UNC10217938A is a 3-deazapteridine analog with strong oligonucleotide enhancing effects. UNC10217938A enhances oligonucleotides effects by modulating their intracellular trafficking and release from endosomes. UNC10217938A also enhances the effects of antisense and siRNA oligonucleotides.
In Vitro
UNC10217938A strongly enhances luciferase induction in HelaLuc705 cells when used in the 5-25 µM range and are substantially more effective and potent than Retro-1. As compared to splice switching oligonucleotide (SSO) alone, UNC10217938A provids a 60-fold enhancement at 10 µM and 220-fold at 20 µM, in contrast to a 11-fold enhancement for 100 µM Retro-1. UNC10217938A can substantially enhance effects of receptor targeted oligonucleotide conjugates. UNC10217938A also can enhance effects of uncharged morpholino oligonucleotides as well as negatively charged oligonucleotides. Exposure of cells to UNC10217938A leads to a major reduction in co-localization of the TAMRA-oliogonucleotide with the late endosome marker Rab7, but had little effect on co-localization with the lysosomal marker LAMP-1. UNC10217938A causes partial release of oligonucleotide from late endosomes to the cytosol followed by nuclear accumulation. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Systemic treatment with SSO623 followed by administration of UNC10217938A (7.5 mg/kg; intravenous injection) produces distinct increases in EGFP fluorescence in liver, kidney and heart in EGFP654 mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organoheterocyclic compounds |
| 分類 | Pyridopyrazines |
| Subclass | Not available |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Pyridopyrazines |
| Alternative Parents | Secondary alkylarylamines Aminopyridines and derivatives Pyrazines Imidolactams Benzene and substituted derivatives Heteroaromatic compounds Carbamate esters Trialkylamines Azacyclic compounds Organic oxides Hydrocarbon derivatives Carbonyl compounds |
| Molecular Framework | Aromatic heteropolycyclic compounds |
| Substituents | Pyridopyrazine - Aminopyridine - Secondary aliphatic/aromatic amine - Monocyclic benzene moiety - Pyrazine - Pyridine - Imidolactam - Benzenoid - Heteroaromatic compound - Carbamic acid ester - Tertiary aliphatic amine - Tertiary amine - Azacycle - Secondary amine - Hydrocarbon derivative - Organic oxide - Organooxygen compound - Organonitrogen compound - Carbonyl group - Organic oxygen compound - Amine - Organic nitrogen compound - Aromatic heteropolycyclic compound |
| 説明 | This compound belongs to the class of organic compounds known as pyridopyrazines. These are aromatic heteropolycyclic compounds containing a pyridine ring fused to a pyrazine ring. |
| External Descriptors | Not available |
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| 溶解度 | DMSO : 10 mg/mL (21.90 mM; ultrasonic and warming and heat to 80°C) |
|---|---|
| 分子量 | 456.500 g/mol |
| XLogP3 | 4.100 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 7 |
| Rotatable Bond Count | 9 |
| Exact Mass | 456.227 Da |
| Monoisotopic Mass | 456.227 Da |
| Topological Polar Surface Area | 92.300 Ų |
| Heavy Atom Count | 34 |
| Formal Charge | 0 |
| Complexity | 622.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 1 |
