- WNK463
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- $72.00 / 1mg
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2025-04-29
- CAS:2012607-27-9
- Min. Order:
- Purity: ≥95%
- Supply Ability: 10g
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| Product Name: | WNK463 | | Synonyms: | 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 | | CAS: | 2012607-27-9 | | MF: | C21H24F3N7O2 | | MW: | 463.46 | | EINECS: | | | Product Categories: | | | Mol File: | 2012607-27-9.mol |  |
| | WNK463 Chemical Properties |
| 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 |
| | WNK463 Usage And Synthesis |
| 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.
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| | IC 50 | WNK2: 1 nM (IC50); WNK3: 6 nM (IC50); WNK4: 9 nM (IC50); WNK1: 5 nM (IC50) |
| | WNK463 Preparation Products And Raw materials |
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