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TH5487 is a novel, potent and selective 8-oxoguanine DNA glycosylase 1 (OGG1) inhibitor with an IC50 of 342 nM. TH5487 inhibits DNA repair, prevents OGG1 from identifying its DNA substrate, and alters OGG1 chromatin dynamics, all of which lead to the suppression of genes involved in the proinflammatory pathway.
| Targets |
OGG1 ( IC50 = 342 nM )
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|---|---|
| ln Vitro |
TH5487 raises the melting temperature of OGG1 in human cells. TH5487 hinders the KBrO3-induced repair of genomic 8-oxoG.In living cells, TH5487 blocks OGG1 from attaching to its genomic substrate.[1]
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| ln Vivo |
In order to evaluate TH5487's potential to downregulate chemotactic (C-C and C-X-C) mediators in vivo, we subject mouse lungs to TNFα challenge and examine the expression of proinflammatory mediators in the gene expression profile. Since TH5487 works well in vivo, it may be possible to treat inflammatory diseases with this substance. [1]
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| Cell Assay |
Cell Line: Murine airway epithelial cell line (MLE 12); Diploid human small-airway epithelial cell (hSAECs)
Concentration: 5 μM Incubation Time: 1 hour Result: Inhibited proinflammatory gene expression dose-dependently. |
| Animal Protocol |
mice (50% female and 50% male) of which lungs are TNFα-challenged intranasally (20 ng/ml)
30 mg/kg IP |
| References |
| Molecular Formula |
C₁₉H₁₈BRIN₄O₂
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|---|---|
| Molecular Weight |
541.180295467377
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| Exact Mass |
539.97
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| Elemental Analysis |
C, 42.17; H, 3.35; Br, 14.76; I, 23.45; N, 10.35; O, 5.91
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| CAS # |
2304947-71-3
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| Appearance |
Solid powder
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| SMILES |
C1CN(CCC1N2C3=C(C(=CC=C3)Br)NC2=O)C(=O)NC4=CC=C(C=C4)I
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| InChi Key |
FZLKVWWPFOLPKF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H18BrIN4O2/c20-15-2-1-3-16-17(15)23-19(27)25(16)14-8-10-24(11-9-14)18(26)22-13-6-4-12(21)5-7-13/h1-7,14H,8-11H2,(H,22,26)(H,23,27)
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| Chemical Name |
4-(4-bromo-2-oxo-3H-benzimidazol-1-yl)-N-(4-iodophenyl)piperidine-1-carboxamide
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| Synonyms |
TH 5487; TH5487; TH-5487
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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: 10~25 mg/mL (18.5~46.20 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.84 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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. Solubility in Formulation 2: 5%DMSO+ Corn oil: 1.5mg/ml (2.77mM) (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8478 mL | 9.2391 mL | 18.4781 mL | |
| 5 mM | 0.3696 mL | 1.8478 mL | 3.6956 mL | |
| 10 mM | 0.1848 mL | 0.9239 mL | 1.8478 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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