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.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 117399-94-7
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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. |
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.
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. |
Prepare stock solution | |||
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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