AS2677131
AS2677131 is a potent and orally active PIKfyve inhibitor. AS2677131 inhibits f IL-12p40, IL-6 and IL-1β through a PIKfyve-c-Rel pathway. AS2677131 selectively inhibits DNA-binding activity of c-Rel to IL-12p40 and IL-1β promoter. AS2677131 inhibits MHC class II expression on B cells. AS2677131 can be used for the researches of inflammation and immunology, such as arthritis.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 2171502-44-4
- Fòrmula: C27H30N6O2
- Peso molecular:470.57
-
Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
- Protocolo
- Pureza y Documentación
- Referencias
-
Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[1]|
IL-12 |
IL-1β |
IL-6 |
MHC II |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| RAW264.7 | IC50 |
2.4 nM
Compound: 69; AS2677131
|
Antiinflammatory activity in mouse RAW264.7 cells assessed as effect on LPS induced IL-12p40 level measured after 24 hrs by RT-qPCR analysis
Antiinflammatory activity in mouse RAW264.7 cells assessed as effect on LPS induced IL-12p40 level measured after 24 hrs by RT-qPCR analysis
|
[PMID: 37981443] |
In Vitro
AS2677131 inhibits IL-12p40 production with an IC50 of 2.4 nM and inhibits IL-1β and IL-6 levels in RAW264.7 mouse macrophage cells[1].
AS2677131 (0.1-10000 nM) inhibits IL-12p40 and IL-6 in mouse peritoneal macrophages[1].
AS2677131 (0.1-10000 nM) inhibits IL-12p40 and IL-6 in mouse bone marrow-derived dendritic cells[1].
AS2677131 (10 μM) shows no significant effect on intracellular Ca2+ influx in Ramos cells[1].
AS2677131 (200 nM) inhibits PI (3,5) P2 production by more than 90% in RAW264.7 cells[1].
AS2677131 (100 nM, 2 h) increases the size of RAW264.7 cells and induces numerous small vesicles in the cytoplasm[1].
AS2677131 (10-100 nM, 2h) decreases the promoter activity and inhibits the binding of c-Rel to the promoters of IL-12p40 and IL-1β in RAW264.7 cells[1].
AS2677131 (100 nM, 2 h) reduces p-Akt levels in RAW264.7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:RAW264.7 cells
-
Concentration:100 nM
-
Incubation Time:2 h
-
Result:Reduced p-Akt levels.
In Vivo
AS2677131 (1-10 mg/kg, p.o.) reduces the expression of MHC class II molecules on the surface of CD45R+ B cells in rats[1].
AS2677131 (1-10 mg/kg, p.o., daily for 24 days) reduces inflammation in rats with adjuvant-induced arthritis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Rats with adjuvant-induced arthritis[1]
-
Dosage:1, 3 and 10 mg/kg
-
Administration:Orally administration, daily for 24 days
-
Result:Reduced paw swelling (swelling inhibition rates of 34.3% and 78.3% at doses of 3 and 10 mg/kg, respectively).
Reversed body weight loss.
Decreased joint histological scores (including bone destruction, cartilage destruction, synovial thickening, and inflammatory cell infiltration.
Reduced the proportion of CD3-CD45RA+CD62Llow activated B cells in peripheral blood.
Chemical Information
-
No. CAS 2171502-44-4
-
Peso molecular 470.57
-
Fòrmula C27H30N6O2
-
SMILES
O=C(C1=CC=C(NC(C)=C2CC)C2=N1)NC3=CN=CC(C4=CC=C(N5C[C@@H](C)O[C@@H](C)C5)N=C4)=C3
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AS2677131 Related Classifications
HY-123876 Related Classifications
Powered by Bioz