GB1107 is a potent, selective, orally active galectin-3 inhibitor with Kd of 37 nM. GB1107 inhibits lung adenocarcinoma growth and augments response to PD-L1 blockade. GB1107 potentiates the effects of a PD-L1 immune checkpoint inhibitor to increase expression of cytotoxic (IFN-γ, granzyme B, perforin-1, Fas ligand) and apoptotic (cleaved caspase-3) effector molecules.
|Solubility (25°C)||DMSO 45 mg/mL|
|Storage||-20°C, dry, sealed|
|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.
|Related Galectin Products|
Belapectin, a galectin 3 inhibitor with a Ki value of 2.8 μM, reduces hepatic fibrosis and portal hypertension in rats, and can be used in studies related to non-alcoholic steatohepatitis (NASH).
Selvigaltin (GB1211) is an orally available galectin-3 (Gal-3) inhibitor.
G3-C12 is a galectin-3 binding peptide, with Kd of 88 nM, and shows anticancer activity.
OTX008 is a selective inhibitor of galectin-1.
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