RTI-7470-44 (C007B-415983)

RTI-7470-44 is a potent, selective and blood-brain barrier (BBB) penetrant human trace amine-associated receptor subtype 1 (hTAAR1) antagonist with an IC 50 value of 8.4 nM and a K i value of 0.3 nM. RTI-7470-44 has moderate metabolic stability, and a favorable preliminary off-target profile. RTI-7470-44 can increase the spontaneous firing rate of mouse ventral tegmental area (VTA) dopaminergic neurons. RTI-7470-44 can be used for researching schizophrenia, agent addiction, and Parkinson’s disease (PD)In VitroRTI-7470-44 (10 μM) shows little to no off-target activity with the exception of the benzylpiperazine (BZP) rat brain site and human sigma 2 with inhibition of 75 and 90%, respectively; has a moderate affinity for the BZP rat brain site (K i =1 μM) and a very weak affinity for human sigma 2 (K i =8.4 μM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoRTI-7470-44 (40 μM) significantly increases the firing rate of dopaminergic neurons in VTA slices from DAT-IRES-Cre; td-Tomato mice, and reverses the inhibitory effect of RO5166017 (a TAAR1 agonist) . RTI-7470-44 (10 μM) has decent stability in human liver microsomes, less stable in mouse liver microsomes and very poor stability in rat liver microsomes . Stability of RTI-7470-44 in Human, Rat, and Mouse Liver Microsomes . species half-life (min) clearance, CLINT (mL/min/mg) Human 83.9 14.9 Rat 9.11 274 Mouse 65.8 63.5 MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:IC 50 : 8.4 nM (human TAAR1), 748 nM (rat TAAR1), 1190 nM (mouse TAAR1).

Specifications and Purity: ≥99%

Molecular Formula: C19H11ClF3N5OS

Molecular Weight: 449.84