Veledimex-INXN-1001-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEVeledimexCat. No.: HY-16785CAS No.: 1093130-72-3Synonyms: INXN-1001; RG-115932分式: CHNO分量: 438.6作靶點: Interleukin Related; Cytochrome P450作通路: Immunology/Inflammation; Metabolic Enzyme/Protease儲存式: Powder -20C 3 years4C 2 yearsIn

2、solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 25 mg/mL (57.00 mM; Need ultrasonic)H2O : 90% corn oilSolubility: 2.5 mg/mL (5.70 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Veledimex種專有基因治療啟動系統(tǒng)的激活劑配體，也是CYP3A4/5的溫和抑制劑配體。體內(nèi)研究 Veledimex generally has mo

3、derate to low oral bioavailability after a single oral administration in mice andmonkeys (-56% in mice and up to 17.4% in cynomolgus monkeys) with mostly low plasma clearance (1399and 1170 mL/h per kilogram in mice and monkeys, respectively), high volume of distribution (20271 and 9180mL/h per kilog

4、ram in mice and monkeys, respectively), and long terminal half-lives (-10 hours in mice and -30hours in monkeys) after intravenous administration 1. Ad-RTS-mIL-12 + veledimex have demonstrated adose-related increase in tumor IL-12 mRNA and IL-12 protein expression. Discontinuation of veledimexresult

5、ed in a return to baseline IL-12 mRNA and protein expression in numerous syngeneic mouse tumormodels. Veledimex crosses the blood-brain-barrier in both naive and orthotopic GL-261 mice with increasedbrain tissue level of -6 fold observed in tumor bearing vs. normal mice. Ad-RTS-mIL-12 + veledimexdem

6、onstrate a dose-related increase in survival without significant adverse events 2.REFERENCES1. Cai H, et al. Plasma Pharmacokinetics of Veledimex, a Small-Molecule Activator Ligand for a Proprietary Gene Therapy PromoterSystem, in Healthy Subjects. Clin Pharmacol Drug Dev. 2017 May;6(3):246-257.2. John A. Barrett, INTRATUMORAL REGULATED EXPRESSION OF IL-12 AS A GENE THERAPY APPROACH TO TREATMENT OFGLIOMA. Neuro Oncol. 2015 Nov; 17(Suppl 5): v113.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only