1. Neuronal Signaling
  2. Beta-secretase
  3. BACE1-IN-5

BACE1-IN-5 

Cat. No.: HY-130244
Handling Instructions

BACE1-IN-5 (Compound 15) is a β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 9.1 nM, and also inhibits cellular amyloid-β (Aβ) with an IC50 of 0.82 nM. BACE1-IN-5 has a medicinal chemistry that improves hERG inhibition and P-gp efflux.

For research use only. We do not sell to patients.

BACE1-IN-5 Chemical Structure

BACE1-IN-5 Chemical Structure

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Description

BACE1-IN-5 (Compound 15) is a β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 9.1 nM, and also inhibits cellular amyloid-β (Aβ) with an IC50 of 0.82 nM. BACE1-IN-5 has a medicinal chemistry that improves hERG inhibition and P-gp efflux[1].

IC50 & Target

IC50: 9.1 nM (BACE1); 0.82 nM (cellular amyloid-β)[1]

In Vivo

BACE1-IN-5 (Compound 15; 1-3 mg/kg; oral administration; for 2-6 hours; male ICR mice) treatment results in a significant and dose-dependent decrease of total Aβ, reduces total Aβ by 76% (4 hours) at a free brain concentration of 4.1 ng/mL (8.9 nM) at 1 mg/kg. BACE1-IN-5 demonstrats a Kp,uu value of 1.3 at 1 mg/kg (4 hours time point). At 3 mg/kg, a maximum Aβ reduction of 87% is achieved at a free brain concentration of 9.5 ng/mL (21 nM) [1].

Animal Model: Male ICR mice[1]
Dosage: 1 mg/kg, 3 mg/kg
Administration: Oral administration; for 2 hours, 4 hours, and 6 hours
Result: A significant and dose-dependent decrease of total Aβ was seen, reduced total Aβ by 76% (4 h) at a free brain concentration of 4.1 ng/mL (8.9 nM) at 1 mg/kg. Demonstrats a Kp,uu value close to 1 (Kp,uu of 1.3) at 1 mg/kg (4 h time point). At 3 mg/kg, a maximum Aβ reduction of 87% was achieved at a free brain concentration of 9.5 ng/mL (21 nM).
Molecular Weight

461.41

Formula

C₁₈H₁₆F₅N₅O₂S

SMILES

O=C(C1=NC=C(OCF)N=C1)NC2=CC=C(F)C([[email protected]@]3(C)N=C(N)S[[email protected]](C(F)(F)F)C3)=C2

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Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Product Name:
BACE1-IN-5
Cat. No.:
HY-130244
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