Mebhydrolin (napadisylate) is an antihistamine, used for symptomatic relief of allergic symptoms caused by histamine release, including nasal allergies and allergic dermatosis.
|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|
Discovery of 5-(1H-indol-5-yl)-1,3,4-thiadiazol-2-amines as potent PIM inhibitors.
Wu B, et al. Bioorg Med Chem Lett. 2015 Feb 15;25(4):775-80. PMID: 25616902.
|Related Histone demethylases Products|
CPI-455 HCl is a potent and selective inhibitor of KDM5 demethylases which reduces survival of drug-tolerant cancer cells, with a half-maximal inhibitory concentration (IC50) of 10 ± 1 nM for full-length KDM5A in enzymatic assays.
CP2 is a cyclic peptide that inhibits the JmjC histone demethylases KDM4 with IC50 values of 42 nM and 29 nM for KDM4A and KDM4C, respectively.
SP2509 is a selective histone demethylase LSD1 inhibitor with IC50 of 13 nM, showing no activity against MAO-A, MAO-B, lactate dehydrogenase and glucose oxidase.
EPZ020411 is a potent and selective inhibitor of PRMT6 with IC50 of 10 nM, has ＞10 fold selectivity for PRMT6 over PRMT1 and PRMT8. IC50 value: 10 nM
ORY-1001 (RG-6016) is the only dual KDM1A/LSD1 inhibitor, and it is also the only KDM1A inhibitor in development for the treatment of neurodegenerative disease.
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