SAR-20347
SAR-20347 Basic information
- Product Name:
- SAR-20347
- Synonyms:
-
- SAR-20347
- CPDD1211
- 2-(2-chloro-6-fluorophenyl)-5-((4-(morpholine-4-carbonyl)phenyl)amino)oxazole-4-carboxamide
- 2-(2-chloro-6-fluorophenyl)-5-({4-[(morpholin-4-yl)carbonyl]phenyl}amino)-1,3-oxazole-4-carboxylic acid amide
- CS-2527
- SAR-20347;SAR 20347;SAR20347
- 4-Oxazolecarboxamide, 2-(2-chloro-6-fluorophenyl)-5-[[4-(4-morpholinylcarbonyl)phenyl]amino]-
- inhibit,SAR 20347,Janus kinase,JAK,SAR-20347,Inhibitor
- CAS:
- 1450881-55-6
- MF:
- C21H18ClFN4O4
- MW:
- 444.84
- Product Categories:
-
- JAK1 & TYK2
- Mol File:
- 1450881-55-6.mol
SAR-20347 Chemical Properties
- Boiling point:
- 698.3±65.0 °C(Predicted)
- Density
- 1.445±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:94.5(Max Conc. mg/mL);212.43(Max Conc. mM)
- form
- A solid
- pka
- 13.97±0.50(Predicted)
- color
- Light yellow to yellow
- InChI
- 1S/C21H18ClFN4O4/c22-14-2-1-3-15(23)16(14)19-26-17(18(24)28)20(31-19)25-13-6-4-12(5-7-13)21(29)27-8-10-30-11-9-27/h1-7,25H,8-11H2,(H2,24,28)
- InChIKey
- HEDPDFHTQKEORT-UHFFFAOYSA-N
- SMILES
- Fc1c(c(ccc1)Cl)c2nc(c([o]2)Nc3ccc(cc3)C(=O)N4CCOCC4)C(=O)N
SAR-20347 Usage And Synthesis
Uses
SAR-20347 is a small molecule inhibitor with specificity for JAK1 and tyrosine kinase 2 (TYK2).
Biochem/physiol Actions
SAR-20347 is an orally active, ATP-competitive, TYK2- and JAK1-selective tyrosine kinase inhibitor (IC50 = 13 nM/TYK2 & 59 nM/JAK1 vs. 0.88 μM/JAK2 & 1.44 μM/JAK3 with 10 μM ATP) that effectively inhibits cellular TYK2- (IL12-induced pSTAT4 IC50 = 107 nM/CD4+ cells, 126 nM/NK-92) and JAK1- (IL6-induced pSTAT3 IC50 = 345 nM/TF-1, 407 nM/CD14+ cells) mediated signaling with little affinity toward 72 other kinases. SAR-20347 suppresses IL22-induced serum amyloid A (by 44%; 50 mg/kg p.o. 30 min prior to 10 μg IL22 i.p.) and alleviates imiquimod-induced psoriasis-like dermatitis (30 min prior and 5 h post daily 62.5 mg 5% imiquimod cream) in mice in vivo.
in vivo
60 mg/kg SAR-20347 inhibits the production of IFN-γ in the serum by 91% compare to vehicle-treated animals, demonstrating that SAR-20347 can inhibit TYK2 signaling in vivo. SAR-20347 treatment significantly reduces IL-17 production as measured by average signal intensity, consistent with the gene expression analysis[1].
IC 50
Tyk2: 0.6 nM (IC50); JAK1: 23 nM (IC50); JAK2: 26 nM (IC50); JAK3: 41 nM (IC50)
SAR-20347Supplier
- Tel
- 400-6206333 13167063860
- anhua.mao@aladdin-e.com
- Tel
- 13816107857
- sales@fortunechem-sh.com
- Tel
- 18149758185 18149758185;
- sales-cpd@caerulumpharma.com
- Tel
- 400-400-164-7117 18317119277
- product02@bidepharm.com
- Tel
- +86-2332782371 +86-18120098618
- sales@adobechem.com