Synonym |
ET-1 |
Species |
Porcine |
Protein Accession |
P05305 |
Purity |
Greater than 95% purity as determined by SDS-PAGE |
Endotoxin Level |
Less than 0.1 ng/µg (1 EU/µg) |
Biological Activity |
The ED50 for this effect is typically 1-5 nM |
Expression System |
E. coli |
Fusion Tag |
None |
Predicted Molecular Mass |
2.6 kDa |
Formulation |
Lyophilized from a 0.2 μm filtered solution in Acetonitrile and TFA |
Reconstitution |
Centrifuge vial before opening. Reconstitute in water to a concentration of 0.1-1.0 mg/ml |
Storage & Stability |
Store at -80°C. It is recommended to reconstitute the lyophilized product in sterile water not
less than 100µg/ml, which can then be further diluted to other aqueous solutions. |
FAQ
What is Big Endothelin-1 (porcine) and how does it function in research?
Big Endothelin-1
(porcine) is a highly selective vasoconstrictor peptide that has gained significant attention in
research environments due to its vital role in various physiological and pathological processes. Derived
from porcine sources, this peptide is a precursor of the potent vasoconstrictor endothelin-1, which
plays a pivotal role in the regulation of vascular tone and blood flow. In the body, Big Endothelin-1 is
predominantly produced by endothelial cells and needs to be converted into the active form,
endothelin-1, through enzymatic cleavage by endothelin-converting enzyme. Once activated, endothelin-1
impacts numerous cellular functions, prominently influencing vasoconstriction, cell proliferation, and
even inflammation.
Its importance extends to its ability to modulate blood pressure, making it a
molecule of interest in cardiovascular research. Studies have highlighted its involvement in various
disorders, including hypertension, pulmonary arterial hypertension, and other cardiovascular diseases,
rendering it a crucial component in understanding and potentially managing these conditions. Moreover,
Big Endothelin-1 is also known to have a role in fibrosis, linking it to kidney diseases and certain
types of cancer due to its capability to promote fibroblast proliferation and extracellular matrix
production.
In research, studying the pathways and interactions of Big Endothelin-1 can help
scientists explore therapeutic targets for new drug developments aimed at blocking or modulating its
effects. Its use in experimental setups allows researchers to simulate disease conditions that can lead
to invaluable insights into the mechanisms underlying cardiovascular pathologies. This peptide,
therefore, is not just a subject of interest for understanding basic physiological processes but is also
a promising focal point for therapeutic interventions and drug development.
Researchers, by
manipulating the Big Endothelin-1 pathway, can delineate its contributions to disease states and
pinpoint precisely where therapeutic interventions may be most effective. This capability enhances the
scientific understanding of cardiovascular pathologies on a molecular level, opening doors for the
development of innovative strategies to manage and treat these diseases effectively. Thus, Big
Endothelin-1 (porcine) is a cornerstone in the research sphere, aiding in the bridging of fundamental
science with clinical applications.
Why is Big Endothelin-1 (porcine) considered crucial in
cardiovascular studies?
Big Endothelin-1 (porcine) stands at the forefront of cardiovascular
studies due to its profound influence on vascular biology and its association with several
cardiovascular conditions. As a precursor to endothelin-1, it is central to the regulation of vascular
tone, impacting both systemic and pulmonary circulation. This regulation is vital because it helps
maintain blood pressure within optimal ranges and ensures adequate tissue perfusion. Its remarkable
vasoconstrictive properties make it a significant player in the onset and progression of hypertension, a
major risk factor for various cardiovascular diseases such as heart attack, stroke, and heart
failure.
The pathological increase in endothelin-1 levels has been consistently linked to several
cardiovascular disorders, highlighting the importance of its precursor, Big Endothelin-1, in
understanding these conditions. Its role is further complicated by its involvement in vascular
remodeling, a process associated with progressive diseases like atherosclerosis, in which changes in the
vessel wall adaptive responses contribute to the disease pathology. In this sense, Big Endothelin-1 is
not only crucial for understanding the etiology of cardiovascular diseases but also for identifying
potential biomarkers for early detection and therapeutic targets for clinical
intervention.
