Antibodies
Guanabenz Acetate
- 貨號 Cat. No.
- S4065
- 規格 Size
- 10mM/1mLã€50mg
- 品牌 Brand
- Selleckchem
Description
Guanabenz Acetate
Catalog No.S4065
Guanabenz Acetate is an selective agonist of α2a-adrenergic receptor, α2b-adrenergic receptor and α2c-adrenergic receptor withpEC50 of 8.25, 7.01 and ~5, respectively.
| Size | Price | Stock | Quantity | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| |||||||||||
Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | Guanabenz Acetate is an selective agonist of α2a-adrenergic receptor, α2b-adrenergic receptor and α2c-adrenergic receptor with pEC50 of 8.25, 7.01 and ~5, respectively. | |||||
|---|---|---|---|---|---|---|
| Targets | α2a-adrenergic receptor | α2b-adrenergic receptor | α2c-adrenergic receptor | |||
| IC50 | 8.25 (pEC50) | 7.01 (pEC50) | <5 (pEC50) [1] | |||
| In vitro | Guanabenz at a concentration of 30 μM causes a time-dependent loss of nNOS-activity, which is present in cytosol prepared from rat nNOS transfected HEK 293 cells, with a Ki of 1 μM. Guanabenz can induce a concentration-dependent loss of nNOS activity. Within the first 3 h of treatment, 50 μM Guanabenz decreases the accumulation of nitrite and nitrate by approximately 75% in cells. Treatment of HEK 293 cells for 24 h with Guanabenz (100 μM) causes an approximately 35% decrease in the amount of immunodetectable nNOS protein. Guanabenz enhances proteolysis of the protein with the half-life decreasing by one-half from 20 to 10 h.[2] Guanabenz is active against [ PSI+] prion in the yeast-based assay independent of its agonist activity on α2-adrenergic receptors. Guanabenz (10 μM) promote complete PrPSc clearance in mammalian MovS6 cell-based assay. [3] | |||||
| In vivo | Guanabenz injected i.v. in doses of 0.1 mg/kg causes an initial increase in blood pressure followed by a prolonged fall and a decrease in cardiac output, contractile force and heart rate in anesthetized dogs, which requires the presence of sympathetic tone. Guanabenz inhibits pressor responses to various procedures which initiate general sympathetic discharge. Guanabenz also antagonizes responses to sympathetic nerve stimulation. [4] Guanabenz injected at doses of 0.5 mg/kg and above lowers blood pressure and heart rate in unanesthetized hypertensive rats and dogs. [5] | |||||
| Features | ||||||
Protocol(Only for Reference)
Kinase Assay: [1]
| GTPγ[35S] binding assay | Cell pellets are suspended in cold homogenization buffer [5 mM of Tris-HCl, 5 mM of EDTA, 5 mM of EGTA, 0.1 mM of phenylmethysulfonyl fluoride (PMSF), pH 7.5 at 4 ℃] and lysed using a Polytron P10 disrupter (setting 6, 5-sec burst). The membranes are centrifuged at 34,000 g for 15 min at 4 ℃ and the supernatant is removed. This wash procedure is repeated, and aliquots of membranes are resuspended in 50 mM of Tris, 1 mM of EDTA, 5 mM of MgCl2, 0.1 mM of PMSF, pH 7.4, at 4 ℃ and frozen in aliquots at -70 ℃. Membranes are thawed and diluted with buffer (50 mM of Tris, pH 7.4 at 25 ℃, 5 mM of MgCl2, 100 mM of NaCl, 1 mM of EDTA, 1 mM of dithiothreitol, 1 μM of propranolol, 2 μM of GDP). Membrane protein (4 -10mg) is incubated with 0.3 nM [35S]GTPγS and agonist for 60 min at 25℃. Reactions are terminated by vacuum filtration over GF/B filters pre-treated with 0.5% BSA. Filters are washed with ice-cold wash buffer (50 mM of Tris, 5 mM of MgCl2, 100 mM of NaCl, pH 7.5, at 4 ℃), and incorporated radioactivity is determined using liquid scintillation counting. |
|---|
References
Chemical Information
Download Guanabenz Acetate SDF
| Molecular Weight (MW) | 291.13 |
|---|---|
| Formula | C8H8Cl2N4.C2H4O2 |
| CAS No. | 23256-50-0 |
| Storage | 3 years -20℃Powder |
|---|---|
| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 58 mg/mL (199 mM) |
|---|---|---|---|
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | 5 mg/mL (17 mM) | ||
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | Hydrazinecarboximidamide, 2-[(2,6-dichlorophenyl)methylene]-, acetate (1:1) |
|---|
Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
|---|---|---|---|---|
| Mass(mg) | 0.29113 | 2.9113 | 5.8226 | 8.7339 |
