GLPBio

SLIGKV-NH2

Catalog No.: GC14540Purity:>98.00%
SLIGKV-NH2 (SLIGKV-NH2) es un péptido activador del receptor 2 activado por proteasa (PAR2) muy potente.

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SLIGKV-NH2
Cas No.: 190383-13-2
10mM (in 1mL Water)In Stock
$86.00
1
1mgIn Stock
$25.00
1
5mgIn Stock
$49.00
1
10mgIn Stock
$84.00
1
25mgIn Stock
$154.00
1

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    618, 1017–1023 (2023)
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    610, 366–372 (2022)
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    Cell
    187(9):2288-2304 (2024)
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    183(7):1867-1883 (2020)
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    31, 1291–1307 (2021)

Descripción (Description)

SLIGKV-NH2 is a protease-activated receptor 2 (PAR2) agonist with an IC50 value of 10.1µM[1]. SLIGKV-NH2 effectively increases intracellular Ca2+ levels, with EC50 values of 109µM, 23.2µM, and 7.46µM in human umbilical vein endothelial cells (HUVECs), A549, and MDA-MB-231 cells, respectively[2]. SLIGKV-NH2 activates PAR2, thereby inducing a strong pro-inflammatory response, and increases the levels of IL-6, IL-8, GM-CSF, and TNF-α[3]. SLIGKV-NH2 has been widely used in immunological research to induce the release of histamine by colonic mast cells[4].

In vitro, SLIGKV-NH2 treatment (50µM) for 24 hours promoted the proliferation of HepG2 cells and enhanced the activity of the ERK/AP-1 pathway[5]. Incubation with 100µM SLIGKV-NH2 for 16 hours promoted the secretion of IL-6 by human T cells[6]. Treatment with 100µM SLIGKV-NH2 for 24 hours downregulated expression of involucrin in HaCaT keratinocytes[7].

In vivo, Intrathecal injection of SLIGKV-NH2 at a dose of 8µg induced thermal hyperalgesia and reduced paw withdrawal latency (PWL) in rats within 4 hours[8].

References:
[1] Maryanoff B E, Santulli R J, McComsey D F, et al. Protease-activated receptor-2 (PAR-2): structure-function study of receptor activation by diverse peptides related to tethered-ligand epitopes[J]. Archives of biochemistry and biophysics, 2001, 386(2): 195-204.
[2] Stahn S, Thelen L, Albrecht I M, et al. Teleocidin A2 inhibits human proteinase‐activated receptor 2 signaling in tumor cells[J]. Pharmacology Research & Perspectives, 2016, 4(4): e00230.
[3] Vesey D A, Suen J Y, Seow V, et al. PAR2-induced inflammatory responses in human kidney tubular epithelial cells[J]. American Journal of Physiology-Renal Physiology, 2013, 304(6): F737-F750.
[4] He S H, He Y S, Xie H. Activation of human colon mast cells through proteinase activated receptor-2[J]. World Journal of Gastroenterology, 2004, 10(3): 327.
[5] Xie L, Zheng Y, Li X, et al. Enhanced proliferation of human hepatoma cells by PAR-2 agonists via the ERK/AP-1 pathway[J]. Oncology Reports, 2012, 28(5): 1665-1672.
[6] Li T, He S. Induction of IL‐6 release from human T cells by PAR‐1 and PAR‐2 agonists[J]. Immunology and cell biology, 2006, 84(5): 461-466.
[7] Joo Y A, Chung H, Yoon S, et al. Skin barrier recovery by protease-activated receptor-2 antagonist lobaric acid[J]. Biomolecules & therapeutics, 2016, 24(5): 529.
[8] Mrozkova P, Spicarova D, Palecek J. Hypersensitivity induced by activation of spinal cord PAR2 receptors is partially mediated by TRPV1 receptors[J]. PLoS One, 2016, 11(10): e0163991.

Protocolo (Protocol)

Cell experiment [1]:

Cell lines

Human umbilical vein endothelial cells (HUVECs)

Preparation Method

HUVECs were cultured in an endothelial cell growth medium (ECGM) containing 12.5µg/ml ECGS, 100µg/ml heparin, 20% FBS, 1% GlutaMax-I, and 1% penicillin-streptomycin, at 37°C in an incubator with 5% CO2. Cells were then exposed to various concentrations of SLIGKV-NH2 (0.1, 1, 10, and 100µM) for 24h. Concentrations of IL-1α, IL-8, IL-10, IFN-γ, and IL-12 in the HUVEC culture supernatants were quantified.

Reaction Conditions

0.1, 1, 10, and 100µM; 24h

Applications

SLIGKV-NH2 treatment enhanced the levels of IL-1α, IL-8, IL-10, IFN-γ, and IL-12 in the HUVECs in a dose-dependent manner.
Animal experiment [2]:

Animal models

Male Wistar rats

Preparation Method

Male Wistar rats (6 weeks old) were housed in a temperature-controlled facility at 23±2°C with free access to food and water and maintained on a 12h light, 12h dark cycle, and were checked twice a day. Intrathecal drugs were applied and flushed (45 or 50μl) from the catheter with physiological solution: SLIGKV-NH2 (10μl; 8μg) and VKGILS-NH2 (10μl; 8μg). The PWL to thermal stimulation was tested using a plantar test apparatus with radiant heat applied to the plantar surface of each hindpaw within 4h.

Dosage form

8μg; once; i.t.

Applications

SLIGKV-NH2 decreased the PWL in response to a thermal stimulus in rats.

References:
[1] Niu Q X, Chen H Q, Chen Z Y, et al. Induction of inflammatory cytokine release from human umbilical vein endothelial cells by agonists of proteinase‐activated receptor‐2[J]. Clinical and Experimental Pharmacology and Physiology, 2008, 35(1): 89-96.
[2] Mrozkova P, Spicarova D, Palecek J. Hypersensitivity induced by activation of spinal cord PAR2 receptors is partially mediated by TRPV1 receptors[J]. PLoS One, 2016, 11(10): e0163991.

Documentos del producto (Product Documents)

Purity:>98.00%Appearance:A solid

Propiedades químicas (Chemical Properties)

N.º CAS
190383-13-2
Nombre químico
(2S)-6-amino-2-[[2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-4-methylpentanoyl]amino]-3-methylpentanoyl]amino]acetyl]amino]-N-[(2S)-1-amino-3-methyl-1-oxobutan-2-yl]hexanamide
SMILES
CCC(C)C(C(=O)NCC(=O)NC(CCCCN)C(=O)NC(C(C)C)C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CO)N
Fórmula molecular
C28H54N8O7
Peso molecular
614.78
Solubilidad
≥ 62.9 mg/mL in DMSO, ≥ 13.48 mg/mL in EtOH with ultrasonic and warming, ≥ 66.2 mg/mL in Water
Almacenamiento
Desiccate at -20°C
Consejos generales
Seleccione un disolvente adecuado según los datos de solubilidad del producto. Una vez preparada, divida la solución madre en alícuotas para evitar ciclos repetidos de congelación y descongelación.
Utilice las soluciones madre en un plazo de 6 meses si se conservan a -80°C, o de 1 mes si se conservan a -20°C.
Para mejorar la solubilidad, caliente el tubo a 37°C y soníquelo durante un periodo adecuado.
Condiciones de envío
Las muestras de evaluación se envían con acumuladores de frío. Los demás tamaños se envían a temperatura ambiente o, previa solicitud, con acumuladores de frío.

Calculadoras (Calculators)Molaridad / Dilución / Peso molecular / Conversión de unidades / Formulación in vivo / Solubilidad

g/mol

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