Introduction：Basic information about CAS 541550-19-0|apilimod, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | apilimod |
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| CAS Number | 541550-19-0 | Molecular Weight | 418.491 |
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| Density | 1.2±0.1 g/cm3 | Boiling Point | 655.1±65.0 °C at 760 mmHg |
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| Molecular Formula | C23H26N6O2 | Melting Point | / |
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| MSDS | / | Flash Point | 350.0±34.3 °C |
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Names
| Name | N-[(E)-(3-methylphenyl)methylideneamino]-6-morpholin-4-yl-2-(2-pyridin-2-ylethoxy)pyrimidin-4-amine |
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| Synonym | More Synonyms |
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apilimod BiologicalActivity
| Description | Apilimod is a potent IL-12/IL-23 inhibitor, and strongly inhibits IL-12 with IC50s of 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs and SAC-treated monkey PBMCs, respectively. |
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| Related Catalog | Signaling Pathways >>Immunology/Inflammation >>Interleukin RelatedResearch Areas >>Inflammation/Immunology |
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| Target | IC50: 1 nM (IL-12, human PBMCs), 2 nM (IL-12, monkey PBMCs) |
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| In Vitro | Apilimod inhibited IFN-γ production induced by either IFN-γ/SAC or SAC in human PBMCs, with an IC50 of approximately 20 nM. Apilimod show some inhibition against IFN-γ/SAC-induced TNF-α and ConA-induced IL-5 from human PBMCs at high concentrations, but no suppressive effect against IL-1β, IL-2, IL-4, IL-8, and IL-18 in all cultures tested. The p35 and p40 promoter-driven luciferase activities are significantly induced after stimulation with IFN-γ/LPS or IFN-γ/SAC, and are completely suppressed by 100 nM Apilimod[1]. |
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| In Vivo | Apilimod (10 mg/kg, p.o.) is effective not only when administered throughout the entire experiment, but also when administration is initiated on day 30 when disease is clearly measurable but not maximal. TA-5326 causes a significant reduction in cell number only in the Th1 model, with an average percentage of inhibition of 51%±8% relative to the vehicle control. Apilimod treatment has no effect in the Th2 setting[1]. Apilimod (5 or 20 mg/kg, p.o.) reduces the level of IL-12 p40 in serum without altering body weight in EAU mice. Oral administration of Apilimod reduces the severity of experimental autoimmune uveoretinitis (EAU) by clinical and histopathological analysis[2]. |
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| Cell Assay | Cervical lymph node cells obtained from immunized mice on day 18 (2×105 cells/well) arecultured in 0.2 mL RPMI 1640 containing 10 mM HEPES, 0.1 mM nonessential amino acid, 1 mM sodium pyruvate, 100 U/mL penicillin, 100 μg/mL streptomycin, 1×10-5 M 2-mercaptoethanol, 10% FCS, and 10 μg/mL IRBP1-20. For cytokine assay, supernatants are collected after 72 hours and analysed for IFN-γ, IL-4 and IL-17 by quantitative capture ELISA using quantikine ELISA kits and mouse IL-17 ELISA Ready-SET-Go kits. Cell proliferation is evaluated using a cell proliferation assay. |
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| Animal Admin | In most experiments, 5 mg/kg or 20 mg/kg Apilimod or vehicle only (0.5% carboxyl methyl cellulose) is orally administered once a day for six days a week from day 0 to day 14 after immunization. In the effector phase experiments, 20 mg/kg Apilimod or vehicle is orally administered once a day, from day 9 to day 14 after immunization. |
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| References | [1]. Wada Y, et al. Selective abrogation of Th1 response by STA-5326, a potent IL-12/IL-23 inhibitor. Blood. 2007 Feb 1;109(3):1156-64. [2]. Keino H, et al. Therapeutic effect of the potent IL-12/IL-23 inhibitor STA-5326 on experimental autoimmune uveoretinitis. Arthritis Res Ther. 2008;10(5):R122. |
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Chemical & Physical Properties
| Density | 1.2±0.1 g/cm3 |
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| Boiling Point | 655.1±65.0 °C at 760 mmHg |
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| Molecular Formula | C23H26N6O2 |
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| Molecular Weight | 418.491 |
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| Flash Point | 350.0±34.3 °C |
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| Exact Mass | 418.211731 |
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| PSA | 84.76000 |
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| LogP | 4.04 |
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| Appearance of Characters | white solid |
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| Vapour Pressure | 0.0±2.0 mmHg at 25°C |
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| Index of Refraction | 1.637 |
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| InChIKey | HSKAZIJJKRAJAV-UQQQWYQISA-N |
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| SMILES | Cc1cccc(C=NNc2cc(N3CCOCC3)nc(OCCc3ccccn3)n2)c1 |
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| Storage condition | -20℃ |
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Synonyms
| UNII-GFW2K84S4L |
| apilimodum |
| 4-{6-[(2E)-2-(3-Methylbenzylidene)hydrazino]-2-[2-(2-pyridinyl)ethoxy]-4-pyrimidinyl}morpholine |
| STA-5326 |
| apilimod |
