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GSK163090
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GSK163090图片
CAS NO:844903-58-8
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 415.53
Formula C25H29N5O
CAS No. 844903-58-8;
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 16.5 mg/mL
Water: <1 mg/mL
Ethanol: <1 mg/mL
SMILES Code O=C1NCCN1C2=CC=CC(CCN3CCN(C4=C5C=CC(C)=NC5=CC=C4)CC3)=C2
Synonyms GSK163090; GSK-163090; GSK 163090.
实验参考方法
In Vitro

In vitro activity: GSK163090 is novel, potent, selective, and orally bioavailable antagonist of the 5-HT1A/B/D receptor that has the potential to be used as a fast-onset antidepressant/anxiolytic. It showed low intrinsic activities and potent affinities across the 5-HT1A, 5-HT1B, and 5-HT1D receptors as well as high selectivity against the serotonin transporter. GSK163090 was found to combine potent in vivo activity with a strong preclinical developability profile, and on this basis it was selected as a drug candidate with the aim of assessing its potential as a fast-onset antidepressant/anxiolytic.


Kinase Assay: 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. 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)


Cell Assay:

In VivoFromamong 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.
Animal model
Formulation & Dosage
ReferencesJ Med Chem. 2010 Dec 9;53(23):8228-40.