BET-IN-13
Modify Date: 2024-01-02 13:00:36
BET-IN-13 structure
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Common Name | BET-IN-13 | ||
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| CAS Number | 2506823-08-9 | Molecular Weight | 497.56 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C28H23N3O4S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of BET-IN-13BET-IN-13 is a potent BET inhibitor with an IC50 value of 1.6 nM. BET-IN-13 reduces LPS-induced TNF-α, IL-1β, IL-6, and NOS2 mRNA expression levels. BET-IN-13 shows anti-inflammatory activity. BET-IN-13 has the potential for the research of acute liver injury[1]. |
| Name | BET-IN-13 |
|---|
| Description | BET-IN-13 is a potent BET inhibitor with an IC50 value of 1.6 nM. BET-IN-13 reduces LPS-induced TNF-α, IL-1β, IL-6, and NOS2 mRNA expression levels. BET-IN-13 shows anti-inflammatory activity. BET-IN-13 has the potential for the research of acute liver injury[1]. |
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| Related Catalog | |
| Target |
BRD4 BD1:57.4 nM (IC50) BRD4 BD2:44.4 nM (IC50) BRD2 BD1:79.3 nM (IC50) BRD2 BD2:27.5 nM (IC50) BRD3 BD1:45.6 nM (IC50) BRD3 BD2:18.9 nM (IC50) BRDT BD1:87.0 nM (IC50) BRDT BD2:43.4 nM (IC50) |
| In Vitro | BET-IN-13 (compound 28) (1.1, 3.3, 10 µM, 2+6 h) 降低 RAW264.7 细胞中 LPS (500 ng/ml) 诱导的 TNF-α、IL-1β、IL-6 和 NOS2 mRNA 的表达水平[1]。 RT-PCR[1] Cell Line: RAW264.7 cells Concentration: 1.1, 3.3, 10 µM Incubation Time: Pre-treated for 2 h before stimulating with LPS for 6 h Result: Significantly reduced LPS (500 ng/ml) induced TNF-α, IL-1β, IL-6 and NOS2 mRNA expression levels in a dose-dependent manner. |
| In Vivo | BET-IN-13 (3 mg/kg；静脉注射；一次) 在小鼠中显示出良好的药代动力学 (PK) 特性，T1/2 为 0.69 h，AUCINF-obs 为 609 h*ng/mL 和 Vss 为 1717 mL/kg[1]。 BET-IN-13 (37.5、75 mg/kg；腹腔注射；一次) 降低 LPS/D-GalN(d-gaiactosamine)诱导的急性肝衰竭 (ALF) 小鼠的炎症和肝损伤而无明显毒性[1]。 Animal Model: 20-22g, Female C57BL/6J mice (LPS/D-GalN(d-gaiactosamine)-induced acute liver failure (ALF))[1] Dosage: 37.5, 75 mg/kg Administration: I.p.; once Result: Reduced inflammatory responses associated with LPS/GalN-induced acute liver failure with the survival rate increased significantly to 69.2% for37.5 mg/kg and to 84.6% for 75 mg/kg. |
| References |
| Molecular Formula | C28H23N3O4S |
|---|---|
| Molecular Weight | 497.56 |