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2018年5月6日星期日

Original:Pifithrin-beta HBr 511296-88-1, stock more than 100g

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Description: Pifithrin-beta, also known as QB102 and Cyclic-Pifithrin-α, is is p53 functional inhibitor. Pifithrin-β counteracts the Alzheimer peptide non-β-amyloid component effects in human SH-SY5Y cells.
Name: Pifithrin-beta HBr 
CAS#: 511296-88-1 (HBr) 
Chemical Formula: C16H17BrN2S 
Exact Mass: 
Molecular Weight: 349.29 
Elemental Analysis: C, 55.02; H, 4.91; Br, 22.88; N, 8.02; S, 9.18

Related CAS #: 60477-34-1 (free base)   511296-88-1 (HBr)   2109248-93-1 (HCl)    
Synonym: Pifithrin-β; Pifithrin-beta; PFTβ; PFT-β; QB102; QB102; QB102; Cyclic-Pifithrin-α
IUPAC/Chemical Name: 5,6,7,8-Tetrahydro-2-(4-methylphenyl)imidazo[2,1-b]benzothiazole hydrobromide
InChi Key: SGNCOAOESGSEOP-UHFFFAOYSA-N
InChi Code: InChI=1S/C16H16N2S.BrH/c1-11-6-8-12(9-7-11)13-10-18-14-4-2-3-5-15(14)19-16(18)17-13;/h6-10H,2-5H2,1H3;1H
SMILES Code: CC1=CC=C(C2=CN3C(SC4=C3CCCC4)=N2)C=C1.[H]Br
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
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).
Harmonized System Code: 293490

REFERENCES
1: Lisachev PD, Pustylnyak VO, Shtark MB. Sirt1 Regulates p53 Stability and Expression of Its Target S100B during Long-Term Potentiation in Rat Hippocampus. Bull Exp Biol Med. 2016 Feb;160(4):432-4. doi: 10.1007/s10517-016-3189-5. Epub 2016 Feb 23. PubMed PMID: 26902357.
2: Da Pozzo E, La Pietra V, Cosimelli B, Da Settimo F, Giacomelli C, Marinelli L, Martini C, Novellino E, Taliani S, Greco G. p53 functional inhibitors behaving like pifithrin-β counteract the Alzheimer peptide non-β-amyloid component effects in human SH-SY5Y cells. ACS Chem Neurosci. 2014 May 21;5(5):390-9. doi: 10.1021/cn4002208. Epub 2014 Mar 28. PubMed PMID: 24646317; PubMed Central PMCID: PMC4030802.
3: Fernández-Cruz ML, Valdehita A, Alonso M, Mann E, Herradón B, Navas JM. Biological and chemical studies on aryl hydrocarbon receptor induction by the p53 inhibitor pifithrin-α and its condensation product pifithrin-β. Life Sci. 2011 Apr 25;88(17-18):774-83. doi: 10.1016/j.lfs.2011.02.019. Epub 2011 Feb 26. PubMed PMID: 21362431.
4: Christodoulou MS, Colombo F, Passarella D, Ieronimo G, Zuco V, De Cesare M, Zunino F. Synthesis and biological evaluation of imidazolo[2,1-b]benzothiazole derivatives, as potential p53 inhibitors. Bioorg Med Chem. 2011 Mar 1;19(5):1649-57. doi: 10.1016/j.bmc.2011.01.039. Epub 2011 Jan 25. PubMed PMID: 21324703.
5: Waters FJ, Shavlakadze T, McIldowie MJ, Piggott MJ, Grounds MD. Use of pifithrin to inhibit p53-mediated signalling of TNF in dystrophic muscles of mdx mice. Mol Cell Biochem. 2010 Apr;337(1-2):119-31. doi: 10.1007/s11010-009-0291-2. Epub 2009 Oct 27. PubMed PMID: 19859789.