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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1185101-22-7
- 分子式: C22H14D8ClN5O2S
- 分子量:464.01
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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.
化学情報
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CAS 番号 1185101-22-7
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非標識Cas 105219-56-5
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分子量 464.01
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分子式 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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別名
WEB 2086-d8
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)