KDU731

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

KDU731 是一种有效的、选择性寄生虫隐孢子虫脂质激酶 PI4K（磷脂酰肌醇-4-OH 激酶）抑制剂，IC50 为 25 nM。

KDU731 is a potent, selective parasite Cryptosporidium lipid kinase PI4K (phosphatidylinositol-4-OH kinase) inhibitor with IC50 of 25 nM, displays >50-fold selectivity window against the human PI4K IIIβ homologue; shows HepG2 CC50 of 15.6 uM and C. parvum CPE EC50 of 0.1 uM; demonstrates a potent reduction in intestinal infection of immunocompromised mice after oral treatment, also leads to rapid resolution of diarrhoea and dehydration in neonatal calves, a clinical model of cryptosporidiosis that closely resembles human infection.

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KDU731 (orally administration; 7 or 10mg/kg; 16 days) has potent activity against Cryptosporidium in immunocompromised IFN-γ KO mice and dramatically reduces oocyst shedding.KDU731 (orally administration; 5 mg/kg; every 12 hours for 7 days) is tolerated in all calves, and treated calves shed significantly fewer oocysts than vehicle treated calves in their stool. Animal Model:6-8 week old C57BL/6 IFN-γ-knockout mice with 10,000 oocysts Dosage:7 or 10 mg/kg Administration:Orally administration; 7 or 10 mg/kg; 16 days Result:Resulted in significant reduction of oocyst shedding.Animal Model:Neonatal calves with 5 x 107 oocysts Dosage:5 mg/kg Administration:Orally administration; 5 mg/kg; every 12 hours for 7 days Result:Resulted in significant reduction of oocyst shedding in treated calves in their stool.

KDU 731

PI3K/Akt/mTOR signaling

PI4K

PI4K

Infection

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1610610-48-4

396.41

C22H16N6O2

>98% (HPLC)

In Vitro:?DMSO : 83.33 mg/mL (210.22 mM)

O=C(C1=CC2=C(C3=CC=C(C(N)=O)C=C3)C=NN2C=C1)N(C4=NC=C(C#N)C=C4)C

3-(4-carbamoylphenyl)-N-(5-cyanopyridin-2-yl)-N-methylpyrazolo[1,5-a]pyridine-5-carboxamide

(-20℃)

With Ice Pack

≥ 2 years