PE859
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MedKoo CAT#: 530903

CAS#: 1402727-29-0

Description: 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

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PE859
CAS# 1402727-29-0

Theoretical Analysis

MedKoo Cat#: 530903
Name: PE859
CAS#: 1402727-29-0
Chemical Formula: C28H24N4O2
Exact Mass: 448.19
Molecular Weight: 448.526
Elemental Analysis: C, 74.98; H, 5.39; N, 12.49; O, 7.13

Price and Availability

Size Price Availability Quantity
100mg USD 1450
200mg USD 1850
500mg USD 2750
1g USD 3650
2g USD 4950
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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:
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/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 50.0 111.84

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.

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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.