EPPTB is a selective antagonist of the trace amine-associated receptor 1 (TAAR1), a G protein-coupled receptor (GPCR) activated by endogenous trace amines (tyramine, tryptamine, synephrine, octopamine, β)-phenylethylamine), which are chemically similar to monoaminergic neurotransmitters (epinephrine, norepinephrine, dopamine). TAAR1 is considered a promising target for the treatment of neuropsychiatric disorders, however study of TAAR1 has hampered by the fact that selective ligands have not been available. EPPTB is the first potent and selective TAAR1 antagonist with an IC50 of 28 nM at mouse TAAR1. EPPTB is less selective for rat and human with IC50 values of 4539 and 7487 nM, respectively.
|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
SPH3127 is an oral direct renin inhibitor (DRI) that is being developed for hypertension. The renin-angiotensin-aldosterone system is responsible for the regulation of blood pressure.
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.
“lipid 10a” (Arcturus tunable lipid for RNA drug delivery).
BAY 1214784 is a potent, selective and orally active antagonist of the human gonadotropin-releasing hormone receptor (hGnRH-R).BAY 1214784 has the potential to be studied in uterine fibroids.
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