Keywords

• GSK163090
• GSK-163090
• GSK 163090

Quick Details

• ProName: GSK163090
• CasNo: 844903-58-8
• Molecular Formula: C25H29N5O
• Application: For laboratory use only- not intended ...
• ProductionCapacity: 1 Kilogram/Month
• Purity: ≥98%
• Storage: -20℃
• Transportation: by air
• LimitNum: 5 Gram

Superiority

We are a CRO company, and our Research and Development team is consisted of PhDs and Masters in chemistry and pharmacy.

We are committed to protect our customer’s privacy with the highest level of ethical standard. Our dedicated team will follow up on every order and provide instant feedback on the status to our customer.

We stand behind our product by providing a complete QA report. The test data of customer order can be provided upon request.

We make our efforts to offer customer innovative, customized, high-quality service.

Our custom manufacturing encompasses everything from pharmaceutical intermediates to API.

Details

GSK163090 is a potent, selective, and orally active 5-HT1A/B/D receptor antagonist with pKi of 9.4/8.5/9.7, and 6.3/6.7 for 5-HT1A/B/D, and dopamine D2/D3, respectively. IC50 value: 9.4/8.5/9.7 (pKi) [1] Target: 5-HT in vitro: GSK163090 demonstrates clear dose-dependent inhibition of the 8-OH-DPAT-induced hyperlocomotor activity (hLMA), with ED50 values ranging from 0.03 to 1 mg/kg. GSK163090 was devoid of agonist activity at R1 receptors, but rather it demonstrated amoderate functional antagonismof the phenylephrineinduced contraction of rabbit aorta (pIC50=6.9).  in vivo: Fromamong these analogues, the cyclic urea derivative, GSK163090, emerged due to its low hERG affinity and excellent in vitro DMPK profile. The superior quality of GSK163090 was further highlighted by its commendable in vivo pharmacokinetic profile in rat and its outstanding activity in the 5-HT1A PD model, where 50% efficacy was achieved at a blood concentration of 3 ng/mL. On the basis of these results and its promising preclinical developability profile, GSK163090 was selected as an appropriate development candidate for progression toward clinical proof-of-concept studies.