SAR 20347 - Names and Identifiers
SAR 20347 - Physico-chemical Properties
Molecular Formula | C21H18ClFN4O4
|
Molar Mass | 444.84 |
Density | 1.445±0.06 g/cm3(Predicted) |
Boling Point | 698.3±65.0 °C(Predicted) |
Solubility | DMSO : 100 mg/mL (224.80 mM; Need ultrasonic and warming) |
pKa | 13.97±0.50(Predicted) |
Storage Condition | -20℃ |
Use | SAR-20347 is a potent dual inhibitor of JAK1 and tyrosine kinase 2 (TYK2). SAR-20347 dose dependently (1 nM-10 μM) inhibited JAK1- and/or TYK2-dependent signaling from the IL-12/IL-23, IL-22, and IFN-α receptors. In vivo, TYK2 mutant mice or treatment of wild-type mice with SAR-20347 significantly reduced IL-12-induced IFN-γ production and IL-22-dependent serum amyloid A to similar extents. |
Target | JAK1 JAK2 JAK3 TYK2 |
SAR 20347 - Reference
Reference Show more | 1: Works MG, Yin F, Yin CC, Yiu Y, Shew K, Tran TT, Dunlap N, Lam J, Mitchell T, Reader J, Stein PL, D'Andrea A. Inhibition of TYK2 and JAK1 ameliorates imiquimod-induced psoriasis-like dermatitis by inhibiting IL-22 and the IL-23/IL-17 axis. J Immunol. 2014 Oct 1;193(7):3278-87. doi:10.4049/jimmunol.1400205. Epub 2014 Aug 25. PubMed PMID: 25156366; PubMed Central PMCID: PMC4170002. |
SAR 20347 - Preparation solution concentration reference
| 1mg | 5mg | 10mg |
---|
1 mM | 2.248 ml | 11.24 ml | 22.48 ml |
5 mM | 0.45 ml | 2.248 ml | 4.496 ml |
10 mM | 0.225 ml | 1.124 ml | 2.248 ml |
5 mM | 0.045 ml | 0.225 ml | 0.45 ml |
Last Update:2024-01-02 23:10:35
SAR 20347 - Cell Experiment
Cells are plated in a 96-well v-bottom plate in starvation medium, incubated with SAR-20347 (0.5% DMSO) for 20 minutes at 37°C, 5% CO2, and stimulated with individual cytokines. P-STAT levels are measured in duplicate using MSD plates following the manufacturer's instructions (MSD).
Last Update:2023-08-16 21:32:38
SAR 20347 - Animal Experiment
Female 7 to 9-week old C57BL/6 mice are used. Mice are administered vehicle or 50 mg/kg SAR-20347 by oral gavage 30 minutes prior to application of 62.5 mg 5% imiquimod cream or control cream. Another dose of vehicle or 50 mg/kg SAR-20347 is given 5.5 hours following the first dose. This treatment is repeated for 5 days and on day 3 and 4, animals are injected with 100 uL saline to prevent dehydration. On the 6th day, the animals are euthanized and photographs are taken.
Last Update:2023-08-16 21:32:38
SAR 20347 - Reference Information
biological activity | SAR-20347 is an effective inhibitor of TYK2, JAK1, JAK2 and JAK3, with corresponding IC50 values of 0.6 nM, 23 nM, 26 nM and 41 nM. SAR-20347 can inhibit TYK2 and JAK1 mediated IL-12 and IFN-α signaling. |
target | TargetValue IL-12 () IFN-α () TYK2 (Cell-Free Assay) 0.6 nM JAK1 (Cell-Free Assay) 23 nM JAK2 (Cell-Free Assay) 26 nM |
Target | Value |
IL-12
()
| |
IFN-α
()
| |
TYK2
(Cell-free assay)
| 0.6 nM |
JAK1
(Cell-free assay)
| 23 nM |
JAK2
(Cell-free assay)
| 26 nM |
Last Update:2024-04-10 22:29:15