GSK163090
Modify Date: 2024-01-02 16:09:13
GSK163090 structure
|
Common Name | GSK163090 | ||
|---|---|---|---|---|
| CAS Number | 844903-58-8 | Molecular Weight | 415.531 | |
| Density | 1.2±0.1 g/cm3 | Boiling Point | N/A | |
| Molecular Formula | C25H29N5O | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of GSK163090GSK163090 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). [1]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 pharmacokineticprofile 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. [1] |
| Name | 1-[3-[2-[4-(2-methylquinolin-5-yl)piperazin-1-yl]ethyl]phenyl]imidazolidin-2-one |
|---|---|
| Synonym | More Synonyms |
| Description | 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). [1]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 pharmacokineticprofile 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. [1] |
|---|---|
| Related Catalog | |
| References |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Molecular Formula | C25H29N5O |
| Molecular Weight | 415.531 |
| Exact Mass | 415.237213 |
| PSA | 55.20000 |
| LogP | 2.35 |
| Index of Refraction | 1.644 |
| Storage condition | 2-8℃ |
|
~70%
GSK163090 CAS#:844903-58-8 |
| Literature: GLAXO GROUP LIMITED Patent: WO2005/14552 A1, 2005 ; Location in patent: Page/Page column 64 ; WO 2005/014552 A1 |
|
~%
GSK163090 CAS#:844903-58-8 |
| Literature: Cimarosti, Zadeo; Giubellina, Nicola; Stabile, Paolo; Laval, Gilles; Tinazzi, Francesco; Maton, William; Pachera, Roberta; Russo, Paola; Moretti, Ramona; Rossi, Sara; Cooke, Jason W. B.; Westerduin, Pieter Organic Process Research and Development, 2011 , vol. 15, # 6 p. 1287 - 1296 |
|
~%
GSK163090 CAS#:844903-58-8 |
| Literature: Cimarosti, Zadeo; Giubellina, Nicola; Stabile, Paolo; Laval, Gilles; Tinazzi, Francesco; Maton, William; Pachera, Roberta; Russo, Paola; Moretti, Ramona; Rossi, Sara; Cooke, Jason W. B.; Westerduin, Pieter Organic Process Research and Development, 2011 , vol. 15, # 6 p. 1287 - 1296 |
![2-[3-(2-oxo-1-imidazolidinyl)phenyl]ethyl methanesulfonate structure](https://www.chemsrc.com/caspic/399/844903-56-6.png)
![1-[3-(2-hydroxyethyl)phenyl]-2-imidazolidinone structure](https://www.chemsrc.com/caspic/437/844903-55-5.png)
| Precursor 3 | |
|---|---|
| DownStream 0 | |
| 1-(3-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone |
| unii-7xi927x82b |
| 2-Imidazolidinone, 1-[3-[2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl]phenyl]- |
| GSK163090 |