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| SKU | Size | Availability |
Price | Qty |
|---|---|---|---|---|
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A646803-1mg
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1mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
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$62.90
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A646803-2mg
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2mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
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$66.90
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A646803-5mg
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5mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
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$132.90
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A646803-10mg
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10mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
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$228.90
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A646803-50mg
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50mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
|
$708.90
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A646803-100mg
|
100mg |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
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$1,020.90
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| 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 |
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 |
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| Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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| 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 |
| 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 |