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Endothelin 1 swine, human

Catalog No.GC30485

Endothelin 1 swine, human is a synthetic peptide with the sequence of human and swine Endothelin 1, which is a potent endogenous vasoconstrictor.

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Endothelin 1 swine, human Chemical Structure

Cas No.: 117399-94-7

Size Price Stock Qty
500μg
$125.00
In stock
1mg
$220.00
In stock
5mg
$883.00
In stock
10mg
$1,471.00
In stock

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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

Endothelin 1 (swine, human) is a 21aa peptide vasoconstrictor and agonist of endothelin (ET) receptors ETA and ETB (IC50s = 0.15 and 0.12 nM, respectively) [1]. Endothelin 1 (swine, human) is the endothelin generated in the endothelium, where it acts in a paracrine or autocrine manner on ETA and ETB receptors on adjacent endothelial or smooth muscle cells [2].

Endothelin 1 (swine, human) activats endothelin-A receptor (ETAR) and drives epithelial-to-mesenchymal transition in ovarian tumor cells through b-arrestin signaling. In cultured mouse podocytes, Endothelin 1 (swine, human) caused loss of the podocyte differentiation marker synaptopodin and acquisition of the mesenchymal marker a-smooth muscle actin. Endothelin 1 (swine, human) promoted podocyte migration via ETAR activation and increased b-arrestin-1 expression [3].

The Endothelin 1 (swine, human) (1nmol/kg) produced strong pressor responses in the anesthetized rats in vivo [4]. Mice received an intradermal injection of 1-30 pmol Endothelin 1 (swine, human) and were caused dose-dependent scratching bouts [5]. A subpressor dose of ET-1 administered to rats was found to increase glomerular permeability and inflammation as well as the excretion of the glomerular slit-diaphragm protein nephrin, effects that could be blocked by an ETA receptor antagonist [6]. The magnitude of the ET-1 rise during antiangiogenic treatment may be useful biomarker of the efficacy of treatment [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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