Ptp1b-in-1 is a small molecule inhibitor of PTP1B with an IC50 value of 1.6mm, and is often used as a parent nucleus derived from analogues.
|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 ≥ 20 mg/mL|
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Abbv-cls-484 is a potent inhibitor of PTPN1 or PTPN2 with subnanomolar activity.
Razuprotafib (AKB-9778) is an effective selective inhibitor of VE-PTP (HPTPß) catalytic activity (IC50=17 pM).
Rmc-4630 (SHP2-IN-7) is a SHP2 inhibitor derived from patent WO2018013597.
Rbin-1 (ribozinoindole-1) is a potent and reversible inhibitor of Midasin (Mdn1), an enzyme belonging to the AAA+ (ATPases associated with diverse cellular activities) protein family (GI50 value 136 nM in wild-type cells).
Voclosporin (ISATX247) is a novel calcineurin (PP2B) (CN) inhibitor.
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