SERT-IN-2 is a potent SERT inhibitor ( IC 50 =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 In Vivo 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 . SERT-IN-2 (10 mg/kg; i.p.; single dose) can cross the blood brain barrier in SD rats . 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 . 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 . Pharmacokinetic Analysis Route Dose (mg/kg) C max (ng/mL) AUC (0-t) (ng·h/mL) T 1/2 (h) V ss (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 Dog IV 1 520 2820 4.39 3.4 5.14 / PO 5 794 7540 16.4 / / 53.5 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 0.58 nM (SERT)
All
Chemical Reagents
Biomedicine
Organic raw materials
Inorganic chemical industry
intermediate
Agricultural chemicals
Auxiliaries and catalysts
Fragrances and Flavors
Dyes and Pigments
Daily chemical industry
SERT-IN-2
CAS number：2055228-33-4 molecular formula：C26H24F2N6
overview
compound introduction
Specs
| Chinese alias | 插入-2 | ||
| English alias | - | ||
| CAS number | 2055228-33-4 | molecular formula | C26H24F2N6 |
| molecular weight | 458.51 g/mol | Exact mass | ≥98% |
| PSA | - | logp | - |
numbering system
No numbering system information yet
physicochemical properties
No physical and chemical property information yet
Safety information
No safety information yet
Production methods and uses
No production method and use information yet
Related
upstream information
No upstream information yet
downstream information
No downstream information yet
MSDS
Found 0 shareMSDS
