SAfit2 is a potent inhibitor of FK506-binding protein 51 (FKBP51) with a Ki value of 6 nM. SAfit2 has been used as a potential agent in the study of major depression, obesity, and chronic pain.
|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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
|Solubility||DMSO ≥ 60 mg/mL|
RGLS4326 (RG4326) is a first-in-class microRNA-17 (miR-17) oligonucleotide inhibitor. RGLS4326 can be used in the study of autosomal dominant polycystic kidney disease (ADPKD). RGLS4326 acts on HeLa cells to inhibit the function of miR-17 with EC50 value of 28.3 nM.
Telaglenastat (CB-839) hydrochloride is a pioneering (first-in-class), selective, reversible, orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat hydrochloride has IC50 values of 23 nM and 28 nM for endogenous glutaminase in the kidney and brain of mice, respectively. Telaglenastat hydrochloride also induces autophagy and has strong antitumor activity.
Ibezapolstat (ACX-362E) is a first-of-its-kind (first-in-class) inhibitor of the orally active DNA polymerase IIIC (DNA pol IIIC) developed for use in the study of Clostridium difficile infection (CDI).
FBA-IN-1 is a pioneer, covalent allosteric inhibitor of 1, 6-bisphosphate fructoalbinase (CaFBA) from Candida albicans. FBA-IN 1 inhibited the growth of azole resistant strain 103 with MIC80 of 1 μg/mL.
Monalizumab is a first-in-class immune checkpoint inhibitor targeting natural killer cell population 2A (NKG2A). Monalizumab can be used in the study of head and neck squamous cell carcinoma (HNSCC).
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