WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 510226
CAS#: 677772-84-8
Description: MRK-560 is an orally bioavailable gamma-secretase inhibitor with the ability to markedly reduce Abeta peptide in the brain and CSF of the rat and confirm the utility of the rat for assessing the effects of gamma-secretase inhibitors on central nervous system Abeta(40) levels in vivo.
MedKoo Cat#: 510226
Name: MRK-560
CAS#: 677772-84-8
Chemical Formula: C19H17ClF5NO4S2
Exact Mass: 517.02077
Molecular Weight: 517.92
Elemental Analysis: C, 44.06; H, 3.31; Cl, 6.85; F, 18.34; N, 2.70; O, 12.36; S, 12.38
Synonym: MRK560; MRK 560; MRK-560
IUPAC/Chemical Name: N-((1r,4r)-4-((4-chlorophenyl)sulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)-1,1,1-trifluoromethanesulfonamide
InChi Key: WDZVWDXOIGQJIO-PPUGGXLSSA-N
InChi Code: InChI=1S/C19H17ClF5NO4S2/c20-12-1-4-15(5-2-12)31(27,28)18(16-11-13(21)3-6-17(16)22)9-7-14(8-10-18)26-32(29,30)19(23,24)25/h1-6,11,14,26H,7-10H2/t14-,18-
SMILES Code: 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
Appearance: white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
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 will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Wang FH, Appelkvist P, Klason T, Gissberg O, Bogstedt A, Eliason K, Martinsson S, Briem S, Andersson A, Visser SA, Ivarsson M, Lindberg M, Agerman K, Sandin J. Decreased axonal transport rates in the Tg2576 APP transgenic mouse: improvement with the gamma-secretase inhibitor MRK-560 as detected by manganese-enhanced MRI. Eur J Neurosci. 2012 Nov;36(9):3165-72. doi: 10.1111/j.1460-9568.2012.08258.x. Epub 2012 Sep 10. PubMed PMID: 22958226.
2: Best JD, Smith DW, Reilly MA, O'Donnell R, Lewis HD, Ellis S, Wilkie N, Rosahl TW, Laroque PA, Boussiquet-Leroux C, Churcher I, Atack JR, Harrison T, Shearman MS. The novel gamma secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifl uoromethanesulfonamide (MRK-560) reduces amyloid plaque deposition without evidence of notch-related pathology in the Tg2576 mouse. J Pharmacol Exp Ther. 2007 Feb;320(2):552-8. Epub 2006 Nov 10. PubMed PMID: 17099072.
3: 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-trifl uoromethanesulfonamide (MRK-560) in the rat. J Pharmacol Exp Ther. 2006 May;317(2):786-90. Epub 2006 Jan 27. PubMed PMID: 16443723.
