| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
Avosentan targets the endothelin A receptor (ETₐ). It is a potent and selective ETₐ antagonist. By blocking the ETₐ receptor, it prevents the vasoconstrictive and proliferative effects of endothelin-1. This leads to vasodilation, reduced blood pressure, and reduced proteinuria. Avosentan has been studied for its renoprotective effects.
|
|---|---|
| ln Vitro |
In vitro, Avosentan is a potent and selective ETₐ receptor antagonist. Its binding affinity and selectivity for the ETₐ receptor have been characterized in radioligand binding assays. It inhibits endothelin-1-mediated signaling in cell-based assays. Avosentan has been shown to reduce endothelin-1-induced vasoconstriction in isolated blood vessels.
|
| ln Vivo |
In vivo, Avosentan has been studied in clinical trials for diabetic nephropathy. It has been shown to reduce proteinuria and slow the progression of kidney disease in diabetic patients. Avosentan also lowers blood pressure and has been investigated for its effects on cardiovascular outcomes. However, clinical development has been associated with fluid retention and edema.
|
| Enzyme Assay |
The activity of Avosentan can be assessed using radioligand binding assays. Membranes prepared from cells expressing the ETₐ receptor are incubated with a radiolabeled endothelin-1 ligand and varying concentrations of Avosentan. The displacement of the radioligand is measured to determine the binding affinity (IC₅₀ or Ki). Functional assays measuring endothelin-1-induced calcium mobilization or vasoconstriction can also be used.
|
| Cell Assay |
To evaluate the cellular effects of Avosentan, cells expressing the ETₐ receptor (e.g., vascular smooth muscle cells) are treated with the compound. The inhibition of endothelin-1-induced signaling (e.g., calcium mobilization, proliferation) is measured. The effects on cell viability and inflammation are assessed.
|
| Animal Protocol |
In vivo studies with Avosentan typically involve administration to animal models via oral routes. In models of diabetic nephropathy, the compound's effects on proteinuria, renal function, and histology are assessed. Its effects on blood pressure and cardiovascular function are also evaluated. Pharmacokinetic parameters, such as oral bioavailability and half-life, are characterized.
|
| ADME/Pharmacokinetics |
Avosentan has a molecular formula and weight that are not specified in the available literature. Its CAS number is 290815-26-8. It is a potent and selective ETₐ receptor antagonist. It is soluble in DMSO and other organic solvents. The purity is typically >98%. It should be stored according to the manufacturer's instructions.
|
| Toxicity/Toxicokinetics |
Avosentan has been associated with fluid retention and edema in clinical trials, which has limited its development. Other side effects may include headache, hypotension, and flushing. It should be used with caution in patients with heart failure or renal impairment.
|
| References |
|
| Additional Infomation |
SPP301 (Avosentan) is a potent and highly selective ET[A] receptor blocker currently under clinical investigation in diabetic nephropathy. This study aims to evaluate whether avosentan affects the pharmacokinetics of oral steroid contraceptives.
Drug Indications It has been studied for the treatment of cardiovascular disease and neuropathy (diabetes). Mechanism of Action Avosentan affects the concentration levels of ethinylestradiol and progesterone. Therefore, the contraceptive efficacy of low-dose combined oral contraceptives may be adversely affected during avosentan treatment. Avosentan is a potent and selective endothelin A receptor antagonist that has been investigated for the treatment of diabetic nephropathy. It reduces proteinuria and slows the progression of kidney disease. Despite its efficacy, clinical development has been limited by fluid retention and edema. Avosentan is a research tool for studying the endothelin system and renal disease. |
| Molecular Formula |
C23H21N5O5S
|
|---|---|
| Molecular Weight |
479.50834
|
| Exact Mass |
479.126
|
| CAS # |
290815-26-8
|
| PubChem CID |
9912992
|
| Appearance |
White to off-white solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
575.5±60.0 °C at 760 mmHg
|
| Flash Point |
301.8±32.9 °C
|
| Vapour Pressure |
0.0±1.6 mmHg at 25°C
|
| Index of Refraction |
1.621
|
| LogP |
0.87
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
34
|
| Complexity |
732
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
YBWLTKFZAOSWSM-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C23H21N5O5S/c1-15-8-9-19(25-14-15)34(29,30)28-22-20(33-18-7-5-4-6-17(18)31-2)23(32-3)27-21(26-22)16-10-12-24-13-11-16/h4-14H,1-3H3,(H,26,27,28)
|
| Chemical Name |
N-[6-methoxy-5-(2-methoxyphenoxy)-2-pyridin-4-ylpyrimidin-4-yl]-5-methylpyridine-2-sulfonamide
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~6.67 mg/mL (~13.91 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.67 mg/mL (1.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.67 mg/mL (1.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0855 mL | 10.4273 mL | 20.8546 mL | |
| 5 mM | 0.4171 mL | 2.0855 mL | 4.1709 mL | |
| 10 mM | 0.2085 mL | 1.0427 mL | 2.0855 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
