| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 2mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
ETA; ETB
Endothelin-1 (ET-1) is an endogenous agonist for two G protein-coupled receptor subtypes: Endothelin Receptor Type A (ETA) and Endothelin Receptor Type B (ETB). [1] |
|---|---|
| ln Vitro |
Endothelin-1 (ET-1) is primarily secreted by endothelial cells and is a powerful endogenous vasoconstrictor. It functions by means of the ETA and ETB receptor subtypes. ET-1 not only has a vasoconstrictive effect but also induces vascular cell fibrosis and increases reactive oxygen species production. Proinflammatory mechanisms are said to be induced by ET-1, leading to an increase in superoxide anion production and cytokine secretion[1].
Endothelin-1 (ET-1) stimulates the production of reactive oxygen species (ROS), primarily superoxide anions, in various cell types, contributing to oxidative stress.[1] Endothelin-1 (ET-1) induces proinflammatory mechanisms, including the activation of transcription factors such as NF-κB and the expression of proinflammatory cytokines like TNF-α, IL-1, and IL-6.[1] Endothelin-1 (ET-1) enhances the expression of adhesion molecules (e.g., VCAM-1) on vascular endothelial cells and stimulates the aggregation of polymorphonuclear neutrophils (PMNs).[1] Endothelin-1 (ET-1) can induce cyclooxygenase-2 (COX-2) expression and prostaglandin E2 (PGE2) release via MAPK and NF-κB pathways.[1] |
| ln Vivo |
During endotoxemia or sepsis, plasma levels of Endothelin-1 (ET-1) are increased in various animal species and in humans. This elevation correlates with the severity of illness and morbidity/mortality rates in septic patients.[1]
Infusion of Endothelin-1 (ET-1) in experimental models of septic shock contributes to the dysfunction of vital organs such as the liver, lung, heart, and kidney. In humans, ET-1 infusion causes cardiovascular changes resembling those in sepsis, including decreased cardiac output and vasoconstriction.[1] Endothelin-1 (ET-1) is implicated in the development of atherosclerosis. Overexpression of ET-1 increased atherosclerotic lesion size in apolipoprotein E knockout mice fed a high-fat diet.[1] Endothelin-1 (ET-1) administration can cause initial vasodilation followed by prolonged vasoconstriction, leading to ischemia and endothelial dysfunction.[1] |
| References | |
| Additional Infomation |
Endothelin-1 (ET-1) is a peptide composed of 21 amino acids that is produced in a variety of tissues, including endothelial cells and vascular smooth muscle cells, neurons and astrocytes in the central nervous system, and endometrial cells. It can regulate vasomotor tone, cell proliferation and hormone secretion. (N Eng J Med 1995;333(6):356-63)
Endothelin-1 (ET-1) is a potent endogenous vasoconstrictive peptide composed of 21 amino acids that is mainly secreted by endothelial cells. It is the most abundant subtype in the endothelin family. [1] Endothelin-1 (ET-1) In addition to vasoconstriction, it is involved in a variety of physiological and pathophysiological processes, including fibrosis, vascular and myocardial remodeling, inflammation, oxidative stress and nociception. [1] In diseases such as sepsis and atherosclerosis, endothelin receptor antagonists (e.g., bosentan, tezosentan, BQ123, BQ788) can attenuate the pathophysiological effects of endothelin-1 (ET-1). [1] In sepsis, endothelin-1 (ET-1) levels are elevated and associated with microcirculatory dysfunction and organ damage. Its effects are mediated by ETA and ETB receptors. [1] |
| Molecular Formula |
