Products for Research Use Only

GSK163090

CAT: 0013-GTR19154907-01Size: 100 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19154907-01Size:100 mg
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Description
GSK163090 is a specific and orally active 5-HT1A/B/D receptor antagonist (pKis: 9.4/8.5/9.7, and 6.3/6.7 for 5-HT1A/B/D, and dopamine D2/D3) . (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.
CAS Number
844903-58-8
Purity
>98% (HPLC)
Solubility
DMSO:14.29 mg/mL (34.39 mM; Need ultrasonic)
Smiles
Cc1ccc (c (N2CCN (CCc3cccc (N (CCN4) C4=O) c3) CC2) ccc2) c2n1
Molecular Formula
C25H29N5O
Molecular Weight
415.53
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.