WNK463

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

第一种有效的、选择性的、口服生物可利用的泛无赖氨酸 (WNK) 激酶催化活性抑制剂，对 WNK1/2/3/4 的 IC50 为 5/1/6/9 nM。

The first, potent, selective, and orally bioavailable pan With-No-Lysine (WNK) Kinase catalytic activity inhibitor with IC50 of 5/1/6/9 nM for WNK1/2/3/4, respectively; shows >50% inhibition against only 2 out of 442 human kinases at 10 uM; affects blood pressure and body fluid and electro-lyte homeostasis in rodent models of hypertension.

Western Blot Analysis Cell Line:Human tissue-engineered corneas (hTECs)Concentration:50 nM, 1 μΜ, 10 μΜ Incubation Time:6 days Result:Reduced phosphorylation of the WNK1 downstream targets SPAK/OSR1 in wounded hTECs.

Animal Model:Spontaneously hypertensive Sprague Dawley rats (34-42 weeks of age) 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.

WNK-463 | WNK 463

Autophagy

WNK Kinase

WNK

Cancer

——

2012607-27-9

463.4562

C21H24F3N7O2

>98% (HPLC)

DMSO: ≥ 30 mg/mL

O=C(C1=CN=CN1C2CCN(C3=NC=C(C4=NN=C(C(F)(F)F)O4)C=C3)CC2)NC(C)(C)C

1H-Imidazole-5-carboxamide, N-(1,1-dimethylethyl)-1-[1-[5-[5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl]-2-pyridinyl]-4-piperidinyl]-

(-20℃)

With Ice Pack

≥ 2 years