| Identification | Back Directory | [Name]
PF-4628935 | [CAS]
1383719-97-8 | [Synonyms]
PF-4628935
PF-04628935
PF-04628935 >=98% (HPLC)
1-[2-[[2-Chloro-4-(2H-1,2,3-triazol-2-yl)phenyl]methyl]-2,7-diazaspiro[3.5]non-7-yl]-2-(2-methylimidazo[2,1-b]thiazol-6-yl)-ethanone | [Molecular Formula]
C24H26ClN7OS | [MDL Number]
MFCD28118979 | [MOL File]
1383719-97-8.mol | [Molecular Weight]
496.03 |
| Chemical Properties | Back Directory | [density ]
1.50±0.1 g/cm3(Predicted) | [storage temp. ]
room temp | [solubility ]
DMSO: soluble10mg/mL, clear | [form ]
powder | [pka]
7.86±0.20(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
PF-04628935 (compound 10n) is a potent ghrelin receptor inverse agonist, with an IC50 of 4.6 nM. PF-04628935 exhibits oral bioavailability of 43% in rats and shows reasonable penetration into the brain. PF-04628935 can be used for stress and anxiety research[1][2]. | [Biological Activity]
PF-04628935 is a potent antagonist/inverse agonist of the ghrelin receptorgrowth hormone secretagogue receptor 1a (GHS-R1a) with an IC50 of 4.6 nM. Ghrelin and GSHR are involved in regulation of food intake and long-term energy homeostasis; GSHR ligands are of interest for obesity and other metabolic disorders. PF-04628935 is orally bioavailable and brain penetrant. | [IC 50]
GHSR1a: 4.6 nM (IC50) | [storage]
Store at -20°C | [References]
[1] Kung DW, et, al. Identification of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor. Bioorg Med Chem Lett. 2012 Jul 1;22(13):4281-7. DOI:10.1016/j.bmcl.2012.05.024
[2] Cavalcante DP, et, al. Role of dorsal raphe nucleus GHS-R1a receptors in the regulation of inhibitory avoidance and escape behaviors in rats. Behav Brain Res. 2019 Jun 3;365:178-184. DOI:10.1016/j.bbr.2019.03.017 |
|
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|