| Identification | Back Directory | [Name]
1-Piperazineacetamide, 4-[4-[[7-[(3,5-difluorophenyl)methyl]-7H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]phenyl]- | [CAS]
909561-15-5 | [Synonyms]
AS1810722
1-Piperazineacetamide, 4-[4-[[7-[(3,5-difluorophenyl)methyl]-7H-pyrrolo[2,3-d]pyrimidin-2-yl]amino]phenyl]- | [Molecular Formula]
C25H25F2N7O | [MOL File]
909561-15-5.mol | [Molecular Weight]
477.51 |
| Chemical Properties | Back Directory | [Boiling point ]
731.4±70.0 °C(Predicted) | [density ]
1.41±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 62.5 mg/mL (130.89 mM) | [form ]
Solid | [pka]
16.30±0.40(Predicted) | [color ]
Brown to black |
| Hazard Information | Back Directory | [Uses]
AS1810722 is an orally active and potent STAT6 inhibitor with an IC50 of 1.9 nM. AS1810722 shows a good profile of CYP3A4 inhibition. AS1810722, a derivative of fused bicyclic pyrimidine, has the potential for allergic diseases such as asthma and atopic diseases research[1]. | [in vivo]
AS1810722 (compound 24; 0.03-0.3 mg/kg; orally; 30 min before, and 24h and 48 h after OVA exposure) suppress eosinophil infiltration in the lung in a dose-dependent manner in an antigen-induced mouse asthmatic model[1].
?
AS1810722 inhibits in vitro Th2 differentiation with an IC50 of 2.4 nM without affecting type 1 helper T (Th1) cell differentiation and eosinophil infiltration in an antigen-induced mouse asthmatic model after oral administration[1].
| Animal Model: | Female Balb/c mice asthmatic model by intraperitoneal injection of ovalbumin (OVA)-containing aluminum hydroxide gel[1] | | Dosage: | 0.03-0.3 mg/kg | | Administration: | Orally; 30 min before, and 24 and 48 h after OVA exposure | | Result: | Suppressed eosinophil infiltration in the lung in a dose-dependent manner.
|
| [IC 50]
STAT6: 1.9 nM (IC50); CYP3A4 | [References]
[1] Shinya Nagashima, et al. Novel 7H-pyrrolo[2,3-d]pyrimidine derivatives as potent and orally active STAT6 inhibitors. Bioorg Med Chem. 2009 Oct 1;17(19):6926-36. DOI:10.1016/j.bmc.2009.08.021 |
|
| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
|