Veledimex S enantiomer(INXN-1001 S enantiome)

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CAS NO:

1093131-03-3

包装与价格：

包装	价格(元)
10mM (in 1mL DMSO)	询价
1mg	询价
5mg	询价
10mg	询价

Veledimex S 对映体 (INXN-1001 S enantiomer) 是 veledimex 的 S 对映体。 Veledimex 是专有基因治疗启动子系统的口服激活剂配体，也是 CYP3A4/5 的中度抑制剂和底物。

Cas No.	1093131-03-3
别名	INXN-1001 (S enantiomer); RG-115932 (S enantiomer)
Canonical SMILES	O=C(NN(C(C1=CC(C)=CC(C)=C1)=O)[C@H](C(C)(C)C)CCC)C2=CC=CC(OC)=C2CC
分子式	C₂₇H₃₈N₂O₃
分子量	438.6
溶解度	Soluble in DMSO
储存条件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	Veledimex S enantiomer is the S enantiomer of veledimex. Veledimex is an oral activator ligand for a proprietary gene therapy promoter system, and a moderate inhibitor of and substrate for CYP3A4/5. Veledimex generally has moderate to low oral bioavailability after a single oral administration in mice and monkeys (∼56% in mice and up to 17.4% in cynomolgus monkeys) with mostly low plasma clearance (1399 and 1170 mL/h per kilogram in mice and monkeys, respectively), high volume of distribution (20271 and 9180 mL/h per kilogram in mice and monkeys, respectively), and long terminal half-lives (∼10 hours in mice and ∼30 hours in monkeys) after intravenous administration[1]. Ad-RTS-mIL-12 + veledimex have demonstrated a dose-related increase in tumor IL-12 mRNA and IL-12 protein expression. Discontinuation of veledimex resulted in a return to baseline IL-12 mRNA and protein expression in numerous syngeneic mouse tumor models. Veledimex crosses the blood-brain-barrier in both naive and orthotopic GL-261 mice with increased brain tissue level of ∼6 fold observed in tumor bearing vs. normal mice. Ad-RTS-mIL-12 + veledimex demonstrate a dose-related increase in survival without significant adverse events[2]. [1]. Cai H, et al. Plasma Pharmacokinetics of Veledimex, a Small-Molecule Activator Ligand for a Proprietary Gene Therapy Promoter System, 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 OF GLIOMA. Neuro Oncol. 2015 Nov; 17(Suppl 5): v113.