1. Neuronal Signaling
  2. Beta-secretase
  3. LY2886721

LY2886721 

製品番号: HY-13240 純度: 99.92%
取扱説明書

LY2886721 is a potent, selective and orally active beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 20.3 nM for recombinant human BACE1. LY2886721 is selectivity against cathepsin D, pepsin, and renin, but lacking selectivity against BACE2 (IC50 of 10.2 nM). LY2886721 can across blood-brain barrier and has the potential for Alzheimer's disease treatment.

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LY2886721 構造式

LY2886721 構造式

CAS 番号 : 1262036-50-9

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1 mL in DMSO USD 119 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 108 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 168 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 468 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 780 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 1 publication(s) in Google Scholar

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製品説明

LY2886721 is a potent, selective and orally active beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 20.3 nM for recombinant human BACE1. LY2886721 is selectivity against cathepsin D, pepsin, and renin, but lacking selectivity against BACE2 (IC50 of 10.2 nM). LY2886721 can across blood-brain barrier and has the potential for Alzheimer's disease treatment[1].

IC50 & Target

IC50: 20.3 nM (Beta-site amyloid precursor protein cleaving enzyme 1 (BACE1)); 10.2 nM (BACE2)[1]

体外実験

Overnight exposure of HEK293Swe cells to increasing concentrations of LY2886721 shows a concentration-dependent decrease in the amount of Aβ secreted into the condition medium. Consistent with a mechanism of BACE inhibition, the EC50s for inhibition of Aβ1-40 and Aβ1-42 are essentially identical, 18.5 and 19.7 nM, respectively[1].
Overnight exposure of PDAPP neuronal cultures to an increasing concentration of LY2886721 produces a concentration-dependent decrease in Aβ production. As observed in HEK293Swe cells, the EC50s for inhibition of Aβ1-40 and Aβ1-42 are comparable in PDAPP neuronal cultures at ∼10 nM[1].

体内実験

LY2886721 (3-30 mg/kg; oral administration; PDAPP mice) treatment significantly reduces the hippocampal and cortical levels of Aβ1-x. LY2886721 treatment results in significant reduction of brain parenchymal levels of C99 and sAPPβ[1].

Animal Model: Female hemizygous APPV717F transgenic mice (PDAPP) (2-3 months old)[1]
Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg
Administration: Oral administration
Result: Hippocampal and cortical levels of Aβ1-x were significantly reduced.
臨床実験
分子量

390.41

分子式

C₁₈H₁₆F₂N₄O₂S

CAS 番号

1262036-50-9

SMILES

FC1=CN=C(C=C1)C(NC2=CC=C(C([[email protected]@]34[[email protected]]([H])(CSC(N)=N4)COC3)=C2)F)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : ≥ 42 mg/mL (107.58 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5614 mL 12.8070 mL 25.6141 mL
5 mM 0.5123 mL 2.5614 mL 5.1228 mL
10 mM 0.2561 mL 1.2807 mL 2.5614 mL
*Please refer to the solubility information to select the appropriate solvent.
参考文献

純度: 99.92%

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Keywords:

LY2886721LY 2886721LY-2886721Beta-secretaseBACEβ-SecretaseAlzheimer'sdiseaseBACE1BACE2BBBC99sAPPβInhibitorinhibitorinhibit

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製品名:
LY2886721
製品番号:
HY-13240
数量:
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