PSEM 89S TFA

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PSEM 89S TFA 是一种脑渗透性和选择性离子通道激动剂，分别对 Q79G 和 L141F 具有正交选择性。

PSEM 89S TFA is a brain-penetrant and selective ion channels agonist, and is orthogonally selective for Q79G and L141F, respectively.

PSEM 89S (10 or 30μM) activates layer 2/3 cortical neurons expressing (Pharmacologically Selective Actuator Module) PSAML141F,Y115F-5HT3 high conductance (HC).PSEM 89S (10 μM) reversibly silenced transfected neurons by reducing cellular input resistance.

PSEM 89S strongly reduces photostimulation-evoked feeding in mice expressing PSAML141F,Y115F- glycine receptor (GlyR) (30 mg/kg) but not in mice expressing only channelrhodopsin-2 (ChR2) (50 mg/kg).PSEM 89S (30 mg/kg) shows good brain penetrance in mice after minimally invasive intraperitoneal administration. Animal Model:Male Agrp-cre mice (3-6 weeks)Dosage:30 mg/kg Administration:I.p. administration Result:Almost completely suppressed fos (a marker of neuron activation) in ChR2-expressing neurons.Animal Model:C57BL/6 mice Dosage:30 mg/kg (Pharmacokinetic Analysis)Administration:I.p. administration Result:Rised rapidly in serum and brain, and was mostly cleared from both compartments in 1 h.

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Endocrinology/Hormones

AChR

nAChR

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1336913-03-1

404.4

C18H23F3N2O5?

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (247.29 mM)

OC(=O)C(F)(F)F.COc1ccc(OC)c(c1)C(=O)N[C@@H]1CN2CCC1CC2

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(-20℃)

With Ice Pack

≥ 2 years