SERT-IN-2 - ≥98% , CAS No.2055228-33-4

CAS: 2055228-33-4 Cat. No.: S646438 분자식: C₂₆H₂₄F₂N₆ 분자량: 458.51

GRADE & PURITY ≥98%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

개요

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)

Specifications

사양 및 순도

≥98%

생화학 및 생리적 메커니즘

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.

보관 조건

Store at -20°C

배송

Ice chest + Ice pads

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순수함

≥98%

이름과 식별자

정식 스마일

N#CC1=CC2=C(NC=C2CCCN3CCN(CC3)C4=NC=C(C5=CC=C(C=C5F)F)C=N4)C=C1

분자량

458.51

화학 및 물리적 특성

• 용해성: DMSO : 200 mg/mL (436.20 mM; Need ultrasonic)