furoyl-LIGRLO-amide

•PLoS Negl Trop Dis. 2024 Jan 2;18(1):e0011874. [Abstract]

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Protease Activated Receptor (PAR) Isoform Specific Products:

View All Isoforms

PAR1 PAR2 PAR4

Biological Activity
Purity & Documentation
References
Customer Review

Description

2-Furoyl-LIGRLO-amide is a potent and selective proteinase-activated receptor 2 (PAR2) agonist with a pD₂ value of 7.0^[1]^[2]..

IC₅₀ & Target

PAR2

Cellular Effect

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]

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^[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.

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^[1].

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.

Molecular Weight

777.95

Formula

C₃₆H₆₃N₁₁O₈

CAS No.

729589-58-6

Appearance

Solid

Color

White to off-white

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)

Solvent & Solubility

In Vitro:

H₂O : 50 mg/mL (64.27 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the 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.

* 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

Add each solvent one by one: PBS
Solubility: 50 mg/mL (64.27 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.87%

Select Batch:

Data Sheet (275 KB) SDS (252 KB)

COA (248 KB) LCMS (119 KB) Elemental Analysis Report (107 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

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.