Free shipping on all orders over $ 500

PF-06751979

Cat. No. M13414
PF-06751979  Structure
Size Price Availability
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

PF-06751979 is a potent, brain permeable inhibitor of β -amyloid precursor protein lyase 1 (BACE1) with an IC50 of 7.3 nM.

Chemical Information
Molecular Weight 455.5
Formula C18H19F2N5O3S2
CAS Number 1818339-66-0
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Alvaro Miranda, et al. J Alzheimers Dis. Selective Secretase Targeting for Alzheimer's Disease Therapy

[2] Ruolun Qiu, et al. J Alzheimers Dis. Safety, Tolerability, Pharmacokinetics, and Pharmacodynamic Effects of PF-06751979, a Potent and Selective Oral BACE1 Inhibitor: Results from Phase I Studies in Healthy Adults and Healthy Older Subjects

[3] Brian T O'Neill, et al. J Med Chem. Design and Synthesis of Clinical Candidate PF-06751979: A Potent, Brain Penetrant, β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor Lacking Hypopigmentation

Related BACE Products
Se-Methylselenocysteine hydrochloride

Se-Methylselenocysteine hydrochloride, a precursor of Methylselenol, has potent cancer chemopreventive activity and anti-oxidant activity.

Glabrolide

Glabrolide, derived from Glycyrrhiza uralensis Fisch., is a β-secretase 1 (BACE-1) inhibitor.

Kushenol C

Kushenol C, isolated from the roots of Sophora flavescens, shows anti-Inflammatory and anti-oxidative stress activities. Kushenol C inhibits BACE1 (β-site APP cleaving enzyme 1) with an IC50 of 5.45 µM.

Deoxyneocryptotanshinone

Deoxyneocryptotanshinone is a high affinity BACE1 (Beta-secretase) inhibitor with an IC50 value of 11.53 μM. Deoxyneocryptotanshinone shows a promising dose-dependent inhibition of protein tyrosine phosphatase 1B (PTP1B) with an IC50 value of 133.5 μM.

β-Secretase Inhibitor IV

β-Secretase Inhibitor IV is a cellular permeability inhibitor that binds to the active site of BACE-1 and blocks its proteolytic activity (IC₅₀= 15 nM in human BACE-1).

  Catalog
Abmole Inhibitor Catalog




Keywords: PF-06751979 supplier, BACE, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.