LY2886721BACE inhibitor CAS# 1262036-50-9 |
- SKLB610
Catalog No.:BCC3647
CAS No.:1125780-41-7
- AP26113
Catalog No.:BCC1069
CAS No.:1197958-12-5
- Pazopanib (GW-786034)
Catalog No.:BCC1286
CAS No.:444731-52-6
- Danusertib (PHA-739358)
Catalog No.:BCC2172
CAS No.:827318-97-8
- BGJ398
Catalog No.:BCC1278
CAS No.:872511-34-7
- Ponatinib (AP24534)
Catalog No.:BCC2522
CAS No.:943319-70-8
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 1262036-50-9 | SDF | Download SDF |
PubChem ID | 49837968 | Appearance | Powder |
Formula | C18H16F2N4O2S | M.Wt | 390.41 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | DMSO : ≥ 42 mg/mL (107.58 mM) *"≥" means soluble, but saturation unknown. | ||
Chemical Name | N-[3-[(4aS,7aS)-2-amino-4,4a,5,7-tetrahydrofuro[3,4-d][1,3]thiazin-7a-yl]-4-fluorophenyl]-5-fluoropyridine-2-carboxamide | ||
SMILES | C1C2CSC(=NC2(CO1)C3=C(C=CC(=C3)NC(=O)C4=NC=C(C=C4)F)F)N | ||
Standard InChIKey | NIDRNVHMMDAAIK-YPMLDQLKSA-N | ||
Standard InChI | InChI=1S/C18H16F2N4O2S/c19-11-1-4-15(22-6-11)16(25)23-12-2-3-14(20)13(5-12)18-9-26-7-10(18)8-27-17(21)24-18/h1-6,10H,7-9H2,(H2,21,24)(H,23,25)/t10-,18-/m0/s1 | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
||
About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
||
Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Description | LY2886721 is an oral, small molecule inhibitor of β-site amyloid protein cleaving enzyme (BACE) used for the treatment of Alzheimer's Disease. | |||||
Targets | BACE |
LY2886721 Dilution Calculator
LY2886721 Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 2.5614 mL | 12.807 mL | 25.6141 mL | 51.2282 mL | 64.0352 mL |
5 mM | 0.5123 mL | 2.5614 mL | 5.1228 mL | 10.2456 mL | 12.807 mL |
10 mM | 0.2561 mL | 1.2807 mL | 2.5614 mL | 5.1228 mL | 6.4035 mL |
50 mM | 0.0512 mL | 0.2561 mL | 0.5123 mL | 1.0246 mL | 1.2807 mL |
100 mM | 0.0256 mL | 0.1281 mL | 0.2561 mL | 0.5123 mL | 0.6404 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
Calcutta University
University of Minnesota
University of Maryland School of Medicine
University of Illinois at Chicago
The Ohio State University
University of Zurich
Harvard University
Colorado State University
Auburn University
Yale University
Worcester Polytechnic Institute
Washington State University
Stanford University
University of Leipzig
Universidade da Beira Interior
The Institute of Cancer Research
Heidelberg University
University of Amsterdam
University of Auckland
TsingHua University
The University of Michigan
Miami University
DRURY University
Jilin University
Fudan University
Wuhan University
Sun Yat-sen University
Universite de Paris
Deemed University
Auckland University
The University of Tokyo
Korea University
LY2886721 is an oral and furothiazine-based inhibitor of β site-amyloid protein cleaving enzyme (BACE) with IC50 of 20.3nM. This product has the potency for the treatment of Alzheimer's disease.
BACE, also known as Beta-Secretase 1, is an aspartic-acid protease that plays important role in the formation of myelin sheaths in peripheral nerve cells.
In vitro, 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 PDAPP mice, oral administration of LY2886721 resulted in a reduction in brain Aβ, C99 and sAPPβ in a dose-dependent pattern 2. Aβ levels in the brain were decreased by 20% -65% as compared with the vehicle-treated groups 3 hours after treatment of LY2886721 at a dosage of 3-30 mg/kg per mice. In addition, LY2886721 significantly lowers plasma and CSF Aβs in the MAD study 1.
