177943-33-8
177943-33-8 structure
- Name: PF-04859989 HCl
- Chemical Name: (3S)-3-amino-1-hydroxy-3,4-dihydroquinolin-2-one,hydrochloride
- CAS Number: 177943-33-8
- Molecular Formula: C9H11ClN2O2
- Molecular Weight: 214.64900
- Catalog: Research Areas Neurological Disease
- Create Date: 2017-11-15 23:32:17
- Modify Date: 2024-01-03 17:09:29
-
PF-04859989 hydrochloride is a brain-penetrant, irreversible kynurenine aminotransferase (KAT) II inhibitor with IC50s of 23 and 263 nM for hKAT II and rKAT II. PF-04859989 hydrochloride is selective for KAT II over human KAT I, KAT III, and KAT IV (IC50s of 22, 11, and >50 μM, respectively)[1].
| Name | (3S)-3-amino-1-hydroxy-3,4-dihydroquinolin-2-one,hydrochloride |
|---|---|
| Synonyms | (3S)-3-Amino-1-hydroxy-3,4-dihydroquinolin-2(1H)-one |
| Description | PF-04859989 hydrochloride is a brain-penetrant, irreversible kynurenine aminotransferase (KAT) II inhibitor with IC50s of 23 and 263 nM for hKAT II and rKAT II. PF-04859989 hydrochloride is selective for KAT II over human KAT I, KAT III, and KAT IV (IC50s of 22, 11, and >50 μM, respectively)[1]. |
|---|---|
| Related Catalog | |
| In Vivo | In vivo pharmacokinetic and efficacy studies in rat show that PF-04859989 is a brain-penetrant, irreversible inhibitor and is capable of reducing brain kynurenic acid by 50% at a dose of 10 mg/kg (sc)[1]. Rats receiving PF-04859989 (5 mg/kg; i.p.) exhibited a significantly lower number of spontaneously active DA neurons pertrack[1]. Animal Model: Male Sprague-Dawley rats[2] Dosage: 5 mg/kg Administration: I.p. Result: Exhibited a significantly lower number of spontaneously active dopamine (DA) neurons pertrack compared to controls. |
| References |
| Molecular Formula | C9H11ClN2O2 |
|---|---|
| Molecular Weight | 214.64900 |
| Exact Mass | 214.05100 |
| PSA | 66.56000 |
| LogP | 1.85950 |
| RIDADR | NONH for all modes of transport |
|---|---|
| HS Code | 2933790090 |
|
~67%
177943-33-8 |
| Literature: Dounay, Amy B.; Anderson, Marie; Bechle, Bruce M.; Campbell, Brian M.; Claffey, Michelle M.; Evdokimov, Artem; Evrard, Edelweiss; Fonseca, Kari R.; Gan, Xinmin; Ghosh, Somraj; Hayward, Matthew M.; Horner, Weldon; Kim, Ji-Young; McAllister, Laura A.; Pandit, Jayvardhan; Paradis, Vanessa; Parikh, Vinod D.; Reese, Matthew R.; Rong, Suobao; Salafia, Michelle A.; Schuyten, Katherine; Strick, Christine A.; Tuttle, Jamison B.; Valentine, James; Wang, Hong; Zawadzke, Laura E.; Verhoest, Patrick R. ACS Medicinal Chemistry Letters, 2012 , vol. 3, # 3 p. 187 - 192 |
| HS Code | 2933790090 |
|---|---|
| Summary | 2933790090. other lactams. VAT:17.0%. Tax rebate rate:9.0%. . MFN tariff:9.0%. General tariff:20.0% |