Research involving Big Endothelin-1 (porcine) allows scientists to delve deeper
into the molecular mechanisms governing cardiovascular health. By exploring its biosynthesis,
conversion, and interaction with various receptors and enzymes, researchers are uncovering the intricate
networks that control vascular function and blood pressure. Such research is vital, as it paves the way
for the development of advanced treatments and preventative strategies against cardiovascular diseases
that currently represent the leading cause of morbidity and mortality worldwide.
Moreover,
cardiovascular studies focused on Big Endothelin-1 are critical in advancing personalized medicine
approaches. Given that genetic variations may influence endothelin expression and function,
understanding the specifics of how Big Endothelin-1 acts allows for more tailored interventions in
patient care. This specificity in targeting the endothelin pathway can potentially reduce drug side
effects and increase therapeutic efficacy in managing cardiovascular diseases.
In the broader
scope of health and disease, research involving Big Endothelin-1 (porcine) extends its importance beyond
just cardiovascular health. Its implications in systemic diseases like metabolic syndrome and its
possible role in modulating inflammation further amplify its significance in medical research. Overall,
Big Endothelin-1 (porcine) is esteemed for its far-reaching impact on cardiovascular studies, aiding in
the comprehensive understanding and innovative management of complex health conditions.
What are
the advantages of using a porcine model in research involving Big Endothelin-1?
The utilization
of porcine models in research involving Big Endothelin-1 offers several advantages, rooted in their
physiological and anatomical similarities to humans. Porcine models are particularly valued in
cardiovascular research, given their comparable heart size, cardiac output, and similar coronary artery
structure to humans. This similarity is crucial when studying the cardiovascular effects of Big
Endothelin-1, as it allows for more accurate extrapolation of data and findings to human physiology and
clinical settings.
One of the primary advantages of the porcine model is its relevance in
studying disease progression and therapeutic responses. Pigs exhibit similar progression patterns of
cardiovascular diseases as seen in humans, especially in atherosclerosis and hypertension. In the
context of Big Endothelin-1, using a porcine model enables researchers to observe the effects of this
potent peptide on blood vessels and blood pressure regulation in a more clinically relevant manner. This
relevance is particularly beneficial in the development of endothelin-targeted therapies, where the
physiological responses in pigs can better predict human outcomes compared to smaller animals like
rodents.
Additionally, porcine models provide the opportunity to conduct longitudinal studies due
to their larger size and longer lifespan relative to other animal models. This capability is vital when
examining chronic effects and long-term therapeutic interventions involving Big Endothelin-1.
Longitudinal studies can offer insights into the chronic impact of endothelin modulation and help assess
the long-term safety and efficacy of potential drug candidates targeting the endothelin
system.
Another advantage lies in the genetic and molecular research capabilities available with
porcine models. With advancements in genetic tools, it's possible to create genetically modified pigs
that model human diseases more accurately than traditional small animal models. In studies requiring
precision, such as those focusing on the specific genetic pathways of Big Endothelin-1, porcine models
can be genetically modified to reflect human gene expressions and mutations pertinent to cardiovascular
diseases. This ability enhances the depth of molecular research and aids in the validation of potential
therapeutic targets.
Moreover, recent technological advancements have allowed for more
cost-effective and efficient maintenance of porcine models in research environments. The availability of
specialized facilities to house and study these animals has grown, making them more accessible to
research institutions aiming to develop innovative cardiovascular therapies.
Overall, the use of
porcine models in studying Big Endothelin-1 is justified by their physiological resemblance to humans,
the potential for longitudinal and genetic studies, and their growing accessibility within the research
community. These advantages make them an invaluable asset in the quest to better understand the
implications of Big Endothelin-1 in human health and disease, particularly within the cardiovascular
realm.
How does Big Endothelin-1 (porcine) influence the research of pulmonary arterial
hypertension?
Pulmonary arterial hypertension (PAH) is a complex and challenging condition
characterized by high blood pressure in the pulmonary arteries, leading to heart failure and reduced
lifespan if left untreated. Big Endothelin-1 (porcine), as a precursor to endothelin-1, plays a central
role in the pathophysiology of PAH by contributing to the vascular remodeling, vasoconstriction, and
proliferation of vascular smooth muscle cells that typify the disease. Its influence on PAH research
lies in elucidating the mechanisms that drive these pathological processes and in identifying potential
therapeutic targets to combat this disease.
