Azilsartan (codenamed TAK-536) is an angiotensin II receptor antagonist used in the treatment of hypertension. Azilsartan potently inhibited vascular cell proliferation in the absence of exogenously supplemented angiotensin II. Azilsartan increased tissue glucose uptake, especially in skeletal muscle and adipose tissue. In cultured 3T3-L1 preadipocytes, azilsartan enhanced adipogenesis and exerted greater effects than valsartan on expression of genes encoding peroxisome proliferator-activated receptor-α (PPARα), PPARδ, leptin, adipsin, and adiponectin. In adipose tissue, Azilsartan (TAK-536) reduced TNF-alpha expression but increased the expression of adiponectin, PPARgamma, C/EBalpha, and aP2. In addition, azilsartan downregulated 11β-hydroxysteroid dehydrogenase type 1 expression. Azilsartan is currently in a phase IV clinical trial in the treatment of hypertension.
Tampere University. 2021.
Novel Targeted Therapies and Prognostic Markers for T Cell Acute Lymphoblastic Leukemia
Azilsartan purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | male Wister rats, aged 6–8 weeks |
| Formulation | Na-CMC |
| Dosages | 3.5 mg/kg, 7 mg/kg |
| Administration | p.o. |
| Molecular Weight | 456.45 |
| Formula | C25H20N4O5 |
| CAS Number | 147403-03-0 |
| Solubility (25°C) | DMSO 25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Angiotensin Receptor Products |
|---|
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(Sar1,Ile4,8)-Angiotensin II is a functionally selective angiotensin II type 1 receptor (AT1R) agonist. |
| TRV055
TRV055, a G-protein-biased agonist, is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). |
| Alamandine
Alamandine, a member of the renin-angiotensin system (RAS), a vasoactive peptide, is an endogenous ligand of the G protein-coupled receptor MrgD. |
| (Sar1)-Angiotensin II
(Sar1)-Angiotensin II, an analogue of Angiotensin II, is a specific agonist of angiotensin AT1 receptor. |
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