product name LY2886721
Description: LY2886721 is a potent and selective BACE inhibitor used for the treatment of Alzheimers Disease. LY2886721 elicits robust central Aβ pharmacodynamic responses in mice, dogs, and humans. LY2886721 has high selectivity against key off-target proteases, which efficiently translates in vitro activity into robust in vivo amyloid β lowering in nonclinical animal models.
References: J Alzheimers Dis. 2011;24 Suppl 2:43-52; J Neurosci. 2015 Jan 21;35(3):1199-210.
390.41
Formula
C18H16F2N4O2S
CAS No.
1262036-50-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 9 mg/mL (23.1 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19399839
| In Vitro |
In vitro activity: LY2886721 is an oral, small molecule of β-site amyloid protein cleaving enzyme (BACE) inhibitor with the potential to inhibit the synthesis of β-amyloid and thereby to slow the clinical progression of AD. LY2886721 can also targetγ-secretase to nhibit the synthesis of β-amyloid. Kinase Assay: Cell Assay: treatment of LY2886721 leads to the inhibition of Aβ in HEK293Swe with IC50 of 18.7nM and PDAPP neuronal culture with IC50 10.7 nM1. LY2886721 decreases CSF sAPPβ and increases CSF sAPPα in a dose- dependent manner 2. |
|---|---|
| In Vivo | At all 3 doses, LY2886721 significantly reduced hippocampal and cortical levels of Aβ1-x. In addition, LY2886721 significantly lowered brain parenchymal levels of C99 and sAPPβ. Although cortical levels of C99 were reduced significantly by LY2886721 at the doses of 10 and 30 mg/kg, the effect of LY2886721 at the dose of 3 mg/kg failed to reach statistical significance. On the other hand, the sAPPβ levels were significantly decreased by LY2886721 at all 3 doses. |
| Animal model | PDAPP mice |
| Formulation & Dosage | 3-30 mg/kg |
| References | J Alzheimers Dis. 2011;24 Suppl 2:43-52; J Neurosci. 2015 Jan 21;35(3):1199-210. |
Related Posts
product name LY2886721
Description: LY2886721 is a potent and selective BACE inhibitor used for the treatment of Alzheimers Disease. LY2886721 elicits robust central Aβ pharmacodynamic responses in mice, dogs, and humans. LY2886721 has high selectivity against key off-target proteases, which efficiently translates in vitro activity into robust in vivo amyloid β lowering in nonclinical animal models.
References: J Alzheimers Dis. 2011;24 Suppl 2:43-52; J Neurosci. 2015 Jan 21;35(3):1199-210.
390.41
Formula
C18H16F2N4O2S
CAS No.
1262036-50-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 9 mg/mL (23.1 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19399839
| In Vitro |
In vitro activity: LY2886721 is an oral, small molecule of β-site amyloid protein cleaving enzyme (BACE) inhibitor with the potential to inhibit the synthesis of β-amyloid and thereby to slow the clinical progression of AD. LY2886721 can also targetγ-secretase to nhibit the synthesis of β-amyloid. Kinase Assay: Cell Assay: treatment of LY2886721 leads to the inhibition of Aβ in HEK293Swe with IC50 of 18.7nM and PDAPP neuronal culture with IC50 10.7 nM1. LY2886721 decreases CSF sAPPβ and increases CSF sAPPα in a dose- dependent manner 2. |
|---|---|
| In Vivo | At all 3 doses, LY2886721 significantly reduced hippocampal and cortical levels of Aβ1-x. In addition, LY2886721 significantly lowered brain parenchymal levels of C99 and sAPPβ. Although cortical levels of C99 were reduced significantly by LY2886721 at the doses of 10 and 30 mg/kg, the effect of LY2886721 at the dose of 3 mg/kg failed to reach statistical significance. On the other hand, the sAPPβ levels were significantly decreased by LY2886721 at all 3 doses. |
| Animal model | PDAPP mice |
| Formulation & Dosage | 3-30 mg/kg |
| References | J Alzheimers Dis. 2011;24 Suppl 2:43-52; J Neurosci. 2015 Jan 21;35(3):1199-210. |