.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: 317.43 YYA-021 es un inhibidor de entrada del VIH que imita a CD4, que inhibe competitivamente la interacción entre gp120 y CD4. \ n Actividad biológica
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Description
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YYA-021 is a CD4-mimic HIV entry inhibitor, competitively inhibiting the interaction between gp120 and CD4.
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Targets
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gp120 [1]
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In vitro
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YYA-021 enhances the neutralization sensitivity of simian-human immunodeficiency virus (SHIV) carrying the envelope from the clade B clinical human immunodeficiency virus type 1 (HIV-1) isolate MNA.
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In vivo
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In rats and rhesus macaques, YYA-021 (i.v.) shows moderate half-lives, wide tissue distribution and relatively high distribution volumes.
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Features
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Protocolo (solo como referencia) Estudio en animales: [2]
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Animal Models
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Rats and rhesus macaques
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Formulation
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Converted to its hydrochloride salt by treatment with 4 M HCl in dioxane.
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Dosages
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14 mg/kg (rats), 13.4 mg/kg (rhesus macaques)
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Administration
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i.v.
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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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317.43
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Formula
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C18 H27 N3 O2
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CAS No.
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144217-65-2
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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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N/A
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Solubility (25°C) *
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In vitro
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DMSO
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0.01 mg/mL
(
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Water
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<1 mg/mL
(
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Ethanol
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<1 mg/mL
(
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Chemical Name
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Ethanediamide, N1-(4-methylphenyl)-N2-(2,2,6,6-tetramethyl-4-piperidinyl)-
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Calculadora de molaridad Calculadora de dilución Calculadora de peso molecular
Grupos de Producto : Otros > Inhibidor de gp120 / CD4
