Avosentan

SKU: orb1296080

Description

Avosentan

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 290815-26-8
• MW: 479.51
• Purity: 98.31%
• Formula: C₂₃H₂₁N₅O₅S
• SMILES: COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(nc1OC)-c1ccncc1
• Target: Endothelin Receptor
• Solubility: H2O:Insoluble;10% DMSO+40% PEG300+5% Tween-80+45% Saline:1 mg/mL (2.09 mM);DMSO:45 mg/mL (93.85 mM)

Bioactivity

• Target IC50:
  ETA:3 nM
• In Vivo:
  METHODS: Avosentan (Ro 67-0565; SPP-301) was administered by intragastric administration in a single dose (6 rats per group: 0.1, 1.0, 10, 100 mg/kg). Rats were placed in metabolic cages for 24 hours after administration to assess body fluid electrolyte homeostasis. RESULTS The highest dose (100 mg/kg) of Avosentan (Ro 67-0565; SPP-301) resulted in reduced 24-hour diuresis (18.3%) and natriuresis (17.6%), hematocrit, and hematocrit in a hypertensive dTGR model Then it dropped. METHODS: Apolipoprotein E (Apoe) knockout (KO) mice were randomly assigned to the following groups: nondiabetic controls and streptozotocin-induced diabetic animals treated daily with placebo, Avosentan (Ro 67-0565; SPP -301) (high dose: 30 mg/kg, or low dose: 10 mg/kg) by intragastric administration for 20 weeks. RESULTS Blood pressure remained unchanged after Avosentan (Ro 67-0565; SPP-301) treatment. High-dose Avosentan (Ro 67-0565; SPP-301) could significantly reduce diabetes-related albuminuria after 10 and 20 weeks of treatment. Creatinine clearance was normalized with Avosentan (Ro 67-0565; SPP-301). In diabetic mice, high-dose Avosentan (Ro 67-0565; SPP-301) treatment significantly attenuated the glomerulosclerosis index, mesangial matrix accumulation, glomerular accumulation of the matrix protein collagen IV, and the encoded connective tissue growth factor , renal expression of genes for vascular endothelial growth factor, transforming growth factor beta, and nuclear factor kappa B (p65 subunit).

Storage & Handling

• Storage: 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

Avosentan, ET-A, EndothelinReceptor, Endothelin Receptor, Inhibitor, inhibit, Ro 67-0565, SPP 301, SPP301, SPP-301

Compound Identifiers

PubChem CID

9912992