UNC10217938A

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.

Product information

CAS Number: 1347749-97-6

Molecular Weight: 456.54

Formula: C26H28N6O2

Chemical Name: ethyl N-(8-{[2-(dimethylamino)ethyl]amino}-2,3-diphenylpyrido[2,3-b]pyrazin-6-yl)carbamate

Smiles: CCOC(=O)NC1C=C(NCCN(C)C)C2N=C(C(=NC=2N=1)C1C=CC=CC=1)C1C=CC=CC=1

InChiKey: HHICWLZMNOCMIQ-UHFFFAOYSA-N

InChi: InChI=1S/C26H28N6O2/c1-4-34-26(33)29-21-17-20(27-15-16-32(2)3)24-25(28-21)31-23(19-13-9-6-10-14-19)22(30-24)18-11-7-5-8-12-18/h5-14,17H,4,15-16H2,1-3H3,(H2,27,28,29,31,33)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 10 mg/mL (21.90 mM; ultrasonic and warming and heat to 80°C).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

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.

References:

1. Yang B, et al. High-throughput screening identifies small molecules that enhance the pharmacological effects of oligonucleotides. Nucleic Acids Res. 2015 Feb 27;43(4):1987-96.

Products are for research use only. Not for human use.