105219-56-5
Chemical Structure
Apafant
Synonym(s): WEB 2086
- CAS No.: 105219-56-5
- Formula:C22H22ClN5O2S
- Molecular Weight:455.96
IUPAC Name: 3-(4-(2-chlorophenyl)-9-methyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-2-yl)-1-morpholinopropan-1-one
InChIKey: JGPJQFOROWSRRS-UHFFFAOYSA-N
SMILES: O=C(N1CCOCC1)CCC(S2)=CC3=C2N4C(CN=C3C5=CC=CC=C5Cl)=NN=C4C
Biological Activity: Apafant (WEB 2086), a chemical probe, is a potent platelet-activating factor (PAF) antagonist, inhibits PAF binding to human PAF receptors with a Ki of 9.9 nM. Apafant increases the gene expression of PAF-r, α-globin, β-globin, decreases the c-myb gene expression. Apafant shows a protective effect on alkyl-PAF-mediated lethalit[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Apafant | 99.93% | Apafant (WEB 2086), a chemical probe, is a potent platelet-activating factor (PAF) antagonist, inhibits PAF binding to human PAF receptors with a Ki of 9.9 nM. Apafant increases the gene expression of PAF-r, α-globin, β-globin, decreases the c-myb gene expression. Apafant shows a protective effect on alkyl-PAF-mediated lethalit. | ||||||||||||||||||||
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Apafant (Standard) | ≥98% | Apafant (Standard) is the analytical standard of Apafant (HY-108634). This product is intended for research and analytical applications. Apafant (WEB 2086), a chemical probe, is a potent platelet-activating factor (PAF) antagonist, inhibits PAF binding to human PAF receptors with a Ki of 9.9 nM. Apafant increases the gene expression of PAF-r, α-globin, β-globin, decreases the c-myb gene expression. Apafant shows a protective effect on alkyl-PAF-mediated lethalit. | ||||||||||||||||||||
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Apafant-d8 | Apafant-d8 is the deuterium labeled Apafant. Apafant (WEB 2086) is a potent platelet-activating factor (PAF) antagonist, inhibits PAF binding to human PAF receptors with a Kiof 9.9 nM. Apafant increases the gene expression of PAF-r, α-globin, β-globin, decreases the c-myb gene expression. Apafant shows a protective effect on alkyl-PAF-mediated lethalit. | |||||||||||||||||||||
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- [1]. Kato M, et al. Apafant, a potent platelet-activating factor antagonist, blocks eosinophil activation and is effective in the chronic phase of experimental allergic conjunctivitis in guinea pigs. J Pharmacol Sci. 2004 Aug;95(4):435-42. [Content Brief]
- [2]. Cellai C, Laurenzana A, Vannucchi AM, Della Malva N, Bianchi L, Paoletti F. Specific PAF antagonist WEB-2086 induces terminal differentiation of murine and human leukemia cells. FASEB J. 2002 May;16(7):733-5. [Content Brief]
- [3]. Chaithra VH, et al. Modulation of inflammatory platelet-activating factor (PAF) receptor by the acyl analogue of PAF. J Lipid Res. 2018 Nov;59(11):2063-2074. [Content Brief]
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