MRK 560
Tocris Bioscience, part of Bio-Techne | Catalog # 4000
γ-secretase inhibitor; attenuates amyloid plaque deposition
Key Product Details
Description
γ-secretase inhibitor; attenuates amyloid plaque deposition
Product Description
MRK 560 is a γ-secretase inhibitor, which selectively inhibits proteolytic cleavage of amyloid precursor protein (APP) over the Notch pathway. MRK 560 reduces levels of Aβ in vitro (inhibits Aβ40 and Aβ42 in SH-SY5Y neuroblastoma cells with an IC50 of 0.65 nM) and attenuates plaque deposition. This compound is orally bioavailable.Licensing Information
Manufactured and sold under license from Merck & Co., Inc. for use solely for preclinical research purposes (ie: not for administration to or other use in humans).Extrernal Portal Information
The Chemical Probes webpages of the Structural Genomics Consortium are a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of MRK 560 is reviewed.Product Specifications
Molecular Weight
517.92
Formula
C19H17ClF5NO4S2
Storage
Store at +4°C
Purity
≥98% (HPLC)
Chemical Name
N-[cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide
CAS Number
677772-84-8
PubChem ID
11577204
InChI Key
WDZVWDXOIGQJIO-UJKQEGAGSA-N
SMILES
FC1=CC(=C(F)C=C1)[C@]1(CC[C@@H](CC1)N[S](=O)(=O)C(F)(F)F)[S](=O)(=O)C1=CC=C(Cl)C=C1
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 51.79 | 100 | |
| Ethanol | 25.9 | 50 |
Preparing Stock Solutions
for MRK 560
The following data is based on the product molecular weight 517.92
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.93 mL | 9.65 mL | 19.31 mL |
| 5 mM | 0.39 mL | 1.93 mL | 3.86 mL |
| 10 mM | 0.19 mL | 0.97 mL | 1.93 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.39 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Best The novel γ-secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) reduces amyloid plaque deposition without evidence of Notch-related pathology in the T J.Pharm.Exp.Ther. 2007 PMID: 17099072
- Best In vivo characterization of Aβ(40) changes in brain and cerebrospinal fluid using the novel γ-secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) J.Pharm.Exp.Ther. 2006 PMID: 16443723
Product Specific Notices for MRK 560
For research use only
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