MRK 560 |
Catalog No.GC16431
One-Click Copy Product Info
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A potent inhibitor of γ-secretase
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 677772-84-8
Sample solution is provided at 25 µL, 10mM.
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IC50: 0.65 nM for both Aβ(40) and Aβ(42)
MRK-560 is a novel γ-secretase inhibitor.
γ-Secretase is a member of the I-CLiP protease family and is reported to cleave a number of additional intramembrane substrates, including Erb4, CD-44, Notch, E-cadherin, and the Notch ligands. γ-Secretase is responsible for the intramembraneous proteolytic cleavage of the C-terminal fragment of APP, resulting in mainly Aβ(40) or Aβ(42) production.
In vitro: In SH-SY5Y neuroblastoma cells, MRK-560 inhibited the production of Aβ(40) and Aβ(42) with similar in vitro IC50 values in the range of 0.65 nM [1].
In vivo: MRK-560 was found to be able to reduce Aβ in the brain and cerebrospinal fluid (CSF) in the rat markedly, with ED50s of 6 and 10 mg/kg, respectively. Time-course experiments demonstrated the reductions in Aβ could be maintained for 24 h. Comparable temporal reductions in rat brain and CSF further suggested that these two pools of Aβ were related. Such relationship between the brain and CSF Aβ was maintained when MRK-560 was dosed once a day for 2 weeks. These results indicated that MRK-560 was a γ-secretase inhibitor with the ability to reduce Aβ peptide in the rat brain and CSF [1].
Clinical trial: N/A
Reference:
[1] Best JD,Jay MT,Otu F,Churcher I,Reilly M,Morentin-Gutierrez P,Pattison C,Harrison T,Shearman MS,Atack JR. In vivo characterization of Abeta(40) changes in brain and cerebrospinal fluid using the novel gamma-secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) in the rat. J Pharmacol Exp Ther.2006 May;317(2):786-90.
| Cas No. | 677772-84-8 | SDF | |
| Chemical Name | N-((1s,4s)-4-((4-chlorophenyl)sulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)-1,1,1-trifluoromethanesulfonamide | ||
| Canonical SMILES | O=S(C(F)(F)F)(N[C@@H]1CC[C@](C2=CC(F)=CC=C2F)(S(=O)(C3=CC=C(Cl)C=C3)=O)CC1)=O | ||
| Formula | C19H17ClF5NO4S2 | M.Wt | 517.92 |
| Solubility | <51.79mg/ml in DMSO; <25.9mg/ml in ethanol | Storage | Store at 4°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9308 mL | 9.654 mL | 19.308 mL |
| 5 mM | 386.2 μL | 1.9308 mL | 3.8616 mL |
| 10 mM | 193.1 μL | 965.4 μL | 1.9308 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)