別品名 |
FK-506, Fujimycin, Prograf, Protopic, CCRIS 7124., 3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R, 26aS)5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-3-(2-(4-hydroxy-3-methoxycyclohexyl)-14,16-dimethoxy-4,10,12,18-tetramethyl-8-(2-propenyl)-5,19-Epoxy-3H-pyrido(2,1-c)(1,4)oxaazacyclotricosine-1,7,20,21(4H,23H)-tetrone
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別包装 |
あり
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純度 |
>=98%
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分子量 |
804.02
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CAS RN® |
104987-11-3
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化合物の概要 |
Calcineurin inhibitor.
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構造 |
C44H69NO12
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溶媒 |
Soluble in DMSO (20 mg/ml), ethanol (30 mg/ml), acetone, ethyl acetate, diethyl ether or chloroform.
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使用目的 |
Tacrolimus is a calcineurin inhibitor that exhibits immunosuppressive, anti-fibrotic, anti-inflammatory, and anti-allergic activities. Clinically, tacrolimus is used to treat atopic dermatitis and conjunctivitis. In vivo, tacrolimus inhibits synthesis of type I collagen polypeptides and the interaction between LARP6 and FKBP3, suppressing the development of alcohol-induced liver fibrosis. In animal models of OVA-induced allergy, tacrolimus decreases allergic symptoms and levels of IgE, eosinophils, IL-5, and GATA-3.
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その他 |
[融点]126-130℃
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参考文献 |
Carr WW. Topical calcineurin inhibitors for atopic dermatitis: review and treatment recommendations. Paediatr Drugs. 2013 Aug;15(4):303-10. PMID: 23549982.Manojlovic Z, Blackmon J, Stefanovic B. Tacrolimus (FK506) prevents early stages of ethanol induced hepatic fibrosis by targeting LARP6 dependent mechanism of collagen synthesis. PLoS One. 2013 Jun 3;8(6):e65897. PMID: 23755290.Grigoriu S, Bond R, Cossio P, et al. The molecular mechanism of substrate engagement and immunosuppressant inhibition of calcineurin. PLoS Biol. 2013;11(2):e1001492. PMID: 23468591.Shin JH, Park HR, Kim SW, et al. The effect of topical FK506 (tacrolimus) in a mouse model of allergic rhinitis. Am J Rhinol Allergy. 2012 Mar-Apr;26(2):e71-5. PMID: 22487280.Izumi S, Nozaki Y, Komori T, et al. Substrate-dependent inhibition of organic anion transporting polypeptide 1B1: comparative analysis with prototypical probe substrates estradiol-17beta-glucuronide, estrone-3-sulfate, and sulfobromophthalein. Drug Metab Dispos. 2013 Oct;41(10):1859-1866. PMID: 23920221.
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メーカー |
品番 |
包装 |
LKT
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T0008
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100 MG
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※表示価格について
当社在庫 |
なし
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納期目安 |
1週間程度
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保存温度 |
常温
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