PKG-drug-G1-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPKG drug G1Cat. No.: HY-112197CAS No.: 374703-78-3分式: CHNOS分量: 257.31作靶点: Others作通路: Others储存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 103 mg/mL (400.30 mM)* means soluble, but saturation unknown

2、.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.8864 mL 19.4318 mL 38.8636 mL5 mM 0.7773 mL 3.8864 mL 7.7727 mL10 mM 0.3886 mL 1.9432 mL 3.8864 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 PKG drug G1 靶向作于 PKG I。PKG drug G1 通过 C42 PKGI 依赖性机制有助于管舒张和压降低。IC50 & Target PKG

3、I 1体内研究PKG drug G1 induces vasodilation of isolated resistance blood vessels and blood pressure lowering in amouse model of angiotensin IIinduced hypertension. PKG drug G1 efficiently relaxes WT but not knockin(KI) vessels, which is then assessed in a murine model of hypertension. PKG drug G1 lowers

4、 blood pressure1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEin hypertensive WT, but not KI, mice in vivo. PKG drug G1 is tested in vivo in healthy mice implanted withtelemetric devices that allow blood pressure and heart rate to be constantly monitored. PKG drug G1 orvehicle control is administr

5、ated by intraperitoneal injection, and the acute impact on hemodynamicsassessed. PKG drug G1 administered at 7.4 mg/kg does not decrease blood pressure, but there is aconcomitant reflex tachycardia. When this is repeated using 14.8 mg/kg dose of PKG drug G1, again bloodpressure is not altered-but th

6、is higher dose induces a potentiated increase in heart rate 1.PROTOCOLAnimal Mice 1Administration 1 Mice constitutively expressing PKG I Cys42Ser are generated on a pure C57BL/6 background. Age-matched and body weightmatched WT or PKG I Cys42Ser KI male mice are used in all studies. Bloodpressure an

7、d heart rate are assessed by radio telemetry in conscious freely moving mice. Alzet osmotic mini-pumps are used to deliver angiotensin II at 1.1 mg/kg per day in some studies. PKG drug G1 is deliveredintraperitoneally (3.7-14.8 mg/kg) or orally (20 mg/kg) in some studies. To deliver PKG drug G1 oral

8、ly,without stress or risk of dislodging the telemetric probe catheter, it is provided suspended in water and set ingelatin flavored with sodium saccharin 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Burgoyne JR, et al. Proof of Principle for a Novel Class of Antihypertensives That Target the Oxidative Activation of PKG I (ProteinKinase G I). Hypertension. 2017 Sep;70(3):577-586.McePdfHeightCaution: Product has not been fully validated for medical appli