Palmatine hydroxide - ≥99% , CAS No.131-04-4

CAS: 131-04-4 Cat. No.: P648530 Fórmula: C₂₁H₂₃NO₅ Peso molecular: 369.41 PubChem CID: 200119

GRADE & PURITY ≥99%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Descripción general

Palmatine hydroxide is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC 50 s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine hydroxide can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC 50 of 96 μM. Palmatine hydroxide shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities

In Vitro

Palmatine (0-100 μM; 42 h) suppresses WNV with an EC 50 value of 3.6 μM, and reduce the viral titers of DENV-2 and YFV with EC 50 values of 26.4 μM and 7.3 μM, respectively. Palmatine (0-1128 μM; 24-72 h) inhibits colon cancer cell proliferation . Palmatine (0-704 μM; 24 h) reduces AURKA protein levels, induces G2/M phase arrest, and induces apoptosis in colon cancer cells via the mitochondrial associated pathway . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation Assay Cell Line: HCT-116, SW480, HT-29 Concentration: 0, 88, 176, 352, and 704 μM (HCT-116, SW480); 0, 141, 282, 564, and 1128 μM (HT-29) Incubation Time: 24, 48 and 72 h Result: Decreased cell viability in a dose-dependent manner. Western Blot Analysis Cell Line: HCT-116, SW480, HT-29 Concentration: 100 nM for HCT-116, 500 nM for SW480 and HT-29 Incubation Time: 24, 48 and 72 h Result: Promoted the expression of apoptosis markers such as P53 / P73, Caspase3, and Caspase9. Reduced AURKA protein levels. Increased cyt. c in the cytoplasm while reduced Bcl2 and Bcl-xl in a dose-dependent manner. Cell Cycle Analysis Cell Line: HCT-116, SW480 Concentration: 88, 176, 352 and 704 μM Incubation Time: 24, 48 and 72 h Result: Induced G2/M phase arrest in a dose-dependent manner. Apoptosis Analysis Cell Line: HCT-116, SW480 Concentration: 88, 176, 352 and 704 μM Incubation Time: 24, 48 and 72 h Result: Induced apoptosis in a dose-dependent manner.

In Vivo

Palmatine (50 or 100 mg/kg; p.o.; daily for 7 days) ameliorates DSS (dextran sulfate sodium)-induced colitis and prevents infiltration of inflammatory cells . Palmatine (0-200 mg/kg; i.p.; once) attenuates D-galactosamine/ Lipopolysaccharides -induced fulminant hepatic failure in mice. Palmatine (0-1 mg/kg; i.p.; 10 days) shows memory-enhancing activity in mice. Palmatine (33.75-135 mg/kg; p.o.; daily for 26 days) can effectively inhibit the growth of HCT-116 xenografts in mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: DSS- induced Colitis BALB/c mice model (8-week-old) Dosage: 50 or 100 mg/kg Administration: Orally, daily, for 7 days Result: Ameliorated DSS-induced colitis and prevented infiltration of inflammatory cells; remarkably extended the colon length; significantly suppressed the colonic MPO activity. Decreased the levels of colonic inflammatory cytokines (TNF-α, IFN-γ, IL-1β, IL-6, IL-4 and IL-10); Protected mucosal integrity by modulating TJs protein and apoptosis proteins; Restored DSS-induced decreases of TJ protein ZO-1, ZO-2 and claudin-1; Reduced Bax expression and enhanced Bcl-2 expression at the dose of 100 mg/kg, prevented epithelial apoptosis and improved intestinal integrity. Prevented DSS-induced changes of gut microbiota in colitis mice. Animal Model: Male ICR mice (20–22 g), D-galactosamine/lipopolysaccharide (GalN/LPS)-induced fulminant hepatic failure modelDosage: 25, 50, 100, or 200 mg/kg Administration: Intraperitoneal injection, 1 h before the GalN/LPS treatment Result: Attenuated the mortality and serum aminotransferase activities increased by GalN/LPS. Prevented the increase of serum TNF-α and augmented that of serum IL-10. Decreased the TNF-a mRNA expression and increased the IL-10 mRNA expression. Attenuated the apoptosis of hepatocytes. Animal Model: Swiss young male albino mice, with Scopolamine - and diazepam-induced amnesia modelDosage: 0.1, 0.5, 1 mg/kg Administration: Intraperitoneal injection, 10 days Result: Significantly improved learning and memory of mice at 0.5 and 1 mg/kg and did not show any significant effect on locomotor activity of the mice. Significantly reversed scopolamine- and diazepam-induced amnesia in mice. Significantly reduced brain acetylcholinesterase activity of mice. Animal Model: BALB/c-nude mice, HCT-116 xenograft modelDosage: 33.75, 67.5 and 135 mg/kg Administration: Oral administration, once a day for 26 days Result: The tumor volume and weight of the treatment group were significantly reduced.

Form:Solid

IC50& Target:IDO-1 3 μM (IC 50 , HEK 293-hIDO-1) IDO-1 157 μM (IC 50 , rhIDO-1) WNV NS2B-NS3 96 μM (IC 50 )

Specifications

Especificaciones y pureza

≥99%

Mecanismos bioquímicos y fisiológicos

Palmatine hydroxide is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC 50 s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine hydroxide can also inhibit West Nile virus (WNV) NS2B-NS3 p

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

INHIBITOR

Pureza

≥99%

Nombres e identificadores

• Isómeros SMILES: COC1=C(C2=C[N+]3=C(C=C2C=C1)C4=CC(=C(C=C4CC3)OC)OC)OC.[OH-]
• PubChem CID: 200119
• Peso molecular: 369.41

Propiedades químicas y físicas

• Solubilidad: DMSO : 15.62 mg/mL (42.28 mM; ultrasonic and warming and heat to 60°C)
• Peso molecular: 369.400 g/mol
• Hydrogen Bond Donor Count: 1
• Hydrogen Bond Acceptor Count: 5
• Rotatable Bond Count: 4
• Exact Mass: 369.158 Da
• Monoisotopic Mass: 369.158 Da
• Topological Polar Surface Area: 41.800 Ų
• Heavy Atom Count: 27
• Formal Charge: 0
• Complexity: 475.000
• 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: 2

XLogP3

Preguntas frecuentes

What is the purity of this product?

This product is supplied at ≥99% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 131-04-4, the molecular formula is C21H23NO5, and the molecular weight is 369.41 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.