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Lexacalcitol Sale

(Synonyms: 来沙骨化醇; KH1060) 目录号 : GC14928

Lexacalcitol (KH1060) 是一种维生素 D 类似物,是细胞生长和免疫反应的有效调节剂。

Lexacalcitol Chemical Structure

Cas No.:131875-08-6

规格 价格 库存 购买数量
1mg
¥767.00
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5mg
¥3,140.00
现货
10mg
¥4,547.00
现货
50mg
¥14,963.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

Lexacalcitol (KH1060) is over 100 times more active than 1alpha,25-dihydroxyvitamin D3 [1alpha,25-(OH)2D3], as judged by in vitro antiproliferative and cell differentiating assays.IC50 value:Target:KH1060 metabolism could be blocked by the cytochrome P450 inhibitor, ketoconazole. KH1060 was not an effective competitor of C24 oxidation of 1alpha,25-(OH)2D3. Certain hydroxylated metabolites of KH1060 retained significant biological activity in vitamin D-dependent reporter gene systems (chloramphenicol acetyltransferase). KH 1060 inhibited PBMC proliferation and decreased TNF-alpha levels in IBD patients and this effect was synergistic with anti-TNF-alpha. VDR protein levels were significantly increased by PBMC treatment with KH 1060 or anti-TNF-alpha or their combination in ulcerative colitis (UC) patients, and decreased in Crohn's disease (CD) patients, treating the cells with KH 1060. A synergistic inhibition was registered combining KH 1060 and anti-TNF, at well-defined concentrations. 0.1 nM KH 1060 produced a significant decrease in TNF-alpha levels, determined by ELISA, although less remarkable than in the presence of anti-TNF.

References:
[1]. Dilworth FJ, et al.The vitamin D analog, KH1060, is rapidly degraded both in vivo and in vitro via several pathways: principal metabolites generated retain significant biological activity.Endocrinology. 1997 Dec;138(12):5485-96.
[2]. Fullerton A, et al. Characterization of irritant patch test reactions to topical D vitamins and all-trans retinoic acid in comparison with sodium lauryl sulphate. Evaluation by clinical scoring and multiparametric non-invasive measuring techniques.Br J De
[3]. Stio M, et al. Interaction among vitamin D(3) analogue KH 1060, TNF-alpha, and vitamin D receptor protein in peripheral blood mononuclear cells of inflammatory bowel disease patients.Int Immunopharmacol. 2006 Jul;6(7):1083-92. Epub 2006 Feb 23.
[4]. Shimizu T, et al. Synergistic induction of gene expression during the differentiation into mature macrophage in human myeloblastic leukemia cells treated with TPA and KH1060.Leuk Res. 2009 Jun;33(6):803-9. Epub 2009 Jan 13.

Chemical Properties

Cas No. 131875-08-6 SDF
别名 来沙骨化醇; KH1060
化学名 (1R,3S,5Z)-5-[(2E)-2-[(1S,3aS,7aS)-1-[(1R)-1-(4-ethyl-4-hydroxyhexoxy)ethyl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol
Canonical SMILES CCC(CC)(CCCOC(C)C1CCC2C1(CCCC2=CC=C3CC(CC(C3=C)O)O)C)O
分子式 C29H48O4 分子量 460.69
溶解度 DMSO 储存条件 -20°C, protect from light, stored under nitrogen,unstable in solution, ready to use.
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mg 5 mg 10 mg
1 mM 2.1707 mL 10.8533 mL 21.7066 mL
5 mM 0.4341 mL 2.1707 mL 4.3413 mL
10 mM 0.2171 mL 1.0853 mL 2.1707 mL
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