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Guanabenz Acetate(BR-750 Wy8678 acetate)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Guanabenz Acetate(BR-750 Wy8678 acetate)图片
CAS NO:23256-50-0
规格:≥98%
包装与价格:
包装价格(元)
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
2g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)291.13
FormulaC8H8Cl2N4.C2H4O2
CAS No.23256-50-0
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 58 mg/mL (199.2 mM)
Water: <1 mg/mL
Ethanol: 5 mg/mL (17.2 mM)
Solubility (In vivo)4% DMSO+30% PEG 300+ddH2O: 5mg/mL
SynonymsBR750; WY-8678, WY 8678, BR-750; Wy-8678; BR 750; Wy 8678; WY-8678 Acetate; WY8678, EIPA
实验参考方法
In Vitro

In vitro activity: 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. 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.

In VivoGuanabenz 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. Guanabenz injected at doses of 0.5 mg/kg and above lowers blood pressure and heart rate in unanesthetized hypertensive rats and dogs.
Animal modelRats and dogs
Formulation & Dosage0.1, 0.5 mg/kg
References

J Biol Chem. 2000 Jan 28;275(4):2376-80; J Pharmacol Exp Ther. 1970 Feb;171(2):276-87.