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WNK463

Product Name
WNK463
CAS No.
2012607-27-9
Chemical Name
WNK463
Synonyms
WNK463;CS-2515;WNK463 ,S8358;WNK 463;WNK-463;WNK463 monohydrate;WNK463, 10 mM in DMSO;Ser/Thr Protease,WNK 463,inhibit,WNK463,Serine proteases,Inhibitor,Serine endopeptidases,Threonine proteases,WNK-463;N-(tert-Butyl)-1-(1-(5-(5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl)-pyridin-2-yl)piperidin-4-yl)-1H-imidazol-5-carboxamide;1H-Imidazole-5-carboxamide, N-(1,1-dimethylethyl)-1-[1-[5-[5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl]-2-pyridinyl]-4-piperidinyl]-
CBNumber
CB23145823
Molecular Formula
C21H24F3N7O2
Formula Weight
463.46
MOL File
2012607-27-9.mol
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WNK463 Property

Density 
1.43±0.1 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
DMSO : ≥ 30 mg/mL (64.73 mM)
pka
15.18±0.46(Predicted)
form 
Solid
color 
White to off-white
InChIKey
HWSHOMMVLGBIDN-UHFFFAOYSA-N
SMILES
C1N(C2CCN(C3=NC=C(C4=NN=C(C(F)(F)F)O4)C=C3)CC2)C(C(NC(C)(C)C)=O)=CN=1
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML2809
Product name
WNK463
Purity
≥98% (HPLC)
Packaging
5MG
Price
$121
Updated
2025/07/31
Sigma-Aldrich
Product number
SML2809
Product name
WNK463
Purity
≥98% (HPLC)
Packaging
25MG
Price
$466
Updated
2025/07/31
TRC
Product number
W499305
Product name
WNK463
Packaging
5mg
Price
$360
Updated
2021/12/16
AK Scientific
Product number
6099EG
Product name
N-Tert-butyl-3-[1-[5-[5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl]pyridin-2-yl]piperidin-4-yl]imidazole-4-carboxamide
Packaging
10mg
Price
$378
Updated
2021/12/16
ChemScene
Product number
CS-5921
Product name
WNK463
Purity
99.55%
Packaging
25mg
Price
$480
Updated
2021/12/16
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WNK463 Chemical Properties,Usage,Production

Uses

WNK 463, is a pan-WNK kinase inhibitor, acting on WNK1, WNK2, WNK3, and WNK4 kinases. It has shown to affect blood pressure, heart rate, body fluid and electrolyte homeostasis in rodent models of hypertension.

Biochem/physiol Actions

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.).

in vivo

WNK463 (1-10 mg/kg; oral administration; 4 hours; Spontaneously hypertensive Sprague Dawley rats) treatment produces dose-dependent decreases in blood pressure and simultaneous increases in heart rate in conscious SHRs. WNK463 produces significant and dose-dependent increases in urine output as well as urinary sodium and potassium excretion rates.
WNK463 is orally bioavailable in Sprague Dawley rats with a half-life of 2.1 hours[1].

Animal Model:Spontaneously hypertensive Sprague Dawley rats (34-42 weeks of age) [1]
Dosage:1 mg/kg, 3 mg/kg, or 10 mg/kg (Pharmacokinetic study)
Administration:Oral administration; 4 hours
Result:Decreased in blood pressure and simultaneous increases in heart rate. WNK463 produced significant and dose-dependent increased in urine output as well as urinary sodium and potassium excretion rates.

IC 50

WNK2: 1 nM (IC50); WNK3: 6 nM (IC50); WNK4: 9 nM (IC50); WNK1: 5 nM (IC50)

WNK463 Preparation Products And Raw materials

Raw materials

Preparation Products

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WNK463 Suppliers

MQ (shanghai) Pharmaceuticals Co., Ltd.
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13761635123
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1014988033@qq
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1014988033@qq.com
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China
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Shanghai Boyle Chemical Co., Ltd.
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86-21-57758967
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sales@boylechem.com
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Nanjing Chemlin Chemical Co., Ltd
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025-83697070
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+86-25-83453306
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China
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Shanghai Lollane Biological Technology Co.,Ltd.
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021-52996696,15000506266 15000506266
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+86-21-52996696
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Tongling HengYou Biotechnology Co., Ltd.
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021-50426030 13856289449
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BOC Sciences
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16314854226
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United States
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Shanghai YuanYe Biotechnology Co., Ltd.
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021-61312847; 18021002903
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ShangHai Biochempartner Co.,Ltd
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2012607-27-9, WNK463Related Search:


  • WNK463
  • WNK 463;WNK-463
  • CS-2515
  • 1H-Imidazole-5-carboxamide, N-(1,1-dimethylethyl)-1-[1-[5-[5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl]-2-pyridinyl]-4-piperidinyl]-
  • Ser/Thr Protease,WNK 463,inhibit,WNK463,Serine proteases,Inhibitor,Serine endopeptidases,Threonine proteases,WNK-463
  • WNK463, 10 mM in DMSO
  • WNK463 monohydrate
  • WNK463 ,S8358
  • N-(tert-Butyl)-1-(1-(5-(5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl)-pyridin-2-yl)piperidin-4-yl)-1H-imidazol-5-carboxamide
  • 2012607-27-9
  • C21H24F3N7O2