Nebentan potassium

SKU: orb1694121

Description

Nebentan potassium (YM598) is a selective, orally bioavailable ETA receptor antagonist. It has demonstrated efficacy in inhibiting pulmonary arterial hypertension in preclinical models, making it a valuable research tool for studying cardiovascular and neurological diseases associated with endothelin signaling.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 342005-82-7
• MW: 529.61
• Purity: 99.05%
• Formula: C₂₄H₂₀KN₅O₅S
• SMILES: O=S([N-]C1=NC(C2=NC=CC=N2)=NC(OC)=C1OC3=C(C=CC=C3)OC)(/C=C/C4=CC=CC=C4)=O.[K+]
• Target: Endothelin Receptor
• Solubility: DMSO:100 mg/mL (188.82 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.23 mM)

Bioactivity

• Target IC50:
  ETB:569 nM (Ki)|ETA:0.679 nM (Ki)
• In Vivo:
  In medullary rats, the DR(2) values of Nebentan potassium are 0.53 mg/kg and 0.77 mg/kg, respectively. When administered orally at 1 mg/kg, Nebentan potassium maintains its antagonistic effects in conscious rats for over 6.5 hours.
• In Vitro:
  Nebentan potassium also inhibited endothelin-1-induced vasoconstriction in isolated rat aorta with a pA(2) value of 7.6.

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

Endothelin Receptor, EndothelinReceptor, ET-A, Nebentan potassium, YM598

Compound Identifiers

PubChem CID

12093171