Oe-9000 is a blocker of voltage-gated Na(+) currents in neurons. It reversibly reduces rapidly activating and inactivating TTX-sensitive (TTX-S) Na(+) currents as well as slowly activating and inactivating tetrodotoxin-resistant (TTX-R) Na(+) currents at
Cefroxadine is an orally active cephalosporin antibiotic with a broad spectrum and a bactericidal action. It showed excellent results in the treatment of acute uncomplicated cystitis (AUC).
Heparin calcium (MW 15000-19000) 是一款高效的抗凝剂,能通过与抗凝血酶 III (ATIII) 形成可逆的复合物——肝素-抗凝血酶 III 复合物。该复合物进一步与凝血酶以及其他活化的凝血因子如IX、X、XI 和 XII 结合,以不可逆的方式使它们失活,从而有效防止纤维蛋白原转变为纤维蛋白。
FR900098 is a derivative of fosmidomycin that has antimalarial activity (IC50s = 170, 170, and 90 nM for HB3, A2, and Dd2 P. falciparum strains, respectively). FR900098 inhibits DOXP reductoisomerase, a key enzyme in the non-mevalonate pathway of isoprenoid biosynthesis, in vitro in a dose-dependent manner. FR900098 (>10 mg/kg, i.p.) eradicated P. vinckei parasites within four days in mice.
CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation by IL-2 expression[1]. CC-90005 shows the exquisite selectivity of CC-90005, with IC50s for all other family members of >3 μM[1].CC-90005 is a moderate inhibitor of both CYP2C9 (IC50=8 μM) and CYP2C19 (IC50=5.9 μM) in human liver microsomes[1].CC-90005 inhibits IL-2 expression in LRS_WBC human PBMCs, with an IC50 of 0.15 μM[1].CC-90005 (1-10 μM; 24 h) inhibits T cell proliferation in PBMCs by 51% at 1 μM and 88% at 3 μM[1]. CC-90005 (3-30 mg kg; p.o. twice daily for 4 days) significantly reduces the popliteal lymph node (PLN) size in a model of chronic T cell activation[1].CC-90005 (100 mg kg; a single p.o.) significantly inhibits plasma and spleen IL-2 release by 51 and 54%, respectively[1].CC-90005 exhibits reasonable oral bioavailability (66 and 46%) and Cmax (1.18 and 1.2 μM) following oral administration (10 and 3 mg kg) in rat and dog, respectively[1].CC-90005 exhibits the mean residence time (0.52 and 2.0 h), CL (69.1 and 20.5 mL min kg) and Vss (2.11 and 2.44 L kg) following intravenous administration (2 and 1 mg kg) in rat and dog, respectively[1]. [1]. Papa P, et, al. Discovery of the Selective Protein Kinase C-θ Kinase Inhibitor, CC-90005. J Med Chem. 2021 Aug 26;64(16):11886-11903.