SERT-IN-2

• CAT Number: I041993
• CAS Number: 2055228-33-4
• Purity: ≥95%
• Synonyms: 3-[3-[4-[5-(2,4-difluorophenyl)pyrimidin-2-yl]piperazin-1-yl]propyl]-1H-indole-5-carbonitrile
• InChI: InChI=1S/C26H24F2N6/c27-21-4-5-22(24(28)13-21)20-16-31-26(32-17-20)34-10-8-33(9-11-34)7-1-2-19-15-30-25-6-3-18(14-29)12-23(19)25/h3-6,12-13,15-17,30H,1-2,7-11H2
• InChIKey: MONCKXMZFAXBAZ-UHFFFAOYSA-N
• SMILES: C1CN(CCN1CCCC2=CNC3=C2C=C(C=C3)C#N)C4=NC=C(C=N4)C5=C(C=C(C=C5)F)F

SERT-IN-2 is a potent SERT inhibitor (IC50=0.58 nM) with promising anti-depression efficacy. SERT-IN-2 shows good bioavailability of 83.28% in rats. SERT-IN-2 can cross the blood-brain barrier[1].
SERT-IN-2 (DH4) (2.5 mg/kg, 5 mg/kg; p.o.; single dose) shows high plasma exposure and oral bioavailability in dogs and rats[1].
SERT-IN-2 (10 mg/kg; i.p.; single dose) can cross the blood brain barrier in SD rats[1].
SERT-IN-2 (1-10 mg/kg; i.p.; single dose) inhibited serotonin uptake and potently antagonizes the p-chloroamphetamine (PCA)-induced depletion of 5-HT in the rat hypothalamus[1].
SERT-IN-2 (1-10 mg/kg; i.v.; 3 times before the test) exerts antidepressant effect in rat, reduces the immobility times in the forced swimming test (FST) in a dose-dependent manner[1].
Pharmacokinetic Analysis[1]

Route
Dose (mg/kg)
Cmax (ng/mL)
AUC(0-t) (ng·h/mL)
T1/2 (h)
Vss (L/kg)
Cl (L/h/kg)
F (%)

Rat
IV
1
193
1340
7.53
6.41
11.6
/

PO
2.5
180
2790
7.28
/
/
83.28