C₁₀₉H₁₅₉N₂₅O₃₂S₅
|
|---|---|
| Molecular Weight |
2491.90
|
| Exact Mass |
2490.018
|
| CAS # |
117399-94-7
|
| Related CAS # |
Endothelin 1 (swine, human) (TFA); 394693-38-0
|
| PubChem CID |
16168476
|
| Sequence |
[Cys1-Cys15, Cys3-Cys11] Cys-Ser-Cys-Ser-Ser-Leu-Met-Asp-Lys-Glu-Cys-Val-Tyr-Phe-Cys-His-Leu-Asp-Ile-Ile-Trpor L-cysteinyl-L-seryl-L-cysteinyl-L-seryl-L-seryl-L-leucyl-L-methionyl-L-alpha-aspartyl-L-lysyl-L-alpha-glutamyl-L-cysteinyl-L-valyl-L-tyrosyl-L-phenylalanyl-L-cysteinyl-L-histidyl-L-leucyl-L-alpha-aspartyl-L-isoleucyl-L-isoleucyl-L-tryptophan (1->15),(3->11)-bis(disulfide) H-Cys(1)-Ser-Cys(2)-Ser-Ser-Leu-Met-Asp-Lys-Glu-Cys(2)-Val-Tyr-Phe-Cys(1)-His-Leu-Asp-Ile-Ile-Trp-OH
|
| SequenceShortening |
CSCSSLMDKECVYFCHLDIIW (Disulfide bridge: Cys1-Cys15, Cys3-Cys11)
|
| Appearance |
White to pink solid powder
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
2467.3±65.0 °C at 760 mmHg
|
| Flash Point |
1446.0±34.3 °C
|
| Vapour Pressure |
0.0±0.3 mmHg at 25°C
|
| Index of Refraction |
1.556
|
| LogP |
-0.36
|
| Hydrogen Bond Donor Count |
32
|
| Hydrogen Bond Acceptor Count |
40
|
| Rotatable Bond Count |
47
|
| Heavy Atom Count |
171
|
| Complexity |
5300
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
ZUBDGKVDJUIMQQ-ZTNLKOGPSA-N
|
| InChi Code |
InChI=1S/C109H159N25O32S5/c1-12-56(9)87(107(163)125-76(109(165)166)39-60-43-113-65-24-18-17-23-63(60)65)134-108(164)88(57(10)13-2)133-99(155)75(42-85(143)144)123-94(150)70(36-54(5)6)118-97(153)73(40-61-44-112-52-114-61)121-103(159)80-49-169-168-48-64(111)89(145)126-77(45-135)102(158)131-81-50-170-171-51-82(105(161)132-86(55(7)8)106(162)124-72(38-59-26-28-62(138)29-27-59)95(151)120-71(96(152)130-80)37-58-21-15-14-16-22-58)129-91(147)67(30-31-83(139)140)116-90(146)66(25-19-20-33-110)115-98(154)74(41-84(141)142)122-92(148)68(32-34-167-11)117-93(149)69(35-53(3)4)119-100(156)78(46-136)127-101(157)79(47-137)128-104(81)160/h14-18,21-24,26-29,43-44,52-57,64,66-82,86-88,113,135-138H,12-13,19-20,25,30-42,45-51,110-111H2,1-11H3,(H,112,114)(H,115,154)(H,116,146)(H,117,149)(H,118,153)(H,119,156)(H,120,151)(H,121,159)(H,122,148)(H,123,150)(H,124,162)(H,125,163)(H,126,145)(H,127,157)(H,128,160)(H,129,147)(H,130,152)(H,131,158)(H,132,161)(H,133,155)(H,134,164)(H,139,140)(H,141,142)(H,143,144)(H,165,166)/t56-,57-,64-,66-,67-,68-,69-,70-,71-,72-,73-,74-,75-,76-,77-,78-,79-,80-,81-,82-,86-,87-,88-/m0/s1
|
| Chemical Name |
(3S)-3-[[(2S)-2-[[(2S)-2-[[(1R,4S,7S,10S,13S,16S,19S,22S,25R,28S,31R,36R,39S,42S,45S)-31-amino-7-(4-aminobutyl)-39-benzyl-4-(2-carboxyethyl)-10-(carboxymethyl)-19,22,28-tris(hydroxymethyl)-42-[(4-hydroxyphenyl)methyl]-16-(2-methylpropyl)-13-(2-methylsulfanylethyl)-3,6,9,12,15,18,21,24,27,30,38,41,44,47-tetradecaoxo-45-propan-2-yl-33,34,49,50-tetrathia-2,5,8,11,14,17,20,23,26,29,37,40,43,46-tetradecazabicyclo[23.22.4]henpentacontane-36-carbonyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-4-methylpentanoyl]amino]-4-[[(2S,3S)-1-[[(2S,3S)-1-[[(1S)-1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-4-oxobutanoic acid
|
| Synonyms |
Endothelin 1 swine, human
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
H2O: ~28 mg/mL (~11.2 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (1.00 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (1.00 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (1.00 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.4013 mL | 2.0065 mL | 4.0130 mL | |
| 5 mM | 0.0803 mL | 0.4013 mL | 0.8026 mL | |
| 10 mM | 0.0401 mL | 0.2007 mL | 0.4013 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
