.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: \ n 383.46 Losmapimod (GW856553X) es un inhibidor de MAPK de p38 selectivo, potente y activo por vía oral con pKi de 8.1 y 7.6 para p38α y p38β, respectivamente. Fase 3. \ n Actividad biológica
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Description
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Losmapimod (GW856553X) is a selective, potent, and orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively. Phase 3.
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Targets
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p38α [1]
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p38β [1]
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IC50
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8.1(pKi)
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7.6(pKi)
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In vitro
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In vivo
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In spontaneously hypertensive stroke-prone rats (SHR-SP), Losmapimod significantly improves survival, endothelial-dependent and -independent vascular relaxation, and indices of renal function, and subsequently attenuates dyslipidemia, hypertension, cardiac remodeling, plasma renin activity (PRA), aldosterone, and interleukin-1beta (IL-1beta).
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Features
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Protocolo (solo como referencia) Ensayo de quinasa: [1]
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In vitro assay
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Inhibition of p38α and p38β are determined by use of a ligand-displacement fluorescence polarization assay.
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Estudio con animales: [1]
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Animal Models
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Spontaneously hypertensive stroke-prone rats
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Formulation
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Dosages
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~12 mg/kg
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Administration
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p.o.
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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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Información química
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Molecular Weight (MW)
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383.46
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Formula
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C22 H26 F N3 O2
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CAS No.
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585543-15-3
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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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GW856553, GSK-AHAB
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Solubility (25°C) *
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In vitro
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DMSO
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76 mg/mL
(198.19 mM)
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Water
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<1 mg/mL
(
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Ethanol
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41 mg/mL
heating
(106.92 mM)
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* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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Chemical Name
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3-Pyridinecarboxamide, 6-[5-[(cyclopropylamino)carbonyl]-3-fluoro-2-methylphenyl]-N-(2,2-dimethylpropyl)-
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Calculadora de molaridad Calculadora de dilución Calculadora de peso molecular
Grupos de Producto : MAPK > Inhibidor p38 MAPK
