Isavuconazole shows good activity against all Candida spp., with active MIC50 of 0.004 mg/L. The MIC50s/MIC90s range from 0.002/0.004 mg/L for C. albicans to 0.25/0.5 mg/L for C. glabrata. Isavuconazole has potent in vitro activity against most common Aspergillus species, Purpureocillium lilacinum, and Scedosporium apiospermum. Isavuconazole shows potent activity against molds, yeasts, and dimorphic fungi. Rhizopus isolates have MIC values to isavuconazole as low as 0.12 µg/mL with others as high as 32 µg/mL. Isavuconazole shows potent activity against molds, yeasts, and dimorphic fungi. Rhizopus isolates have MIC values to isavuconazole as low as 0.12 µg/mL with others as high as 32 µg/mL.
|Cell lines||L‐type Ca2+ channels|
|Preparation method||The in vitro effects of isavuconazole on a panel of human cardiac Ca2+, K+, and Na+ channels were assessed by recording transmembrane currents in cultured cells stably transfected with genes encoding each channel.|
|Concentrations||1, 3, 10, or 30 μM|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||10 mM in DMSO|
QT Interval Shortening With Isavuconazole: In Vitro and In Vivo Effects on Cardiac Repolarization.
Keirns J, et al. Clin Pharmacol Ther. 2017 Jun;101(6):782-790. PMID: 28074556.
CA3 has potent inhibitory effects on YAP1/Tead transcriptional activity and primarily targets YAP1 high and therapy-resistant esophageal adenocarcinoma cells endowed with CSC properties.
YM 511 is a potent aromatase (CYP19) inhibitor.
|YM 298198 hydrochloride
YM 298198 hydrochloride is a highly potent, selective non-competitive mGlu 1 antagonist.
YM 022 is a highly potent, selective non-peptide CCK 2 antagonist.
YK 3-237 is a sIRT1 activator.
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