| CAS NO: | 1779796-27-8 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| Molecular Weight (MW) | 421.91 |
|---|---|
| Formula | C22H28ClNO5 |
| CAS No. | 1779796-27-8 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: ≥ 31 mg/mL |
| Water: <1 mg/mL | |
| Ethanol: N/A | |
| SMILES Code | O=C(O)CN(CCOC1=CC=C(C2=CC=C(OCO3)C3=C2)C=C1C(C)(C)C)C.[H]Cl |
| Synonyms | LY2365109 HCl; LY 2365109 HCl; LY-2365109 HCl; LY2365109 Hydrochloride |
| In Vitro | In vitro activity: LY2365109 is a novel, potent and selective inhibitor of GlyT1 (glycine transporter 1) with IC50 value of 15.8 nM. Selective inhibitors of the glycine transporter 1 (GlyT1) have been implicated in central nervous system disorders related to hypoglutamatergic function such as schizophrenia. The selective GlyT1 inhibitors ALX5407 (NFPS) and LY2365109 increased cerebrospinal fluid levels of glycine and potentiated NMDA-induced increases in dialysate levels of neurotransmitters in the prefrontal cortex (PFC) and the striatum. Kinase Assay: LY2365109 is a potent and selective GlyT1 inhibitors with IC50 value of 15.8 nM. |
|---|---|
| In Vivo | LY2365109 is administered at 0.3 or 30 mg/kg by PO. LY2365109 appeared slightly more potent than ALX5407 over the dose-range tested on CSF levels of glycine in the rat LY2365109 can act to potentiate NMDA function in the PFC but also mediate sustained inhibition of GlyT1 transporters in caudal areas of the brain. LY2365109 increased seizure thresholds in mice. Importantly, chronic seizures in the mouse model of TLE were robustly suppressed by systemic administration of the GlyT1 inhibitor LY2365109. |
| Animal model | Mice |
| Formulation & Dosage | 0.3 or 30 mg/kg by PO. |
| References | Neuropharmacology. 2015 Dec;99:554-65; Neuropharmacology. 2008 Oct;55(5):743-54. |
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