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Veledimex racemate

Catalog No. T13293 CAS 755013-59-3

Synonyms: RG-115932 racemate, INXN-1001 racemate

Veledimex racemate, the racemic form of veledimex, is an orally available, small-molecule ligand that activates the RheoSwitch Therapeutic System.

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Veledimex racemate, CAS 755013-59-3

Pack Size	Availability	Price/USD
25 mg	8-10 weeks	$ 1,970.00
50 mg	8-10 weeks	$ 2,580.00
100 mg	8-10 weeks	$ 3,400.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

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Description	Veledimex racemate, the racemic form of veledimex, is an orally available, small-molecule ligand that activates the RheoSwitch Therapeutic System.
In vitro	Interleukin 12 (IL-12) is a pro-inflammatory cytokine critical for stimulating anti-cancer immune responses. Ad-RTS-IL-12 is an adenovirus vector engineered to express hIL-12. Veledimex is an orally active small molecule diacylhydrazine, which can control the expression of target genes. The amount of gene product produced by the system and the duration of action depend on the dose level of veledimex and the time of administration.
In vivo	In murine models of melanoma, breast cancer, and glioma, the combined intratumoral injection of Ad-RTS-mIL-12 and oral dose of veledimex has shown to produce a dose-dependent antitumor effect. This response is associated with increased veledimex levels in plasma and tumor tissues. Notably, this combination therapy leads to a dose-responsive activation of IL-12 mRNA (switch on) and subsequent elevations of IL-12p70 within the tumor, while only minimally increasing its levels in the serum. Enhanced tumor levels of IL-12 are linked with an upsurge in CD8+ cytotoxic T cells and a reduction in regulatory T cells within the tumor microenvironment. Consequently, this regimen achieves dose-dependent reductions in tumor growth rates without significantly affecting body weight in both breast and melanoma syngeneic mouse models. Veledimex exhibits moderate to low oral bioavailability (-56% in mice and up to 17.4% in cynomolgus monkeys), alongside relatively low plasma clearance (1399 mL/h/kg in mice and 1170 mL/h/kg in monkeys), a high volume of distribution (20271 mL/kg in mice and 9180 mL/kg in monkeys), and prolonged terminal half-lives (-10 hours in mice and -30 hours in monkeys), following single oral or intravenous administrations.

Synonyms	RG-115932 racemate, INXN-1001 racemate
Molecular Weight	438.6
Formula	C27H38N2O3
CAS No.	755013-59-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Cai H, et al. Plasma Pharmacokinetics of Veledimex, a Small-Molecule Activator Ligand for a Proprietary GeneTherapy Promoter System, in Healthy Subjects. Clin Pharmacol Drug Dev. 2017 May;6(3):246-257.

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Keywords

Veledimex racemate 755013-59-3 Others RG-115932 racemate INXN-1001 racemate inhibitor inhibit

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