Description
GSK163090 is a potent, selective and orally active 5-HT1A/1B/1D receptor antagonist with pKi values of 9.4/8.5/9.7, respectively. GSK163090 inhibits the functional activity of serotonin reuptake transporter (SerT) with a pKi value of 6.1. GSK163090 has antidepressant and anxiolytic activities.
Product information
CAS Number: 844903-58-8
Molecular Weight: 415.53
Formula: C25H29N5O
Chemical Name: 1-(3-{2-[4-(2-methylquinolin-5-yl)piperazin-1-yl]ethyl}phenyl)imidazolidin-2-one
Smiles: CC1C=CC2C(=CC=CC=2N2CCN(CCC3=CC(=CC=C3)N3CCNC3=O)CC2)N=1
InChiKey: ANGUXJDGJCHGOG-UHFFFAOYSA-N
InChi: InChI=1S/C25H29N5O/c1-19-8-9-22-23(27-19)6-3-7-24(22)29-16-14-28(15-17-29)12-10-20-4-2-5-21(18-20)30-13-11-26-25(30)31/h2-9,18H,10-17H2,1H3,(H,26,31)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 14.29 mg/mL (34.39 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
GSK163090 (compound 36) is devoid of agonist activity at R1 receptors, but rather it demonstrates a moderate functional antagonismof the phenylephrineinduced contraction of rabbit aorta (pIC50=6.9). At 1 μM concentration, the ratio of the apparent permeabilities measured from basolateral-to-apical (BA) to apical-to-basolateral (AB) indicated that GSK163090 is a moderate P-glycoprotein (P-gp) substrate (BA/AB = 2.8).
In Vivo:
In male Sprague-Dawley rats, GSK163090 (compound 36) treatment shows clear dose-dependent inhibition of the 8-OH-DPAT-induced hyperlocomotor activity (hLMA), with ED50 values ranging from 0.03 to 1 mg/kg.
Products are for research use only. Not for human use.
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