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Merck

SML2974

Apilimod

≥98% (HPLC), IL-12 and IL-23 inhibitor, powder

Synonym(s):

3-Methyl-benzaldehyde 2-[6-(4-morpholinyl)-2-[2-(2-pyridinyl)ethoxy]-4-pyrimidinyl]hydrazone, STA 5326, STA-5326

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About This Item

Empirical Formula (Hill Notation):
C23H26N6O2
CAS Number:
Molecular Weight:
418.49
UNSPSC Code:
51111800
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
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Product Name

Apilimod, ≥98% (HPLC)

Quality Segment

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

−20°C

SMILES string

N4(CCOCC4)c1nc(nc(c1)N\N=C\c3cc(ccc3)C)OCCc2ncccc2

InChI

1S/C23H26N6O2/c1-18-5-4-6-19(15-18)17-25-28-21-16-22(29-10-13-30-14-11-29)27-23(26-21)31-12-8-20-7-2-3-9-24-20/h2-7,9,15-17H,8,10-14H2,1H3,(H,26,27,28)/b25-17+

InChI key

HSKAZIJJKRAJAV-KOEQRZSOSA-N

Biochem/physiol Actions

Apilimod (STA-5326) is a potent, orally active and selective inhibitor of the cytokines IL-12 and IL-23. Apilimod selectively suppresses synthesis of IL-12 and IL-23 by inhibition of phosphotransferase activity of TLR-4 regulator lipid kinase PIKfyve (phosphatidylinositol-3-phosphate 5-kinase). It suppresses Th1 cells response in vivo and reduces inflammatory histopathologic changes. Also, it exhibits strong anti COVID-19 activity in two cell lines (Vero E6:IC50 < 0.08 μM; A549-ACE2:IC50 = 0.007 μM). Apilimod potently reduces entry of SARS-CoV S pseudovirions on 293/hACE2 cells.
potent, orally active and selective IL-12 and IL-23 inhibitor; PIKfyve inhibitor; Exhibit strong anti COVID-19 activity in cell lines


Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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