| Name | Avosentan |
| Description | Avosentan（Ro 67-0565; SPP-301） is a potent endothelin receptor (ETA) antagonist with strong inhibitory effects on endothelin-1-induced contraction and may have protective effects against chronic kidney disease. [2] |
| 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. [1]
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). [2] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | H2O : Insoluble
DMSO : 45 mg/mL (93.85 mM), Sonication is recommended.
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| Keywords | SPP301 | SPP 301 | Inhibitor | inhibit | Endothelin Receptor | Avosentan |
| Inhibitors Related | Macitentan | BMS 182874 | Bosentan | BMS 182874 hydrochloride | Sitaxsentan sodium | Edonentan | Sulfisoxazole | Ambrisentan | Sparsentan | Aprocitentan | Nebentan potassium | Clazosentan |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | ReFRAME Related Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Compound Library | Human Metabolite Library | Anti-Cancer Drug Library |
United States
