sd rats

Lerisetron is an antagonist of serotonin type 3 (5-HT3) receptor, with antiemetic activity.

LZ-007 is an agonist of the Farnesoid X receptor (FXR), with an EC50 of 51 nM as determined by TR-FRET assay, and an EC50 of 76 nM in HepG2 cells. It exhibits favorable pharmacokinetic properties in SD rats and can improve metabolic dysfunction-associated steatohepatitis induced by high-fat diets and CCl4 in mice.

FLT3-IN-28 (Compound 12y) is an orally active FLT3 inhibitor with antitumor properties. It selectively targets cancer cells with FLT3 internal tandem duplication (ITD) mutations, demonstrating IC50 values of 85, 290, 130, 65, and 220 nM against BaF3-FLT3-ITD, BaF3-TEL-VEGFR2, MV4-11, MOLM-13, and MOLM-14 cell lines, respectively. These lines include acute myeloid leukemia (AML) cells harboring FLT3-ITD mutations such as MV4-11 and MOLM-13 14. The compound also reduces phosphorylation levels of FLT3 and STAT5 in MOLM-13 cells, leading to cell cycle arrest and apoptosis. With an oral bioavailability of 19.2% in SD rats, FLT3-IN-28 extends survival in a dose-dependent manner in MOLM-13 xenografted NSG mouse models. It holds promise for research in FLT3-ITD-related cancer studies.

VISTA-IN-4 (Compound B3) is an orally active inhibitor of the immune checkpoint protein VISTA, with a KD of 0.452 μM. It degrades VISTA in HepG2 cells with a degradation rate of 77% at a concentration of 5 μM. VISTA-IN-4 counteracts VISTA-mediated immune suppression, restoring T cell activity and promoting the release of cytokine IL-2. Additionally, it exhibits antitumor activity in CT26 xenograft mouse models and demonstrates favorable pharmacokinetic properties, with good oral serum exposure in SD rats, reflected by an AUC(0-t) of 412.9 mg·h mL.

S-8510 is a GABA-A receptor inverse agonist. S-8510 selectively potentiated pentylenetetrazol-induced convulsion without affecting minimal electroconvulsive shock- or strychnine-induced convulsion in ddY mice. S-8510 ameliorated memory impairment induced

Ensartinib (X-396) is a potent and orally active dual ALK MET inhibitor for the treatment of ALK-positive non-small cell lung cancer (NSCLC).

Isofuranodiene protects GalN LPS-induced liver injury in SD rats, it may be a potential functional food ingredient for the prevention and treatment of liver diseases. Isofuranodiene has anticancer activity, by inhibiting the proliferation and inducing apo