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Avosentan
🥰Excellent
Catalog No. TQ0282Cas No. 290815-26-8
Alias SPP-301, Ro 67-0565
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]
Avosentan
🥰Excellent
Purity: 99.47%
Catalog No. TQ0282Alias SPP-301, Ro 67-0565Cas No. 290815-26-8
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]
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $34 | In Stock | |
| 5 mg | $77 | In Stock | |
| 10 mg | $108 | In Stock | |
| 25 mg | $228 | In Stock | |
| 50 mg | $396 | In Stock | |
| 100 mg | $579 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $81 | In Stock |
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Purity:99.47%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| 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] |
| Alias | SPP-301, Ro 67-0565 |
| Molecular Weight | 479.51 |
| Formula | C23H21N5O5S |
| Cas No. | 290815-26-8 |
| Smiles | COc1ccccc1Oc1c(NS(=O)(=O)c2ccc(C)cn2)nc(nc1OC)-c1ccncc1 |
| Relative Density. | 1.364 g/cm3 |
Storage & Solubility Information
| 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.  | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
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DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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