LY2886721
LY2886721
CAS: 1262036-50-9
Molecular Formula: C18H16F2N4O2S
LY2886721 - Names and Identifiers
LY2886721 - Physico-chemical Properties
| Molecular Formula | C18H16F2N4O2S |
| Molar Mass | 390.41 |
| Density | 1.57 |
| Solubility | DMSO 9 mg/mL (23.05 mM); Water <1 mg/mL (<1 mM); Ethanol <1 mg/mL (<1 mM) |
| pKa | 10.08±0.70(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | LY2886721 is an oral, small molecule β-amyloid lyase (BACE) inhibitor with the potential to inhibit β-amyloid synthesis, thereby slowing the clinical progression of AD. LY2886721 can also target gamma-secretion to inhibit beta-amyloid synthesis. The IC50 of LY2886721 to recombinant human source BACE1 was 20.3 nM. The IC50s for LY2886721 inhibiting Abeta in HEK293Swe and PDAPP neurons were 18.7 nM and 10.7 nM, respectively. LY2886721 is highly selective for some key off-target proteases with little inhibition. Its potent in vitro activity, translated into in vivo, is strongly effective in reducing amyloidβ levels in non-clinical animal models. LY2886721 has an IC50 of 10.2 nM for hBACE2 and has no inhibitory effect on cathepsin D, pepsin, renin or other important aspartyl proteases (IC50 >100,000 nM), this indicates that the activity of LY2886721 against these common aspartyl proteases is not significant. |
| In vivo study | Oral administration of LY2886721 to PDAPP mice resulted in a concentration-dependent reduction of Abeta, C99, and aAPPbeta in the brain. Three hours after oral administration of LY2886721 at a concentration of 3-30 mg/kg, Abeta levels in the brains of the treated mice were reduced by-20%-65% compared to the control group. The in vivo pharmacokinetic response of LY2886721 persisted for 9 hours in the brain of PDAPP mice. Pharmacokinetic studies in beagle dogs indicate that the administration of 1 mg/kg of LY2886721 causes a significant and sustained Abeta reduction effect in their plasma. In dogs, administration of 0.5mg/kg of LY2886721 resulted in a 50% decrease in CSF Abeta after 9 hours. The mean terminal half-life t 1/2 of LY2886721 in vivo is 17.2 h (range 8.19-36.3 h). The mean apparent oral clearance was 34.8 L/h (38% CV) and the volume of distribution at terminal stage was 863 L(56% CV). LY2886721 is freely permeable across the blood-brain barrier. |
LY2886721 - Introduction
LY2886721 are BACE inhibitors used to treat Alzheimer's disease. Phase 1/2.
Last Update：2022-10-16 17:41:23
Supplier List
Multiple SpecificationsSpot supply
Product Name: N-(3-((4aS,7aS)-2-Amino-4a,5-dihydro-4H-furo[3,4-d][1,3]thiazin-7a(7H)-yl)-4-fluorophenyl)-5-fluoropicolinamide Request for quotationCAS: 1262036-50-9
Tel: 400-968-2212
Email: 3623107365@qq.com
Mobile: 18916960931
QQ: 3623107365
Wechat: 18916960931
Spot supply
Product Name: LY2886721 Visit Supplier Webpage Request for quotationCAS: 1262036-50-9
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
WhatsApp: +86-18821248368
Spot supply
Product Name: LY2886721 Visit Supplier Webpage Request for quotationCAS: 1262036-50-9
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
Spot supply
Product Name: LY2886721 Visit Supplier Webpage Request for quotationCAS: 1262036-50-9
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Product Name: LY2886721 Visit Supplier Webpage Request for quotation
CAS: 1262036-50-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
CAS: 1262036-50-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Multiple SpecificationsSpot supply
Product Name: N-(3-((4aS,7aS)-2-Amino-4a,5-dihydro-4H-furo[3,4-d][1,3]thiazin-7a(7H)-yl)-4-fluorophenyl)-5-fluoropicolinamide Request for quotationCAS: 1262036-50-9
Tel: 400-968-2212
Email: 3623107365@qq.com
Mobile: 18916960931
QQ: 3623107365
Wechat: 18916960931
Spot supply
Product Name: LY2886721 Visit Supplier Webpage Request for quotationCAS: 1262036-50-9
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
WhatsApp: +86-18821248368
Spot supply
Product Name: LY2886721 Visit Supplier Webpage Request for quotationCAS: 1262036-50-9
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
Spot supply
Product Name: LY2886721 Visit Supplier Webpage Request for quotationCAS: 1262036-50-9
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Product Name: LY2886721 Visit Supplier Webpage Request for quotation
CAS: 1262036-50-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
CAS: 1262036-50-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
View History
LY2886721
直接棕 GTL
2-BROMOPHENETOLE
1540-28-9
溴乙酸乙
BMY-26538-01
3042-22-6
2-CHLORO-3-CHLOROMETHYLTHIOPHENE
156223-05-1
s-Tribromopropane
直接棕 GTL
2-BROMOPHENETOLE
1540-28-9
溴乙酸乙
BMY-26538-01
3042-22-6
2-CHLORO-3-CHLOROMETHYLTHIOPHENE
156223-05-1
s-Tribromopropane