Aldumastat (GLPG1972; S201086) is a potent, selective, orally active ADAMTS-5 (IC50=19 nM) inhibitor, whose selectivity is ADAMTS-4 (IC50=8 times 156 nM). Aldumastat has antimetabolic activity for osteoarthritis research.
|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|
|SNAP 94847 hydrochloride
SNAP 94847 Hydrochloride is a novel high affinity selective melanin concentration hormone receptor 1 (MCHR1) antagonist with antidepressant like activity. SNAP 94847 Hydrochloride is a high-affinity antagonist (pA2=7.81) of MYo-inositol phosphate formation induced by MCH.
Procysteine is a powerful antioxidant and cysteine precursor compound. It is inert and metabolized in cells into cysteine, which stimulates glutathione synthesis.
CE-245677 is a potent and reversible inhibitor of Tie2 and TrkA/B, with IC50 values of 4.7 and 1 nM, respectively, in the cellular system.
RP-6306 is a PKMYT1 inhibitor that can be used in cancer research.
RP-6306 is the only inhibitor of PKMYT1 currently available in the clinic, which is synthetically fatal to CCNE1 amplification, FBXW7 deletion or other specific mutations.
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