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Endothelin 1 swine, human

Catalog No.GC30485

Endotelina 1 porcina, humana es un péptido sintético con la secuencia de Endotelina 1 humana y porcina, que es un potente vasoconstrictor endógeno.

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Endothelin 1 swine, human Chemical Structure

Cas No.: 117399-94-7

Tamaño Precio Disponibilidad Cantidad
500μg
125,00 $
Disponible
1mg
220,00 $
Disponible
5mg
883,00 $
Disponible
10mg
1.471,00 $
Disponible

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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

Immortalized mouse podocytes

Preparation Method

Immortalized mouse podocytes were incubated with RPMI 1640 medium alone or with 100 nM Endothelin 1 (swine, human) for 5, 15, or 30 minutes.

Reaction Conditions

100 nM for 5, 15, 30 minutes, 16, 24 hours.

Applications

Endothelin 1 (swine, human) reduced synaptopodin and increased a-SMA expression at 6 hours and even more so at 24 hours

Animal experiment [2]:

Animal models

Male severe combined immunodeficiency (SCID) mice

Preparation Method

The mice were inoculated with PPC-1 (4×105 cells/25 µl/paw) subcutaneously in the left paw using a microsyringe. After acclimation, 10 µl of vehicle alone or vehicle with Endothelin 1 (swine, human) (10 pmol/paw) or sarafotoxin S6c was subcutaneously injected into the left hind paw.

Dosage form

10 pmol/paw, s.c.

Applications

Endothelin 1 (swine, human) (10 pmol/paw) induced pain responses in the sham-operated animals and potentiated responses in the PPC-1 inoculated animals

References:

[1]: Buelli S, RosanÒ L, Gagliardini E, et al. β-Arrestin-1 drives endothelin-1-mediated podocyte activation and sustains renal injury[J]. Journal of the American Society of Nephrology, 2014, 25(3): 523-533.
[2]: Yuyama H, Koakutsu A, Fujiyasu N, et al. Effects of selective endothelin ETA receptor antagonists on endothelin-1-induced potentiation of cancer pain[J]. European journal of pharmacology, 2004, 492(2-3): 177-182.

Background

Endotelina 1 (cerdo, humano) es un péptido vasoconstrictor de 21aa y agonista de los receptores ETA y ETB de la endotelina (IC50s = 0.15 y 0.12 nM, respectivamente) [1]. Endotelina 1 (cerdo, humano) es la endotelina generada en el endotelio, donde actúa de manera paracrina o autocrina sobre los receptores ETA y ETB en células endoteliales o musculares lisas adyacentes [2].

Endotelina 1 (porcina, humana) activa el receptor de endotelina-A (ETAR) y promueve la transición epitelial-mesenquimal en células tumorales ováricas a través de la señalización de b-arrestin. En podocitos cultivados de ratón, Endotelina 1 (porcina, humana) causó pérdida del marcador de diferenciación sinaptopodina y adquisición del marcador mesenquimal actina a-smooth muscle. Endotelina 1 (porcina, humana) promovió la migración de los podocitos mediante la activación del ETAR y aumentó la expresión de b-arrestin-1 [3].

El Endotelina 1 (cerdo, humano) (1nmol/kg) produjo fuertes respuestas presoras en ratas anestesiadas in vivo [4]. Los ratones recibieron una inyección intradérmica de 1-30 pmol de Endotelina 1 (cerdo, humano) y presentaron episodios de rascado dependientes de la dosis [5]. Se encontró que una dosis subpresora de ET-1 administrada a ratas aumentaba la permeabilidad glomerular e inflamación, así como la excreción de la proteína del diafragma escleral glomerular nephrin, efectos que podían ser bloqueados por un antagonista del receptor ETA [6]. La magnitud del aumento de ET-1 durante el tratamiento antiangiogénico puede ser un biomarcador útil para evaluar su eficacia [7].

References:
[1]. Kikuchi T, Kubo K, Ohtaki T, et al. Endothelin-1 analogues substituted at both position 18 and 19: highly potent endothelin antagonists with no selectivity for either receptor subtype ETA or ETB[J]. Journal of medicinal chemistry, 1993, 36(25): 4087-4093.
[2]. Schiffrin E L. Role of endothelin-1 in hypertension and vascular disease[J]. American journal of hypertension, 2001, 14(S3): 83S-89S.
[3]. Buelli S, RosanÒ L, Gagliardini E, et al. β-Arrestin-1 drives endothelin-1-mediated podocyte activation and sustains renal injury[J]. Journal of the American Society of Nephrology, 2014, 25(3): 523-533.
[4]. Inoue A, Yanagisawa M, Kimura S, et al. The human endothelin family: three structurally and pharmacologically distinct isopeptides predicted by three separate genes[J]. Proceedings of the national academy of sciences, 1989, 86(8): 2863-2867.
[5]. Trentin P G, Fernandes M B, D'OrlÉans-Juste P, et al. Endothelin-1 causes pruritus in mice[J]. Experimental biology and medicine, 2006, 231(6): 1146-1151.
[6]. Saleh M A, Pollock J S, Pollock D M. Distinct actions of endothelin A-selective versus combined endothelin A/B receptor antagonists in early diabetic kidney disease[J]. Journal of Pharmacology and Experimental Therapeutics, 2011, 338(1): 263-270.
[7]. Lankhorst S, Jan Danser A H, van den Meiracker A H. Endothelin-1 and antiangiogenesis[J]. American Journal of Physiology-Regulatory, Integrative and Comparative Physiology, 2016, 310(3): R230-R234.

Chemical Properties

Cas No. 117399-94-7 SDF
Canonical SMILES Cys-Ser-Cys-Ser-Ser-Leu-Met-Asp-Lys-Glu-Cys-Val-Tyr-Phe-Cys-His-Leu-Asp-Ile-Ile-Trp (Disulfide bridge: Cys1-Cys15, Cys3-Cys11)
Formula C109H159N25O32S5 M.Wt 2491.9
Solubility H2O : 1.8 mg/mL (0.72 mM; ultrasonic and adjust pH to 3 with HCl) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 0.4013 mL 2.0065 mL 4.013 mL
5 mM 0.0803 mL 0.4013 mL 0.8026 mL
10 mM 0.0401 mL 0.2007 mL 0.4013 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 29 reference(s) in Google Scholar.)

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