APY0201(APY-0201)|PIKfyve inhibitor|

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Datasheet of APY0201

Description:. APY0201 is a potent, highly selective, ATP-competitive PIKfyve inhibitor (IC50=5.2 nM) that interrupts the conversion of phosphatidylinositol 3-phosphate (PtdIns3P) to PtdIns(3,5)P2; a unique small molecular IL-12/23 production inhibitor. in vitro: APY0201 works differently from anti-IL-12/23 antibodies and acts by inhibiting production of these proinflammatory cytokines with characteristic selectivity over other cytokines, including tumor necrosis factor-alpha (TNF-α). In stimulated thioglycollate-induced mouse peritoneal exudate cells (TG-PEC), APY0201 strongly inhibited IL-12p70 and IL-12p40 production, with IC50 values of 8.4 and 16 nM, respectively. APY0201 also inhibited IL-12p40 at 99 nM in human PBMC. APY0201 showed significant selectivity for the production of IL-12p70 and IL-12p40 over TNF-α, and this selectivity was maintained across species. in vivo: Oral APY0201 at a 30 mg/kg dose showed significant reduction of IL-12p70 production (78% inhibition relative to that of the vehicle control), which implied that the inhibitory potential of APY0201 against IL-12 was confirmed in the animal experiment.

Chemical Information Catalog

DC7922

Purity of current batch:

>98%

Molecular Weight (MW)

413.2

Molecular Formula

C23H23N7O

CAS No.

1232221-74-7

Solubility (25°C)

DMSO

Storage

Store at -20°C (desiccating conditions).

Handling: Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months. Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.


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