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APILIMOD

APILIMOD Structure
APILIMOD
  • CAS No.541550-19-0
  • Chemical Name:APILIMOD
  • CBNumber:CB61091430
  • Molecular Formula:C23H26N6O2
  • Formula Weight:418.49
  • MOL File:541550-19-0.mol
APILIMOD Property
  • Boiling point 655.1±65.0 °C(Predicted)
  • Density 1.24
  • storage temp. -20°C
  • solubility Soluble in DMSO (>25 mg/ml)
  • form solid
  • pka 12.56±0.10(Predicted)
  • color White
  • Stability Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
  • FDA UNII GFW2K84S4L
  • UNSPSC Code 51111800
  • NACRES NA.77
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordWarning
  • Hazard statements H302
  • Precautionary statements P264-P270-P301+P312-P330-P501

APILIMOD Chemical Properties,Usage,Production

  • Description Apilimod (541550-19-0) is a potent (IC50 = 10 nM IFN-g/LPS-stimulated human PMBC’s; IC50 = 1 nM in IFN-g/SAC-stimulated human PMBC’s) IL-12/IL-23 inhibitor downregulating both at the transcriptional level.? Suppresses Th1 but not Th2 immune response.1? Inhibition was also observed in human monocytes, monocyte-derived dendritic cells, and THP-1 cells.? Apilimod’s mechanism of action is mediation of TLR signaling via inhibition of phosphatidylinositol-3-phosphate 5-kinase (PIKfyve; IC50 = 14 nM).2? It displayed selective cytotoxic activity in B-cell non-Hodgkin lymphoma compared with normal cells.3? Apilimod prevented infection of VSV-ZEBOV and VSV-SARS-CoV-2 (IC50 = 50 nM) as well as SARS-CoV-2 strain 2019-nCoVB/USA-1WA/2020.4
  • Chemical Properties Off-White Solid
  • Uses Apilimod is a small-molecule that selectively suppresses synthesis of IL-12 and IL-23. Apilimod reduces dendritic cell infiltration in psoriasis.
  • 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].

  • IC 50 IL-4; IL-5; IL-8; IL-12; IL-23
  • References Wada et al. (2007), Selective abrogation of Th1 response by STA-5326, a potent IL-12/IL23 inhibitor; Blood 109 1156 Cai et al. (2013), PIKfyve, a class III PI-kinase, is the target of the small molecule IL12/23 inhibitor apilimod and a new player in toll-like receptor signaling; Chem. Biol., 20 912 Gayle et al. (2016), Identification of apilimod as a first-in-class PIKfyve kinase inhibitor for treatment of B-cell non-Hodgkin lymphoma; Blood, 129 1768 Kang et al. (2020), Inhibition of PIKfyve kinase prevents infection by Zaire ebola virus and SARS-CoV-2; Proc. Natl. Acad. Sci. USA 117 20803
APILIMOD Preparation Products And Raw materials
Raw materials
Preparation Products
APILIMOD Suppliers
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APILIMOD Spectrum
541550-19-0, APILIMODRelated Search:
  • Pharmaceuticals
  • Intermediates & Fine Chemicals
  • Heterocycles
  • Aromatics
  • Amines
  • API
  • Inhibitors
  • 药靶配体
  • 抑制剂
  • 小分子抑制剂，天然产物
  • 小分子抑制剂
  • APILIMOD 阿匹莫德 |CAS 541550-19-0
  • 阿匹莫德,10 MM DMSO 溶液
  • 盐酸阿吡莫德
  • 4-(6-(2-(3-甲基亚苄基)肼基)-2-(2-(吡啶-2-基)乙氧基)嘧啶-4-基)吗啉
  • 阿匹莫德
  • 阿吡莫德, >98%
  • 阿吡莫德
  • 541550-19-0
  • Apilimod, 10 mM in DMSO
  • Apimod
  • Apilimod Hydrochloride
  • 1H-Benzimidazole-1-carboxylicacid,2,3-dihydro-6-oxo-,ethylester
  • STA 5326; STA5326; STA-5326
  • Apilimod, >98%
  • 4-(6-(2-(3-Methylbenzylidene)hydrazinyl)-2-(2-(pyridin-2-yl)ethoxy)pyrimidin-4-yl)morpholine
  • Benzaldehyde,3-methyl-,2-[6-(4-morpholinyl)-2-[2-(2-pyridiny...
  • APILIMOD
  • N-[(e)-(3-methylphenyl)methylideneamino]-6-morpholin-4-yl-2-(2-pyridin-2-ylethoxy)pyrimidin-4-amine
  • 4-{6-[(E)-2-[(3-methylphenyl)methylidene]hydrazin-1-yl]-2-[2-(pyridin-2-yl)ethoxy]pyrimidin-4-yl}morpholine
  • 4-{6-[(2E)-2-(3-Methylbenzylidene)hydrazino]-2-[2-(2-pyridinyl)ethoxy]-4-pyrimidinyl}morpholine
  • Benzaldehyde,3-methyl-,2-[6-(4-morpholinyl)-2-[2-(2-pyridinyl)ethoxy]-4-pyrimidinyl]hydrazone
  • 3-Methylbenzaldehyde [6-(4-morpholinyl)-2-[2-(2-pyridinyl)ethoxy]-4-pyrimidinyl]hydrazone
  • 3-Methylbenzaldehyde 2-[6-(4-Morpholinyl)-2-[2-(2-pyridinyl)ethoxy]-4- pyriMidinyl]hydrazone
  • ApiliMod(STA5326)
  • Sta-5326
  • Sta5326
  • Sta 5326
  • (E)-4-(6-(2-(3-methylbenzylidene)hydrazinyl)-2-(2-(pyridin-2-yl)ethoxy)pyrimidin-4-yl)morpholine
  • APILIMODUM

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