WNK463
- CAS No.
- 2012607-27-9
- Chemical Name:
- WNK463
- Synonyms
- WNK463;CS-2515;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;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
- Molecular Weight:
- 463.46
- MDL Number:
- MFCD30489744
- MOL File:
- 2012607-27-9.mol
WNK463 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | SML2809 | WNK463 ≥98% (HPLC) | 2012607-27-9 | 5MG | $118 | 2024-03-01 | Buy |
| Sigma-Aldrich | SML2809 | WNK463 ≥98% (HPLC) | 2012607-27-9 | 25MG | $453 | 2024-03-01 | Buy |
| TRC | W499305 | WNK463 | 2012607-27-9 | 5mg | $360 | 2021-12-16 | Buy |
| AK Scientific | 6099EG | N-Tert-butyl-3-[1-[5-[5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl]pyridin-2-yl]piperidin-4-yl]imidazole-4-carboxamide | 2012607-27-9 | 10mg | $378 | 2021-12-16 | Buy |
| ChemScene | CS-5921 | WNK463 99.55% | 2012607-27-9 | 25mg | $480 | 2021-12-16 | Buy |
WNK463 Chemical Properties,Uses,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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32268 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| TargetMol Chemicals Inc. | support@targetmol.com | United States | 38663 | 58 | |
| ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11681 | 58 |
| LEAPCHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 43340 | 58 |
| Shanghai Acmec Biochemical Technology Co., Ltd. | +86-18621343501; +undefined18621343501 | product@acmec-e.com | China | 33338 | 58 |
| Aladdin Scientific | tp@aladdinsci.com | United States | 57505 | 58 | |
| Wuhan Jingkang en Biomedical Technology Co., Ltd | +8613720134139 | orders@jknbiochem.com | China | 5221 | 58 |
| SHANGHAI KEAN TECHNOLOGY CO., LTD. | +8613817748580 | cooperation@kean-chem.com | China | 40066 | 58 |
