E1231 - ≥98% , CAS No.1031195-19-3

CAS: 1031195-19-3 Cat. No.: E647878 Fórmula: C₂₁H₂₁N₃O₃ Peso molecular: 363.41 Número EC: 862-668-7 PubChem CID: 24980435

CALIDAD & PUREZA ≥98%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Descripción general

E1231 is an orally active activator of Sirtuin 1 ( SIRT1 ) ( EC 50 =0.83 μM), to modulate cholesterol and lipid metabolism. E1231 interactes with SIRT1 (K D =9.61 μM) and deacetylated liver X receptor-alpha ( LXRα ), and increases ATP-binding cassette transporter A1 (ABCA1) expression. E1231 also reduces atherosclerotic plaque development in ApoE -/- mice model. E1231 can be used for research in cholesterol and lipid disorder-related diseases

In Vitro

E1231 (0.1-10 μM; 18 h) promotes cholesterol efflux and inhibits lipid accumulation in RAW 264.7 cells. E1231 (10 μM; 6 h) significantly increases deacetylation of Doxo-induced p53 in HepG2 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

E1231 (40 mg/kg; po; once daily for 7 days) regulates cholesterol and lipid metabolism in Golden hamsters fed with HFD diet . E1231 (25, 50, and 100 mg/kg, in 0.5% CMC-Na; po; once daily for 12 weeks) reduces atherosclerosis development, without hepatotoxicity ornephrotoxicity in ApoE -/- mice fed with atherogenic diet . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: HFD-diet Golden hamsters (80-90 g) Dosage: 40 mg/kg Administration: PO; once daily for 7 days Result: Increased SIRT1 protein expression but not SIRT3, SIRT6, or SIRT7. And reduced liver and serum cholesterol in hamsters. Animal Model: Atherogenic diet ApoE -/- mice Dosage: 25, 50, and 100 mg/kg Administration: PO; once daily for 12 weeks Result: Modulated plaque composition, immunofluorescence staining. And reduced CD68 positive areas while increasing ABCA1 expression in the aortic sinus.

Form:Solid

IC50& Target:SIRT1 0.83 μM (EC 50 )

Especificaciones

Especificaciones y pureza

≥98%

Mecanismos bioquímicos y fisiológicos

E1231 is an orally active activator of Sirtuin 1 ( SIRT1 ) ( EC 50 =0.83 μM), to modulate cholesterol and lipid metabolism. E1231 interactes with SIRT1 (K D =9.61 μM) and deacetylated liver X receptor-alpha ( LXRα ), and increases ATP-binding cassette tra

Condiciones de almacenamiento de almacenamiento

Store at -20°C

Enviado en

Ice chest + Ice pads

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Tipo de acción

ACTIVATOR

Pureza

≥98%

Nombres e identificadores

Isómeros SMILES

CC1=CC=C(O1)C2=NC3=CC=CC=C3C(=C2)C(=O)N4CCN(CC4)C(=O)C

PubChem CID

24980435

Peso molecular

363.41

Objetivos asociados (humanos)

GBA1 Tclin Beta-glucocerebrosidase (14647 Activities)

Discover Target: GBA1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

GLP1R Tclin Glucagon-like peptide 1 receptor (111429 Activities)

Discover Target: GLP1R

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

HepG2 (196354 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

POLI Tchem DNA polymerase iota (116820 Activities)

Discover Target: POLI

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

BRCA1 Tchem Breast cancer type 1 susceptibility protein (15908 Activities)

Discover Target: BRCA1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

TDP1 Tchem Tyrosyl-DNA phosphodiesterase 1 (345557 Activities)

Discover Target: TDP1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

GMNN Tbio Geminin (128009 Activities)

Discover Target: GMNN

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

ATAD5 Tbio ATPase family AAA domain-containing protein 5 (122566 Activities)

Discover Target: ATAD5

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Objetivos asociados (no humanos)

GCN5 Histone acetyltransferase GCN5 (89 Activities)

Discover Target: GCN5

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Luciferin 4-monooxygenase (66902 Activities)

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Txnrd1 Thioredoxin reductase 1, cytoplasmic (45279 Activities)

Discover Target: Txnrd1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Mecanismos de acción

Propiedades químicas y físicas

• Solubilidad: DMSO : 100 mg/mL (275.17 mM; Need ultrasonic)
• Peso molecular: 363.400 g/mol
• XLogP3: 2.100
• Hydrogen Bond Donor Count: 0
• Hydrogen Bond Acceptor Count: 4
• Rotatable Bond Count: 2
• Exact Mass: 363.158 Da
• Monoisotopic Mass: 363.158 Da
• Topological Polar Surface Area: 66.700 Ų
• Heavy Atom Count: 27
• Formal Charge: 0
• Complexity: 561.000
• Isotope Atom Count: 0
• Defined Atom Stereocenter Count: 0
• Undefined Atom Stereocenter Count: 0
• Defined Bond Stereocenter Count: 0
• Undefined Bond Stereocenter Count: 0
• The total count of all stereochemical bonds: 0
• Covalently-Bonded Unit Count: 1