Stock solution can be stored below -20℃ for several months. For higher solubility, warming the tube at 37 ℃ and shaking it in the ultrasonic bath is recommended.
SML2809
WNK463
≥98% (HPLC)
Sinónimos:
N-(1,1-Dimethylethyl)-1-[1-[5-[5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl]-2-pyridinyl]-4-piperidinyl]-1H-imidazole-5-carboxamide, N-tert-Butyl-1-(1-(5-(5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl)pyridin-2-yl)piperidin-4-yl)-1H-imidazole-5-carboxamide
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About This Item
Fórmula empírica (notación de Hill):
C21H24F3N7O2
Número de CAS:
Peso molecular:
463.46
Número MDL:
Código UNSPSC:
12352200
NACRES:
NA.77
En este momento no podemos mostrarle ni los precios ni la disponibilidad
Productos recomendados
Nivel de calidad
Ensayo
≥98% (HPLC)
Formulario
powder
color
white to beige
solubilidad
DMSO: 2 mg/mL, clear
temp. de almacenamiento
2-8°C
cadena SMILES
FC(F)(F)c1nnc([o]1)c2cnc(cc2)N3CCC(CC3)[n]4cncc4C(=O)NC(C)(C)C
InChI
1S/C21H24F3N7O2/c1-20(2,3)27-17(32)15-11-25-12-31(15)14-6-8-30(9-7-14)16-5-4-13(10-26-16)18-28-29-19(33-18)21(22,23)24/h4-5,10-12,14H,6-9H2,1-3H3,(H,27,32)
Clave InChI
HWSHOMMVLGBIDN-UHFFFAOYSA-N
Acciones bioquímicas o fisiológicas
Orally active, highly selective & potent ATP-competitive inhibitor against with-No-Lysine (K) kinases WNK1-4 with in vivo efficacy in rodent models of hypertension.
WNK463 is a high-affinity, ATP-competitive inhibitor against with-No-Lysine (K) kinases (hWNK1/3/4 IC50 = 5/6/9 nM with MBP & 1 μM ATP, hWNK2 IC50 = 1 nM with MBP & 2 μM ATP, hWNK1 IC50 = 41 nM with OSR1 & 0.5 μM ATP; hWNK1/4 KD = 3.71/3.84 by SPR), exhibiting weak affinity against only two other human kinases among a panel of 442. WNK463 downregulates the overexpressed OSR1 phosphorylation level in HEK293 cells (IC50 = 106 nM; 1 hr) and displays in vivo efficacy in rodent hypertension models (1-10 mg/kg in rats p.o., 10 mg/kg in hWNK1 transgenic mice p.o.) with good orally availability (F = 100%/mice & 74%/rats post 1.5 mg/kg p.o.).
Código de clase de almacenamiento
11 - Combustible Solids
Clase de riesgo para el agua (WGK)
WGK 3
Punto de inflamabilidad (°F)
Not applicable
Punto de inflamabilidad (°C)
Not applicable
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Certificados de análisis (COA)
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Encuentre la documentación para los productos que ha comprado recientemente en la Biblioteca de documentos.
Jinwei Zhang et al.
Science signaling, 9(450), e3-e3 (2016-11-05)
The with-no-lysine (K) WNK kinases are master regulators of the Na+-(K+)-Cl- cotransporters, including the renal-specific NCC and NKCC2 cotransporters. The discovery of WNK463, an orally bioavailable pan-WNK kinase inhibitor that exploits unique structural properties of the WNK catalytic domain to
Ken Yamada et al.
Nature chemical biology, 12(11), 896-898 (2016-10-19)
The With-No-Lysine (K) (WNK) kinases play a critical role in blood pressure regulation and body fluid and electrolyte homeostasis. Herein, we introduce the first orally bioavailable pan-WNK-kinase inhibitor, WNK463, that exploits unique structural features of the WNK kinases for both
Melaine A Kuenemann et al.
Molecular informatics, 37(6-7), e1700138-e1700138 (2018-02-24)
The With-No-Lysine (WNK) serine/threonine kinase family constitutes a unique and distinctive branch of the kinome. The four proteins of this family (WNK1/2/3/4) are involved in blood pressure regulation, body fluid, and electrolyte homeostasis. Herein, we modeled and analyzed the binding
Adam Volanakis et al.
Genes & development, 31(21), 2175-2185 (2017-12-03)
Nuclear gene transcription is coordinated with transcript release from the chromatin template and messenger RNA (mRNA) export to the cytoplasm. Here we describe the role of nuclear-localized kinase WNK1 (with no lysine [K] 1) in the mammalian mRNA export pathway
Ken Yamada et al.
ACS chemical biology, 11(12), 3338-3346 (2016-10-08)
Protein kinases are known for their highly conserved adenosine triphosphate (ATP)-binding site, rendering the discovery of selective inhibitors a major challenge. In theory, allosteric inhibitors can achieve high selectivity by targeting less conserved regions of the kinases, often with an
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