For research use only. Not for therapeutic Use.
Veledimex（Cat No.:I009537）, also known as RG-115932 and INXN-1001, is a drug candidate with immunostimulant properties. It belongs to the class of small-molecule inducers of gene expression (SMIGs). Veledimex works by activating a genetically engineered receptor system called the RheoSwitch Therapeutic System (RTS). This system allows for the regulation of gene expression in a controllable and reversible manner. Veledimex is being investigated for its potential therapeutic applications in various diseases, including cancer, by enabling the controlled expression of therapeutic genes and enhancing immune responses.
| Catalog Number | I009537 |
| CAS Number | 1093130-72-3 |
| Synonyms | INXN-1001; INXN 1001; INXN1001; RG-115932; RG 115932; RG115932; Veledimex.;(R)-N/’-(3,5-dimethylbenzoyl)-N/’-(2,2-dimethylhexan-3-yl)-2-ethyl-3-methoxybenzohydrazide |
| Molecular Formula | C27H38N2O3 |
| Purity | ≥95% |
| Target | Interleukin Related |
| Solubility | Soluble in DMSO, not in water |
| Storage | Store at -20°C |
| IUPAC Name | N'-(3,5-dimethylbenzoyl)-N'-[(3R)-2,2-dimethylhexan-3-yl]-2-ethyl-3-methoxybenzohydrazide |
| InChI | InChI=1S/C27H38N2O3/c1-9-12-24(27(5,6)7)29(26(31)20-16-18(3)15-19(4)17-20)28-25(30)22-13-11-14-23(32-8)21(22)10-2/h11,13-17,24H,9-10,12H2,1-8H3,(H,28,30)/t24-/m1/s1 |
| InChIKey | LZWZPGLVHLSWQX-XMMPIXPASA-N |
| SMILES | CCCC(C(C)(C)C)N(C(=O)C1=CC(=CC(=C1)C)C)NC(=O)C2=C(C(=CC=C2)OC)CC |
| Reference | 1:Clin Pharmacol Drug Dev. 2017 May;6(3):246-257. doi: 10.1002/cpdd.287. Epub 2016 Aug 4. Plasma Pharmacokinetics of Veledimex, a Small-Molecule Activator Ligand for a Proprietary Gene Therapy Promoter System, in Healthy Subjects.Cai H,Sun L,Miao J,Krishman S,Lebel F,Barrett JA, PMID: 27364771 DOI: 10.1002/cpdd.287 </br><span>Abstract:</span> Major obstacles to developing effective immunotherapy are the ability of tumors to escape the immune system and the toxicity associated with systemic administration. To overcome these challenges, a gene delivery platform technology, RheoSwitch Therapeutic System (RTS), has been developed to enable the regulated expression of a target gene, Ad-RTS-IL-12, administered intratumorally, where IL-12 expression is controlled via the administration of an oral activator ligand, veledimex. Pharmacokinetics in healthy human subjects indicated that veledimex plasma exposure increased with increasing dose after single- and multiple-dose administration in Labrasol slurry and F-22 capsule formulations. No apparent formulation or sex-related difference in veledimex pharmacokinetics (PK) was observed. Minimal or no plasma accumulation of veledimex was observed after once-daily oral administration for 14 days. Veledimex steady state in plasma was reached after 5 daily doses. Food consumption prior to veledimex administration prolonged and enhanced absorption with no impact on the elimination rate and extent of metabolism of veledimex, resulting in significantly increased systemic exposure to veledimex and its 2 major circulating metabolites. Overall, veledimex was well tolerated and exhibited a PK profile supportive of once-daily dosing. For enhanced efficacy, veledimex should be taken under fed conditions to ensure optimal absorption and sufficient systemic exposure.© 2016, The American College of Clinical Pharmacology. |
