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医薬品及び創薬化学品の専門商社

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化合物検索・調査依頼・データベース提供生理・薬理活性化合物/ポジコン

Calcitriol【別名:1,25-Dihydroxyvitamin D3】

HY-10002構造式

CAS No.
32222-06-3
製品コード
HY-10002
サプライヤー
Medchemexpress
純度
>98%
Target
VD/VDR
参考納期(在庫有りの場合)
約5-10営業日

詳細情報

FormulaC27H44O3
M.W.416.6365
PathwayVitamin D Related
Solubility10 mM in DMSO
備考Calcitriol is the most active metabolite of vitamin D. Many of the effects of Calcitriol are mediated by its interaction with the vitamin D receptor (VDR).
IC50 & Target: Vitamin D receptor (VDR)[1]
In Vitro: In parathyroid cells, Calcitriol acts through the vitamin D receptor (VDR) to inhibit PTH mRNA expression. In normal dog parathyroid glands, culture with Calcitriol (10-10 to 10-7 M) for 24 h produces a dose-dependent inhibitory effect on the progression of cells into the cell cycle and into apoptosis. Even a low Calcitriol concentration (10-11 and 10-10 M) reduces the progression to the S phase and to apoptosis. As the Calcitriol concentration is increased from 10-9 to 10-8M, a further suppression of cells entering the cell cycle and apoptosis is observed. Moreover, a significant correlation (r=0.95, P<0.01) is observed at the different Calcitriol concentrations between the number of cells in S phase and those undergoing apoptosis[1]. Calcitriol binds to the vitamin D receptor (VDR), a member of the steroid receptor superfamily to regulate gene expression in all tissues of the body. In addition to its actions on calcium and bone homeostasis, Calcitriol also exhibits anti-proliferative and pro-differentiation activities indicating its potential use in the prevention and treatment of multiple cancers, including breast cancer (BCa). Calcitriol inhibits the growth of both estrogen receptor-positive (ER+) and ER-negative human BCa cell lines by regulating many molecular pathways. Calcitriol reduces the invasive and metastatic potential of several BCa cells. Calcitriol evokes significant anti-inflammatory actions in several cancer cells including BCa cells. Calcitriol also mediates actions that would be especially effective in ER+ BCa[2].
In Vivo: Combinations of Calcitriol with aromatase inhibitors or the analog EB1089 with all-trans-retinoic acid exhibit enhanced inhibition of the growth of MCF-7 xenografts. Calcitriol also exhibits potent anti-angiogenic activity that could contribute to its actions to inhibit invasion and metastasis[2]. Body-weight of HFD-fed animals become different as it gradually but noticeably decreased in Calcitriol group (150 IU/kg/day, p.o.) compared with controls after 12 weeks of treatment (11.4% versus 30.2%, p<0.05). At the end of the study, the animals that receive HFD with Calcitriol has the smallest percentage weight gain as opposed to control mice (6.8% versus 28.7%, p<0.01)[3].
URLhttp://www.medchemexpress.com/Calcitriol.html

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