Endothelin-2 (49-69), human

SKU: orb1296724

Description

Human endothelin-2 (49-69) is a 21-residue bioactive peptide that acts as an agonist for endothelin receptor subtypes ET-RA and ET-RB. This peptide is widely used in cardiovascular research to study vasoconstriction, cellular signaling pathways, and receptor pharmacology in both in vitro and in vivo experimental models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 123562-20-9
• MW: 2546.92
• Purity: 98.26% (May vary between batches)
• Formula: C₁₁₅H₁₆₀N₂₆O₃₂S₄
• SMILES: C(C=1C=2C(NC1)=CC=CC2)[C@H]3C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@]4(CSSC[C@@](C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N3)(NC(=O)[C@H](CO)NC(=O)[C@@H](N)CSSC[C@@H](C(N[C@@H](CC5=CN=CN5)C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@@H](CC=6C=7C(NC6)=CC=CC7)C(O)=O)=O)[C@H](CC)C)=O)[C@H](CC)C)=O)CC(O)=O)=O)CC(C)C)=O)=O)NC(=O)[C@H](CC8=CC=CC=C8)NC(=O)[C@H](CC9=CC=C(O)C=C9)NC(=O)[C@H](C(C)C)NC4=O)[H])[H]
• Target: Endothelin Receptor,Others
• Solubility: H2O:Soluble

Bioactivity

• In Vivo:
  Rats For the assay of pressor activity, male Wistar rats weighing 300-350 g are anesthetized with urethane (1 g/kg i.p.) and pretreated with atropine (0.25 mg/kg i.v.), propranolol (1 mg/kg i.v.), and bunazocine (1 mg/kg i.v.). Additional maintenance doses (one-half of the initial doses) of the autonomic blockades are administered every 3-4 hr. Each animal is given only one bolus of Endothelin-2. 1 nM of Endothelin-2 in 50 渭L of buffer is bolus injected from a cannula inserted in the right femoral vein. The blood pressure is recorded from a cannula, which is placed in the right carotid artery and connected to a pressure transducer.
• In Vitro:
  At nanomolar concentrations, Endothelin-2 significantly induces strong and persistent vasoconstriction, similar to the effects observed with other endothelins (EC50=0.52 nM). It functions as a potent chemoattractant specifically for macrophages and THP-1 monocytic cells, but does not attract freshly isolated monocytes. The chemotactic activity towards Endothelin-2 demonstrates a characteristic bell-shaped curve. Research utilizing endothelin receptor antagonists has revealed that the ET-RB receptor mediates the directed cell migration towards Endothelin-2. Moreover, the presence of Endothelin-2 in tumor environments suggests it plays a role in modifying macrophage behavior, leading to the accumulation of activated macrophages in hypoxic regions.

Storage & Handling

• Storage: keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

transmembrane, peptide, vasoactive, ET-RA, ET-RB, Endothelin-2, Endothelin2 (4969), human, Endothelin-2 (human, canine), Endothelin-2 , human, Endothelin-2, human, Endothelin 2 (49 69), human, Human endothelin 2, Human endothelin2, Human endothelin-2, Inhibitor, inhibit, acid, 21-amino

Compound Identifiers

PubChem CID

16219332