Lexacalcitol, Inhibitor

Lexacalcitol

Cat. Num. AAA5755095

• Purity: 98.00%
• Synonyms: Lexacalcitol; KH1060; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: <1mg/ml refers to the product slightly soluble or insoluble
• Formula: C29H48O4
• SMILES: C[C@]1(CCC/2)[C@](CC[C@@H]1[C@@H](C)OCCCC(CC)(CC)O)([H])C2=C\C=C(C[C@@H](O)C[C@@H]3O)/C3=C
• CAS Number: 131875-08-6
• Target & IC50: Others
• In Vitro: KH1060 was not an effective competitor of C24 oxidation of 1alpha,25-(OH)2D3. KH 1060 inhibited PBMC proliferation and decreased TNF-alpha levels in IBD patients and this effect was synergistic with anti-TNF-alpha. KH1060 metabolism could be blocked by the cytochrome P450 inhibitor, ketoconazole. Certain hydroxylated metabolites of KH1060 retained significant biological activity in vitamin D-dependent reporter gene systems. 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. 0.1nM KH 1060 produced a significant decrease in TNF-alpha levels, determined by ELISA, although less remarkable than in the presence of anti-TNF.
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for Lexacalcitol, inhibitor

Lexacalcitol 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.

References

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.
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.
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 Dermatol. 1997 Aug;137(2):234-40.
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 Dermatol. 1997 Aug;137(2):234-40.
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.
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.
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.
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.