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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- CAS. Nr.: 1185101-22-7
- Formel: C22H14D8ClN5O2S
- Molecular Weight:464.01
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS. Nr. 1185101-22-7
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Unlabeled Cas 105219-56-5
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Molecular Weight 464.01
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Formel C22H14D8ClN5O2S
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SMILES
O=C(N1C([2H])([2H])C([2H])([2H])OC([2H])([2H])C1([2H])[2H])CCC2=CC3=C(S2)N4C(CN=C3C5=C(C=CC=C5)Cl)=NN=C4C
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Synonyms
WEB 2086-d8
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [Content Brief]
[2]. 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]
[3]. 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]
[4]. 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]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Apafant-d8 Related Classifications
HY-108634S Related Classifications
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