Research focusing on Big Endothelin-1 helps shed
light on its conversion to the active endothelin-1 peptide and its interaction with endothelin
receptors, which are abundantly expressed in the pulmonary vasculature. This interaction is critical, as
the binding of endothelin-1 to its receptors triggers a cascade of intracellular signaling events that
promote the aforementioned pathological changes in the pulmonary arteries. Understanding these signaling
pathways is essential for developing therapeutic interventions that can mitigate the progression of
PAH.
The role of Big Endothelin-1 in PAH research extends to evaluating the efficacy of
endothelin receptor antagonists (ERAs), a class of drugs that block the effects of endothelin-1. Studies
utilizing Big Endothelin-1 can model the pathobiology of PAH to test these drugs' ability to reduce
vascular remodeling and improve hemodynamic parameters. Such research provides valuable insights into
the effectiveness of ERAs, offering data that could guide therapeutic protocols and drug development
efforts aimed at enhancing patient outcomes.
Moreover, Big Endothelin-1 (porcine) research has
paved the way for investigating combination therapies involving ERAs with other PAH treatments, such as
phosphodiesterase inhibitors or prostacyclin analogs. Exploring these combinations in experimental
models helps determine synergistic effects that may improve treatment efficacy and overcome limitations
seen with monotherapies.
The impact of Big Endothelin-1 on PAH research also includes its
potential role as a biomarker for disease progression and treatment response. Since changes in
endothelin levels are associated with PAH severity, monitoring Big Endothelin-1 could provide a
non-invasive means to assess patient status and adjust therapeutic strategies accordingly. Such
applications underscore the multifaceted importance of Big Endothelin-1 in advancing both the basic
understanding and clinical management of PAH.
In summary, Big Endothelin-1 (porcine) is a
critical component in the landscape of PAH research. It provides essential insights into disease
mechanisms, aids in the evaluation of ERAs and combination therapies, and holds promise as a biomarker
for monitoring PAH. Its study is indispensable for driving the innovation and therapeutic advancements
needed to improve outcomes for patients suffering from this debilitating condition.
What
distinguishes Big Endothelin-1 from other endothelin family peptides in research?
Big
Endothelin-1 is distinguished from other endothelin peptides by its role as the precursor to
endothelin-1, which is one of the most potent vasoconstrictors known. While other members of the
endothelin family, such as endothelin-2 and endothelin-3, also modulate vascular tone and impact various
physiological processes, Big Endothelin-1 serves a unique function in its involvement in the
biosynthesis pathway of endothelin-1. The conversion of Big Endothelin-1 to endothelin-1 by
endothelin-converting enzyme (ECE) is a critical regulatory step in controlling the availability of
active endothelin-1 peptide, thus influencing its physiological and pathological effects in the vascular
system.
In research, Big Endothelin-1 is often studied to understand the regulation of
endothelin-1 production and secretion, as these processes are essential in maintaining vascular
homeostasis and contributing to disease states when dysregulated. In contrast to other endothelin
peptides, Big Endothelin-1 is particularly informative in research settings where the emphasis is placed
on the enzymatic pathways responsible for peptide activation and the genetic expressions leading to
endothelin synthesis.
Furthermore, Big Endothelin-1's distinction lies in its clinical relevance
to cardiovascular pathologies. The precursor nature of Big Endothelin-1 makes it a focal point in the
investigation of endothelin-related diseases, particularly as it relates to conditions such as pulmonary
arterial hypertension, systemic hypertension, heart failure, and kidney diseases. Research involving Big
Endothelin-1 critically examines the modulation of its conversion to elucidate potential therapeutic
targets that could offer additional or alternative therapeutic pathways beyond the receptor antagonists
targeting mature endothelin-1.
In comparison to other peptides in the family, Big Endothelin-1
also provides opportunities for exploring biomarkers related to disease progression and therapeutic
efficacy. Since it directly reflects the precursor levels leading to active endothelin-1 production,
measuring Big Endothelin-1 levels offers a window into dynamic changes occurring in the cardiovascular
system and possibly other systems affected by endothelins.
Overall, what sets Big Endothelin-1
apart in research is its function as a precursor molecule, offering insights into the regulation of one
of the body's critical endothelin pathways. This distinction gives researchers a specialized angle for
unraveling complex pathophysiological mechanisms, specifically related to the potent amount of
endothelin-1 produced and its significant biological effects. Therefore, Big Endothelin-1 serves as an
essential molecule in advancing both fundamental research and practical therapeutic applications devoted
to endothelin-related conditions.