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- Yuki Sasaki, .et al. Blockade of the CXCR3/CXCL10 axis ameliorates inflammation caused by immunoproteasome dysfunction, JCI Insight, 2022, Apr 8;7(7) PMID: 35393946
- Yutian Lei, .et al. A multicenter blinded preclinical randomized controlled trial on Jak1/2 inhibition in MRL/MpJ-Fas lpr mice with proliferative lupus nephritis predicts low effect size, Kidney Int, 2021, Feb 16 PMID: 33607177
Biological Activity
Baricitinib, also known as INCB028050 or LY3009104, is a selective orally bioavailable JAK1/JAK2 inhibitor with nanomolar potency against JAK1 (5.9 nM) and JAK2 (5.7 nM).
Targets
| Target | Value |
|---|---|
| JAK2 | IC50: 5.7nM |
| JAK1 | IC50: 5.9nM |
| TYK2 | IC50: 53nM |
| JAK3 | IC50: >400nM |
| Chk2 | IC50: >1μM |
| c-Met | IC50: >10μM |
| In vitro (25°C) | DMSO | 65 mg/mL (175 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
| In vivo | 2% DMSO+30% PEG 300+5% Tween 80+ddH2O | 4 mg/mL | |
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 26.93 mL | 134.63 mL | 269.25 mL |
| 0.5 mM | 5.39 mL | 26.93 mL | 53.85 mL |
| 1 mM | 2.69 mL | 13.46 mL | 26.93 mL |
| 5 mM | 0.54 mL | 2.69 mL | 5.39 mL |
*The above data is based on the productmolecular weight 371.4 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A11329 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 1187594-09-7 |
| Formula | C16H17N7O2S |
| M. Wt | 371.4 |
| Purity | >98% |
| Synonyms | INCB28050, LY3009104 |
| SMILES | CCS(=O)(=O)N1CC(C1)(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3 |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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