Protease-Activated Receptor-2, amide

Name: Protease-Activated Receptor-2, amide
Brand: MedChemExpress
SKU: HY-P0283
Rating: 4.5 (2 reviews)

Cat. No.: HY-P0283 Purity: 99.33%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Protease-Activated Receptor-2, amide (SLIGKV-NH₂) is a highly potent protease-activated receptor-2 (PAR2) activating peptide.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

Protease-Activated Receptor-2, amide Chemical Structure

CAS No. : 190383-13-2

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in Water ready for reconstitution	USD 124	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in Water	USD 124	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 43	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 92	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 158	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 290	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 2 publication(s) in Google Scholar

2 Publications Citing Use of MCE Protease-Activated Receptor-2, amide

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity
Purity & Documentation
References
Customer Review

Description

Protease-Activated Receptor-2, amide (SLIGKV-NH₂) is a highly potent protease-activated receptor-2 (PAR2) activating peptide.

IC₅₀ & Target

PAR2^[1]

In Vitro

The PAR2-activating peptides used are: SLIGKV-OH, SLIGRL-OH, SLIGKV-NH₂, SLIGRL-NH₂. The synthetic agonist peptides mimicking the tethered ligand of PAR2, Ser-Leu-Ile-Gly-Lys-Val (SLIGKV-OH), Ser-Leu-Ile-Gly-Arg-Leu (SLIGRL-OH) and their amidated forms Ser-Leu-Ile-Gly-Lys-Val-amide (SLIGKV-NH₂) Ser-Leu-Ile-Gly-Arg-Leu-amide (SLIGRL-NH₂) have also been demonstrated being able to activate the receptor without enzymatic cleavage, therefore, have been utilised as biological tools to examine physiological functions of PAR2. Protease-Activated Receptor-2, amide is one of a four family subgroup of G-protein-coupled receptors (GPCRs), called PARs. Protease-activated receptors are distinguished from other GPCRs through their unique proteolytic mechanism of activation. For PAR2, activating proteases, such as trypsin, tryptase and coagulation factors VIIa and Xa, cleave a specific extracellular amino-terminal domain of the receptor to reveal a "tethered ligand", SLIGKV- and SLIGRL- for human and mouse/rat PAR2, respectively, which subsequently interacts with the activation domain of the receptor, initiating intracellular signaling pathways^[1]. The protease-activated receptor-2 (PAR2) has been implicated in the pathogenesis of several inflammatory and autoimmune disorders, and is expressed in a wide variety of human tissues and cells. PAR2 belongs to a family of seven transmembrane domain receptor proteins that are activated by proteolysis. Enzymatic digestion exposes an N-terminus ligand sequence that binds intramolecularly to the activation site on the extracellular loop II, initiating a G-protein-mediated cell-signalling cascade and nuclear factor-kappa B (NF-κB)-regulated gene transcription^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

614.78

Formula

C₂₈H₅₄N₈O₇

CAS No.

190383-13-2

Appearance

Solid

Color

White to off-white

Sequence

Ser-Leu-Ile-Gly-Lys-Val-NH2

Sequence Shortening

SLIGKV-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 : 33.33 mg/mL (54.21 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.6266 mL	8.1330 mL	16.2660 mL
5 mM	0.3253 mL	1.6266 mL	3.2532 mL
10 mM	0.1627 mL	0.8133 mL	1.6266 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

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: 100 mg/mL (162.66 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: 99.33%

Select Batch:

Data Sheet (273 KB) SDS (252 KB)

COA (246 KB) RP-HPLC (97 KB)

Handling Instructions (2659 KB)

References

[1]. Kanke T, et al. Binding of a highly potent protease-activated receptor-2 (PAR2) activating peptide, [3H]2-furoyl-LIGRL-NH2, to human PAR2. Br J Pharmacol. 2005 May;145(2):255-63. [Content Brief]

[2]. Ramelli G, et al. Protease-activated receptor 2 signalling promotes dendritic cell antigen transport and T-cellactivation in vivo. Immunology. 2010 Jan;129(1):20-7. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O	1 mM	1.6266 mL	8.1330 mL	16.2660 mL	40.6650 mL
	5 mM	0.3253 mL	1.6266 mL	3.2532 mL	8.1330 mL
	10 mM	0.1627 mL	0.8133 mL	1.6266 mL	4.0665 mL
	15 mM	0.1084 mL	0.5422 mL	1.0844 mL	2.7110 mL
	20 mM	0.0813 mL	0.4066 mL	0.8133 mL	2.0332 mL
	25 mM	0.0651 mL	0.3253 mL	0.6506 mL	1.6266 mL
	30 mM	0.0542 mL	0.2711 mL	0.5422 mL	1.3555 mL
	40 mM	0.0407 mL	0.2033 mL	0.4066 mL	1.0166 mL
	50 mM	0.0325 mL	0.1627 mL	0.3253 mL	0.8133 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.