References:
1. Vassar R. BACE1 inhibitor drugs in clinical trials for Alzheimer's disease. Alzheimer's research & therapy. 2014;6(9):89.
2. Nishitomi K, Sakaguchi G, Horikoshi Y, et al. BACE1 inhibition reduces endogenous Abeta and alters APP processing in wild-type mice. Journal of neurochemistry. 2006;99(6):1555-1563.
- Spiranthol A
Catalog No.:BCN7893
CAS No.:126192-35-6
- Icariside E5
Catalog No.:BCN6140
CAS No.:126176-79-2
- BAPTA-AM
Catalog No.:BCC5456
CAS No.:126150-97-8
- GNF179
Catalog No.:BCC5175
CAS No.:1261114-01-5
- Siamenoside I
Catalog No.:BCN2540
CAS No.:126105-12-2
- 11-Oxo-mogroside V
Catalog No.:BCN2509
CAS No.:126105-11-1
- Rubiyunnanin C
Catalog No.:BCN8045
CAS No.:1261030-04-9
- I-BET-762
Catalog No.:BCC4474
CAS No.:1260907-17-2
- 6-O-Methylcerevisterol
Catalog No.:BCN6139
CAS No.:126060-09-1
- Atractyloside A
Catalog No.:BCN5383
CAS No.:126054-77-1
- GSK 525768A
Catalog No.:BCC1603
CAS No.:1260530-25-3
- 3-O-beta-Allopyranosyl-(1->4)-beta-oleandropyranosyl-11-O-isobutyryl-12-O-acetyltenacigenin B
Catalog No.:BCN6765
CAS No.:1260252-18-3
- Ginsenoside Rg4
Catalog No.:BCN2713
CAS No.:126223-28-7
- Agrimonolide 6-O-glucoside
Catalog No.:BCN6141
CAS No.:126223-29-8
- INCB3344
Catalog No.:BCC1648
CAS No.:1262238-11-8
- Uralsaponin C
Catalog No.:BCN7906
CAS No.:1262326-46-4
- 24-Hydroxy-licoricesaponin A3
Catalog No.:BCN7896
CAS No.:1262326-47-5
- Uralsaponin D
Catalog No.:BCN7895
CAS No.:1262489-44-0
- (2R,3S)-Dihydrodehydroconiferyl alcohol
Catalog No.:BCN7886
CAS No.:126253-41-6
- Fumitremorgin B
Catalog No.:BCN6453
CAS No.:12626-17-4
- Assamicadine
Catalog No.:BCN1957
CAS No.:126260-96-6
- GS967
Catalog No.:BCC6401
CAS No.:1262618-39-2
- Benzoylmesaconine hydrochloride
Catalog No.:BCN5399
CAS No.:126266-38-4
- Penitrem A
Catalog No.:BCC7957
CAS No.:12627-35-9
The potent BACE1 inhibitor LY2886721 elicits robust central Abeta pharmacodynamic responses in mice, dogs, and humans.[Pubmed:25609634]
J Neurosci. 2015 Jan 21;35(3):1199-210.
BACE1 is a key protease controlling the formation of amyloid beta, a peptide hypothesized to play a significant role in the pathogenesis of Alzheimer's disease (AD). Therefore, the development of potent and selective inhibitors of BACE1 has been a focus of many drug discovery efforts in academia and industry. Herein, we report the nonclinical and early clinical development of LY2886721, a BACE1 active site inhibitor that reached phase 2 clinical trials in AD. LY2886721 has high selectivity against key off-target proteases, which efficiently translates in vitro activity into robust in vivo amyloid beta lowering in nonclinical animal models. Similar potent and persistent amyloid beta lowering was observed in plasma and lumbar CSF when single and multiple doses of LY2886721 were administered to healthy human subjects. Collectively, these data add support for BACE1 inhibition as an effective means of amyloid lowering and as an attractive target for potential disease modification therapy in AD.