.cp_wz tabla {borde superior: 1px sólido #ccc; borde izquierdo: 1px sólido #ccc; } .cp_wz table td {borde derecho: 1px sólido #ccc; borde inferior: 1px sólido #ccc; padding: 5px 0px 0px 5px;} .cp_wz table th {border-right: 1px solid #ccc; border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;} \ n Peso molecular: 420,63 El ácido obeticólico es un agonista potente y selectivo del receptor X farnesoide (FXR) con una CE50 de 99 nM. Fase 3. \ n Actividad biológica
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Description
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Obeticholic Acid is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. Phase 3.
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Targets
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FXR [1]
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IC50
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99 nM(EC50)
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In vitro
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In HuH7 cells, Obeticholic Acid acts as a potent FXR agonist with EC50 of 85 nM.
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In vivo
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In rat cholestasis model, Obeticholic Aci promotes bile flow, and protects hepatocytes against acute necrosis caused by LCA. Obeticholic Acid (p.o.) improves proteinuria, ameliorates renal structural changes, and modulates renal inflammation and oxidative stress in WD-fed DBA mice. In thioacetamide (TAA)-intoxicated and bile-duct-ligated (BDL) rats, Obeticholic Acid (30 mg/kg p.o.) reactivates the FXR downstream signaling pathway and decreases portal pressure by lowering total IHVR without deleterious systemic hypotension.
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Features
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Protocolo (solo como referencia) Ensayo de quinasa: [1]
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Binding Potency of Obeticholic Acid to FXR
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The compound is tested in an established cell-free ligand sensing assay, which measures the ligand-dependent recruitment of an SRC1 peptide to FXR by fluorescence resonance energy transfer.
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Estudio con animales: [1]
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Animal Models
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Rat cholestasis model
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Formulation
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7 μmol/kg/min
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Dosages
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Saline
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Administration
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Infused at the right jugular vein using PE-50 polyethylene tubing
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Conversión de diferentes modelos de animales basados en BSA (valor basado en datos del Borrador de Directrices de la FDA)
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Species
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Baboon
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Dog
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Monkey
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Rabbit
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Guinea pig
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Rat
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Hamster
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Mouse
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Weight (kg)
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12
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10
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3
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1.8
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0.4
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0.15
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0.08
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0.02
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Body Surface Area (m2)
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0.6
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0.5
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0.24
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0.15
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0.05
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0.025
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0.02
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0.007
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Km factor
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20
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20
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12
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12
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8
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6
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5
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3
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Animal A (mg/kg) = Animal B (mg/kg) multiplied by
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Animal B Km
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Animal A Km
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Por ejemplo, para modificar la dosis de resveratrol utilizada para un ratón (22,4 mg / kg) a una dosis basada en el BSA para una rata, multiplique 22,4 mg / kg por el factor Km para un ratón y luego divida por el factor Km para una rata. Este cálculo da como resultado una dosis equivalente para ratas de resveratrol de 11,2 mg / kg.
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Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×
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mouse Km(3)
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= 11.2 mg/kg
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rat Km(6)
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\ n Información química
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Molecular Weight (MW)
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420.63
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Formula
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C26H44O4
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CAS No.
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459789-99-2
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Storage
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3 years -20℃Powder
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6 months-80℃in solvent (DMSO, water, etc.)
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Synonyms
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INT-747, 6-ECDCA
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Solubility (25°C) *
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In vitro
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DMSO
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84 mg/mL
(199.7 mM)
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Water
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<1 mg/mL
(
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Ethanol
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84 mg/mL
(199.7 mM)
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Chemical Name
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(3α,5β,6α,7α)-6-ethyl-3,7-dihydroxy-cholan-24-oic acid
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Calculadora de molaridad Calculadora de dilución Calculadora de peso molecular
Grupos de Producto : Otros > Inhibidor de FXR
