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MedKoo Cat#: 530903 | Name: PE859
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

PE859 is a potent inhibitor of both tau and Aβ aggregation with IC50 values of 0.66 and 1.2 μM, respectively. PE859 inhibits Amyloid-β and Tau Aggregation, and Ameliorates Cognitive Dysfunction in Senescence-Accelerated Mouse Prone 8. PE859 reduces aggregated tau and prevents onset and progression of neural dysfunction in vivo.

Chemical Structure

PE859
PE859
CAS#1402727-29-0

Theoretical Analysis

MedKoo Cat#: 530903

Name: PE859

CAS#: 1402727-29-0

Chemical Formula: C28H24N4O2

Exact Mass: 448.1899

Molecular Weight: 448.53

Elemental Analysis: C, 74.98; H, 5.39; N, 12.49; O, 7.13

Price and Availability

Size Price Availability Quantity
100mg USD 1,450.00 2 Weeks
200mg USD 1,850.00 2 Weeks
500mg USD 2,750.00 2 Weeks
1g USD 3,650.00 2 Weeks
2g USD 4,950.00 2 Weeks
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Related CAS #
No Data
Synonym
PE859; PE-859; PE 859.
IUPAC/Chemical Name
6-((E)-2-(5-((E)-2-methoxy-4-(pyridin-2-ylmethoxy)styryl)-1H-pyrazol-3-yl)vinyl)-1H-indole
InChi Key
AMBZHNVCLPHAKA-NSJFVGFPSA-N
InChi Code
InChI=1S/C28H24N4O2/c1-33-28-18-26(34-19-25-4-2-3-14-29-25)12-9-22(28)8-11-24-17-23(31-32-24)10-6-20-5-7-21-13-15-30-27(21)16-20/h2-18,30H,19H2,1H3,(H,31,32)/b10-6+,11-8+
SMILES Code
COC1=CC(OCC2=NC=CC=C2)=CC=C1/C=C/C3=CC(/C=C/C4=CC5=C(C=C4)C=CN5)=NN3
Appearance
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
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
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
PE859 is a potent inhibitor of both tau and Aβ aggregation with IC50 values of 0.66 and 1.2 μM.
In vitro activity:
This study investigated the inhibitory activity of PE859 on Aβ aggregationin vitro and the therapeutic effects of PE859 on cognitive dysfunction via dual inhibition of Aβ and tau aggregation in vivo. PE859 inhibited Aβ aggregation in vitro and protected cultured cells from Aβ-induced cytotoxicity. Reference: J Alzheimers Dis. 2017;59(1):313-328. https://pubmed.ncbi.nlm.nih.gov/28598836/
In vivo activity:
This study identified a novel tau aggregation inhibitor, PE859. An oral administration of PE859 resulted in the significant reduction of sarkosyl-insoluble aggregated tau along with the prevention of onset and progression of the motor dysfunction in JNPL3 P301L-mutated human tau transgenic mice. These results suggest that PE859 is useful for the treatment of tauopathies. Reference: PLoS One. 2015 Feb 6;10(2):e0117511. https://pubmed.ncbi.nlm.nih.gov/25659102/
Solvent mg/mL mM
Solubility
DMSO 50.0 111.84
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 448.53 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.

Recalculate based on batch purity %
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
Formulation protocol:
1. Okuda M, Fujita Y, Hijikuro I, Wada M, Uemura T, Kobayashi Y, Waku T, Tanaka N, Nishimoto T, Izumi Y, Kume T, Akaike A, Takahashi T, Sugimoto H. PE859, A Novel Curcumin Derivative, Inhibits Amyloid-β and Tau Aggregation, and Ameliorates Cognitive Dysfunction in Senescence-Accelerated Mouse Prone 8. J Alzheimers Dis. 2017;59(1):313-328. doi: 10.3233/JAD-161017. PMID: 28598836. 2. Okuda M, Hijikuro I, Fujita Y, Wu X, Nakayama S, Sakata Y, Noguchi Y, Ogo M, Akasofu S, Ito Y, Soeda Y, Tsuchiya N, Tanaka N, Takahashi T, Sugimoto H. PE859, a novel tau aggregation inhibitor, reduces aggregated tau and prevents onset and progression of neural dysfunction in vivo. PLoS One. 2015 Feb 6;10(2):e0117511. doi: 10.1371/journal.pone.0117511. PMID: 25659102; PMCID: PMC4319983.
In vitro protocol:
Okuda M, Fujita Y, Hijikuro I, Wada M, Uemura T, Kobayashi Y, Waku T, Tanaka N, Nishimoto T, Izumi Y, Kume T, Akaike A, Takahashi T, Sugimoto H. PE859, A Novel Curcumin Derivative, Inhibits Amyloid-β and Tau Aggregation, and Ameliorates Cognitive Dysfunction in Senescence-Accelerated Mouse Prone 8. J Alzheimers Dis. 2017;59(1):313-328. doi: 10.3233/JAD-161017. PMID: 28598836.
In vivo protocol:
Okuda M, Hijikuro I, Fujita Y, Wu X, Nakayama S, Sakata Y, Noguchi Y, Ogo M, Akasofu S, Ito Y, Soeda Y, Tsuchiya N, Tanaka N, Takahashi T, Sugimoto H. PE859, a novel tau aggregation inhibitor, reduces aggregated tau and prevents onset and progression of neural dysfunction in vivo. PLoS One. 2015 Feb 6;10(2):e0117511. doi: 10.1371/journal.pone.0117511. PMID: 25659102; PMCID: PMC4319983.
1: Okuda M, Fujita Y, Hijikuro I, Wada M, Uemura T, Kobayashi Y, Waku T, Tanaka N, Nishimoto T, Izumi Y, Kume T, Akaike A, Takahashi T, Sugimoto H. PE859, A Novel Curcumin Derivative, Inhibits Amyloid-β and Tau Aggregation, and Ameliorates Cognitive Dysfunction in Senescence-Accelerated Mouse Prone 8. J Alzheimers Dis. 2017;59(1):313-328. doi: 10.3233/JAD-161017. PubMed PMID: 28598836. 2: Okuda M, Hijikuro I, Fujita Y, Teruya T, Kawakami H, Takahashi T, Sugimoto H. Design and synthesis of curcumin derivatives as tau and amyloid β dual aggregation inhibitors. Bioorg Med Chem Lett. 2016 Oct 15;26(20):5024-5028. doi: 10.1016/j.bmcl.2016.08.092. Epub 2016 Aug 31. PubMed PMID: 27624076. 3: Okuda M, Hijikuro I, Fujita Y, Wu X, Nakayama S, Sakata Y, Noguchi Y, Ogo M, Akasofu S, Ito Y, Soeda Y, Tsuchiya N, Tanaka N, Takahashi T, Sugimoto H. PE859, a novel tau aggregation inhibitor, reduces aggregated tau and prevents onset and progression of neural dysfunction in vivo. PLoS One. 2015 Feb 6;10(2):e0117511. doi: 10.1371/journal.pone.0117511. eCollection 2015. PubMed PMID: 25659102; PubMed Central PMCID: PMC4319983. 4: Urano Y, Takahachi M, Higashiura R, Fujiwara H, Funamoto S, Imai S, Futai E, Okuda M, Sugimoto H, Noguchi N. Curcumin Derivative GT863 Inhibits Amyloid-Beta Production via Inhibition of Protein N-Glycosylation. Cells. 2020 Feb 3;9(2):349. doi: 10.3390/cells9020349. PMID: 32028683; PMCID: PMC7072163.