765914-60-1
765914-60-1 structure
- Name: Emprumapimod
- Chemical Name: Emprumapimod
- CAS Number: 765914-60-1
- Molecular Formula: C24H29F2N5O3
- Molecular Weight: 473.52
- Catalog: Signaling Pathways MAPK/ERK Pathway p38 MAPK
- Create Date: 2022-05-22 12:30:31
- Modify Date: 2024-01-17 16:54:27
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Emprumapimod is a potent, orally bioavailable and selective inhibitor of p38α MAPK directly inhibits LPS-induced IL-6 production from RPMI-8226 cell (IC50=100 pM). Emprumapimod can be used for the research of dilated cardiomyopathy and acute inflammatory pain[1][2].
| Name | Emprumapimod |
|---|
| Description | Emprumapimod is a potent, orally bioavailable and selective inhibitor of p38α MAPK directly inhibits LPS-induced IL-6 production from RPMI-8226 cell (IC50=100 pM). Emprumapimod can be used for the research of dilated cardiomyopathy and acute inflammatory pain[1][2]. |
|---|---|
| Related Catalog | |
| Target |
p38α:100 pM (IC50) |
| In Vivo | In SCID-beige mice, LPS (3 μg/kg) induced IL-6 (7897±827 pg/mL) and TNF-α (1922±282 pg/mL) after 2 hours and these cytokines are inhibited by oral administration of Emprumapimod (ARRY-797; 30 mg/kg) by 91% and 95%, respectively[1]. In MM xenograft models, Emprumapimod (30 mg/kg, BID, PO) inhibits RPMI 8226 tumor growth by 72% as a single agent and by 56% when LPS is administered to stimulate growth in vivo[1]. Emprumapimod also inhibits LPS-induced phosphorylation of p38 in RPMI-8226 xenografts[1]. Treatment of LmnaH222P/H222P mice with the p38α inhibitor Emprumapimod (ARRY-371797; 30 mg/kg; orally twice daily; for 4 weeks initiated at 16 weeks of age) prevents left ventricular (LV) dilatation and deterioration of fractional shortening (FS). LV end-diastolic diameter (LVEDD) and LV end-systolic diameter (LVESD) in LmnaH222P/H222P mice treated with Emprumapimod are significantly smaller and FS is significantly increased compared with the placebo-treated mice[2]. Animal Model: LmnaH222P/H222P mice were[2] Dosage: 30 mg/kg Administration: Administered orally by gavage starting when mice were 16 weeks of age and continuing until 20 weeks of age Result: There were significant increases in LVEDD and LVESD as well as a decrease in FS, a parameter directly proportional to the LV ejection fraction. |
| References |
| Molecular Formula | C24H29F2N5O3 |
|---|---|
| Molecular Weight | 473.52 |