Endothelin-1, human CAS NO.117399-94-7
Endothelin-1, human CAS NO.117399-94-7
TECHNICAL SPECIFICATIONS
| Item | Specification |
|---|---|
| Product Name | Endothelin-1, human |
| CAS NO. | 117399-94-7 |
| Appearance | White to off-white lyophilized powder |
| Molecular Formula | C109H159N25O32S5 |
| Molecular Weight | 2491.95g/mol |
| Purity (RP-HPLC) | ≥ 95.0% |
| Solubility | Soluble in 0.1% acetic acid (0.1 mM) or aqueous buffers; reconstitute with sterile water or buffer before use |
| Endotoxin | < 1.0 EU/mg (Typical for research-grade peptides) |
| Biological Activity | Potent vasoconstrictor peptide; agonist at ETₐ and ETᵦ endothelin receptors, with IC₅₀ values in the nanomolar range in competitive binding assays |
| Storage Conditions | -20°C (or -80°C for long-term storage); avoid repeated freeze-thaw cycles; store desiccated. |
| Stock Location | Stock in USA |
| MOQ | 1g |
1.MECHANISM OF ACTION
Endothelin-1 exerts its effects by binding to two G protein-coupled receptors: Endothelin A (ETA) and Endothelin B (ETB). The primary mechanism involves:
- Vasoconstriction: Binding to ETA receptors on vascular smooth muscle cells activates phospholipase C, leading to increased inositol trisphosphate and intracellular calcium, resulting in sustained and potent vasoconstriction.
- Receptor-Mediated Effects: Binding to ETB receptors on endothelial cells stimulates nitric oxide and prostacyclin release, initially causing vasodilation. However, ETB receptors on smooth muscle can also mediate vasoconstriction.
- Cellular Proliferation: ET-1 also acts as a growth factor, promoting smooth muscle cell, fibroblast, and cardiomyocyte proliferation, contributing to vascular and cardiac remodeling.
2.PRODUCT INDICATIONS
This product is indicated for in vitro and in vivo research in the following areas:
- Cardiovascular Research: Modeling hypertension, heart failure, and atherosclerosis by studying vascular contraction and remodeling.
- Pulmonary Research: Investigating pulmonary arterial hypertension (PAH) and airway constriction.
- Renal Physiology: Studying renal blood flow regulation and its role in chronic kidney disease.
- Cancer Biology: Researching tumor angiogenesis and cancer progression, as ET-1 is often overexpressed in tumors.
- Drug Discovery: Screening for endothelin receptor antagonists (e.g., bosentan, ambrisentan) used to treat PAH.
- Cell Signaling: Elucidating pathways involving G-proteins, calcium signaling, and mitogen-activated protein kinases (MAPKs).
3.CLINICAL EFFICACY OF PRODUCT
Endothelin-1 itself is not a therapeutic agent; it is a pathophysiological mediator. Its immense clinical relevance is demonstrated by the success of drugs that block its action. The clinical efficacy of targeting this pathway is well-established:
- Pulmonary Arterial Hypertension (PAH) Treatment: Endothelin receptor antagonists (ERAs) like bosentan, ambrisentan, and macitentan are FDA-approved therapies for PAH. They work by blocking the effects of ET-1, leading to vasodilation and improved exercise capacity, validating ET-1 as a critical drug target.
- Other Conditions: ERAs are also used or under investigation for resistant hypertension, scleroderma renal crisis, and certain cancers, proving the broad pathogenic role of ET-1.
- Biomarker: Plasma ET-1 levels are a prognostic marker in cardiovascular diseases like heart failure and PAH.
4.DELIVERY & SHIPPING
We specialize in global logistics for various cosmetic peptides. Your order will be handled with the utmost care, ensuring safe, reliable, and intact delivery.
Professional and Secure Packaging
Each bottle of peptide is protected with a special packaging solution to ensure stability and integrity during transportation.
We can also customize packaging according to customer needs.
Shipping Methods
Main Method: International Air Freight
We primarily use DHL, FedEx, UPS, and TNT because of their global reliability, speed, and advanced tracking systems. Air freight ensures the fastest transit time and minimizes the impact of environmental factors on the product.
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