.cp_wz table {border-top: 1px solid #ccc; border-left: 1px solid #ccc; } .cp_wz table td {border-right: 1px solid #ccc; borda inferior: 1px sólido #ccc; preenchimento: 5px 0px 0px 5px;} .cp_wz tabela th {border-right: 1px solid #ccc; border-bottom: 1px solid #ccc; preenchimento: 5px 0px 0px 5px;} \ n Peso molecular: 420,63 O ácido obeticólico é um potente e seletivo agonista do receptor farnesóide X (FXR) com EC50 de 99 nM. Fase 3. \ n Atividade 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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Ensaio de cinase de protocolo (apenas para referência): [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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Estudo Animal: [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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Conversão de diferentes modelos de animais com base em BSA (valor com base em dados das diretrizes preliminares da 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 exemplo, para modificar a dose de resveratrol usada para um camundongo (22,4 mg / kg) para uma dose baseada na BSA para um rato, multiplique 22,4 mg / kg pelo fator Km para um camundongo e, em seguida, divida pelo fator Km para um rato. Este cálculo resulta em uma dose equivalente de rato para o 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 Informação 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 molaridade Calculadora de diluição Calculadora de peso molecular
Grupo de Produto : Outros > Inibidor FXR
