ChemicalBook > Product Catalog > Biochemical Engineering > Biochemical Reagents > Agonist Inhibitors > (E)-4-(5-(2-(3-methylbenzylidene)hydrazinyl)-2-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-7-yl)morpholine
(E)-4-(5-(2-(3-methylbenzylidene)hydrazinyl)-2-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-7-yl)morpholine
(E)-4-(5-(2-(3-methylbenzylidene)hydrazinyl)-2-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-7-yl)morpholine Basic information
- Product Name:
- (E)-4-(5-(2-(3-methylbenzylidene)hydrazinyl)-2-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-7-yl)morpholine
- Synonyms:
-
- (E)-4-(5-(2-(3-methylbenzylidene)hydrazinyl)-2-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-7-yl)morpholine
- APY0201
- N-(3-Methylbenzylidene)-N'-[7-(morpholin-4-yl)-2-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-5-yl]hydrazine
- N-(3-methylbenzylidene)-N'-(7-morpholin-2-pyridin-4-yl-pyrazolo[1,5-a]pyrimidin-5-yl)hydrazine
- APY 0201 ;APY-0201 ;APY0201
- APY0201, >98%
- 4-{5-[(E)-2-[(3-methylphenyl)methylidene]hydrazin-1-yl]-2-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-7-yl}morpholine
- Benzaldehyde, 3-methyl-, 2-[7-(4-morpholinyl)-2-(4-pyridinyl)pyrazolo[1,5-a]pyrimidin-5-yl]hydrazone
- CAS:
- 1232221-74-7
- MF:
- C23H23N7O
- MW:
- 413.48
- Product Categories:
-
- Inhibitors
- Mol File:
- 1232221-74-7.mol
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(E)-4-(5-(2-(3-methylbenzylidene)hydrazinyl)-2-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-7-yl)morpholine Chemical Properties
- Density
- 1.33±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:20.0(Max Conc. mg/mL);48.37(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:2):0.33(Max Conc. mg/mL);0.8(Max Conc. mM)
DMF:3.0(Max Conc. mg/mL);7.26(Max Conc. mM) - form
- A crystalline solid
- pka
- 17.36±0.70(Predicted)
- color
- Light yellow to yellow
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(E)-4-(5-(2-(3-methylbenzylidene)hydrazinyl)-2-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-7-yl)morpholine Usage And Synthesis
Uses
APY0201 is a potent PIKfyve inhibitor, which inhibits the conversion of PtdIns3P to PtdIns(3,5)P2 in the presence of in the presence of [33P]ATP with an IC50 of 5.2 nM. APY0201 also inhibits IL-12/IL-23 production.
in vivo
Oral APY0201 at a 30 mg/kg dose shows significant reduction of IL-12p70 production (78% inhibition relative to that of the vehicle control), which implys that the inhibitory potential of APY0201 against IL-12 is confirmed in the animal experiment[1].
IC 50
PIKfyve: 5.2 nM (IC50); IL-12; IL-23
References
[1] Hayakawa N, et al. Structure-activity relationship study, target identification, and pharmacological characterization of a small molecular IL-12/23 inhibitor, APY0201. Bioorg Med Chem. 2014 Jun 1;22(11):3021-9. DOI:10.1016/j.bmc.2014.03.036
(E)-4-(5-(2-(3-methylbenzylidene)hydrazinyl)-2-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-7-yl)morpholineSupplier
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