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APY0201 - 98%, high purity , CAS No.1232221-74-7

    Grade & Purity:
  • ≥98%
In stock
Item Number
A646803
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A646803-1mg
1mg
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$62.90
A646803-2mg
2mg
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$66.90
A646803-5mg
5mg
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$132.90
A646803-10mg
10mg
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$228.90
A646803-50mg
50mg
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$708.90
A646803-100mg
100mg
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$1,020.90

Basic Description

Specifications & Purity ≥98%
Biochemical and Physiological Mechanisms APY0201 is a potent PIKfyve inhibitor, which inhibits the conversion of PtdIns3P to PtdIns(3,5)P 2 in the presence of in the presence of [ 33 P]ATP with an IC 50 of 5.2 nM. APY0201 also inhibits IL-12/IL-23 production.
Storage Temp Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Product Description

APY0201 is a potent PIKfyve inhibitor, which inhibits the conversion of PtdIns3P to PtdIns(3,5)P 2 in the presence of in the presence of [ 33 P]ATP with an IC 50 of 5.2 nM. APY0201 also inhibits IL-12/IL-23 production.

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 inhibits IL-12p70 and IL-12p40 production, with IC 50 s of 8.4 and 16 nM, respectively. APY0201 also inhibits IL-12p40 at 99 nM in human PBMC. APY0201 shows significant selectivity for the production of IL-12p70 and IL-12p40 over TNF-α, and this selectivity is maintained across species. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

IC50& Target:PIKfyve 5.2 nM (IC 50 ) IL-12 IL-23

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organoheterocyclic compounds
Class Pyrazolopyrimidines
Subclass Pyrazolo[1,5-a]pyrimidines
Intermediate Tree Nodes Not available
Direct Parent Pyrazolo[1,5-a]pyrimidines
Alternative Parents Dialkylarylamines  Toluenes  Aminopyrimidines and derivatives  Pyridines and derivatives  Morpholines  Imidolactams  Pyrazoles  Heteroaromatic compounds  Oxacyclic compounds  Hydrazones  Dialkyl ethers  Azacyclic compounds  Hydrocarbon derivatives  
Molecular Framework Aromatic heteropolycyclic compounds
Substituents Pyrazolo[1,5-a]pyrimidine - Dialkylarylamine - Aminopyrimidine - Toluene - Monocyclic benzene moiety - Morpholine - Oxazinane - Imidolactam - Benzenoid - Pyrimidine - Pyridine - Azole - Heteroaromatic compound - Pyrazole - Dialkyl ether - Ether - Hydrazone - Oxacycle - Azacycle - Organic nitrogen compound - Amine - Organic oxygen compound - Organonitrogen compound - Organooxygen compound - Hydrocarbon derivative - Aromatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as pyrazolo[1,5-a]pyrimidines. These are aromatic heterocyclic compounds containing a pyrazolo[3,4-d]pyrimidine ring system, which consists of a pyrazole ring fused to and sharing exactly one nitrogen atom with a pyrimidine ring.
External Descriptors Not available

Associated Targets(Human)

PIKFYVE Tchem 1-phosphatidylinositol 3-phosphate 5-kinase (270 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Murine hepatitis virus (113 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

IUPAC Name N-[(E)-(3-methylphenyl)methylideneamino]-7-morpholin-4-yl-2-pyridin-4-ylpyrazolo[1,5-a]pyrimidin-5-amine
INCHI InChI=1S/C23H23N7O/c1-17-3-2-4-18(13-17)16-25-27-21-15-23(29-9-11-31-12-10-29)30-22(26-21)14-20(28-30)19-5-7-24-8-6-19/h2-8,13-16H,9-12H2,1H3,(H,26,27)/b25-16+
InChIKey RFZQYGBLRIKROZ-PCLIKHOPSA-N
Smiles CC1=CC(=CC=C1)C=NNC2=NC3=CC(=NN3C(=C2)N4CCOCC4)C5=CC=NC=C5
Isomeric SMILES CC1=CC(=CC=C1)/C=N/NC2=NC3=CC(=NN3C(=C2)N4CCOCC4)C5=CC=NC=C5
PubChem CID 56927660
MeSH Entry Terms APY0201
Molecular Weight 413.5

Certificates(CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Chemical and Physical Properties

Solubility DMSO : ≥ 35 mg/mL (84.65 mM)
Molecular Weight 413.500 g/mol
XLogP3 3.300
Hydrogen Bond Donor Count 1
Hydrogen Bond Acceptor Count 7
Rotatable Bond Count 5
Exact Mass 413.196 Da
Monoisotopic Mass 413.196 Da
Topological Polar Surface Area 79.900 Ų
Heavy Atom Count 31
Formal Charge 0
Complexity 592.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 0
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 1
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 1
Covalently-Bonded Unit Count 1

Solution Calculators

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