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Purity: =99.15%
UNC10217938A (UNC7938), a 3-deazapteridine analog with high oligonucleotide enhancing effects, is a destabilizer of the endosome membrane that can enhance the endosome-leakage activity of cell-penetrating peptides and facilitating the endosomal escape of macromolecules initially internalized by mammalian cells via endocytosis.
| ln Vitro |
Compared to Retro-1, UNC10217938A is significantly more effective and potent as it significantly increases luciferase induction in HelaLuc705 cells within the 5-25 µM range. UNC10217938A offers a 60-fold enhancement at 10 µM and a 220-fold enhancement at 20 µM when compared to splice switching oligonucleotide (SSO) alone[1]. In contrast, 100 µM Retro-1 only delivers an 11-fold enhancement. Receptor-targeted oligonucleotide conjugates can have their effects significantly increased by UNC10217938A. UNC10217938A has the ability to amplify the effects of both negatively charged and uncharged morpholino oligonucleotides[1]. Cells exposed to UNC10217938A exhibit a significant decrease in TAMRA-oligonucleotide co-localization with the late endosome marker Rab7, but little change in co-localization with the lysosomal marker LAMP-1. UNC10217938A induces a partial release of oligonucleotides into the cytosol from late endosomes through nuclear accumulation[1].
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| ln Vivo |
In EGFP654 mice, systemic treatment with SSO623 and intravenous injection of UNC10217938A (7.5 mg/kg) result in discernible increases in EGFP fluorescence in the liver, kidney, and heart[3].
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| References |
| Molecular Formula |
C26H28N6O2
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|---|---|
| Molecular Weight |
456.5395
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| Exact Mass |
456.227
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| CAS # |
1347749-97-6
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| PubChem CID |
57402790
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
34
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| Complexity |
622
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C([H])([H])C([H])([H])[H])C(N([H])C1C([H])=C(C2=C(N=1)N=C(C1C([H])=C([H])C([H])=C([H])C=1[H])C(C1C([H])=C([H])C([H])=C([H])C=1[H])=N2)N([H])C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])[H])=O
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| InChi Key |
HHICWLZMNOCMIQ-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
ethyl N-[8-[2-(dimethylamino)ethylamino]-2,3-diphenylpyrido[2,3-b]pyrazin-6-yl]carbamate
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| Synonyms |
UNC 7938UNC 10217938A UNC7938 UNC 10217938A UNC-7938UNC10217938AUNC-10217938-A
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~10 mg/mL (~21.90 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.19 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 + to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1904 mL | 10.9519 mL | 21.9039 mL | |
| 5 mM | 0.4381 mL | 2.1904 mL | 4.3808 mL | |
| 10 mM | 0.2190 mL | 1.0952 mL | 2.1904 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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