产品说明书

Calcipotriol monohydrate

Print
Chemical Structure| 147657-22-5 同义名 : Calcipotriol (hydrate);Calcipotriene
CAS号 : 147657-22-5
货号 : A648541
分子式 : C27H42O4
纯度 : 97%
分子量 : 430.62
MDL号 : N/A
存储条件:

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(243.83 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

无水乙醇: 100 mg/mL(232.22 mM),配合低频超声助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇

动物实验配方:
生物活性
描述 AZD0156, a potent and selective ATM inhibitor, exhibits oral activity with an IC50 of 0.58 nM. It blocks ATM-dependent signaling pathways, inhibits DNA damage checkpoint activation, impairs DNA damage repair, and triggers apoptosis in tumor cells. Furthermore, AZD0156 suppresses ATM kinase activity, leading to the prevention of DNA damage checkpoint activation, disruption of DNA repair mechanisms, induction of apoptosis, and ultimately causing death in tumor cells with high ATM expression. Calcipotriol monohydrate, a synthetic analogue of Vitamin D3, binds strongly to the vitamin D receptor. In NHEK cells, without IL-17A or IL-22 stimulation, Calcipotriol marginally increases IL-8 mRNA levels at 0.2 nM or has no effect from 2 to 20 nM. However, IL-17A and IL-22 significantly boost IL-8 mRNA expression, aligning with previous findings. Calcipotriol at 2, 20, and 40 nM dose-dependently diminishes this upregulation[1]. Drug treatments alter NK cell expression of cytotoxicity receptors or KIR. Human NK cells pretreated with 1,25(OH)2D3, Calcipotriol, or FTY720 at 100, 10, or 1 ng/mL for 4 hours show a notable increase in NKp30 surface expression[2].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02518048 Skin and Connective Tissue Dis... 展开 >>eases 收起 << Phase 2 Completed - France ... 展开 >> Centre de Pharmacologie Clinique Appliquée à la Dermatologie (CPCAD) Nice, France, 06000 收起 <<
NCT02416258 Skin and Connective Tissue Dis... 展开 >>eases 收起 << Phase 2 Completed - France ... 展开 >> Centre de Pharmacologie Clinique Appliquée à la Dermatologie (CPCAD) Nice, France, 06000 收起 <<
NCT02518048 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.32mL

0.46mL

0.23mL

11.61mL

2.32mL

1.16mL

23.22mL

4.64mL

2.32mL

参考文献

[1]Al-Jaderi Z, et al. Effects of vitamin D3, calcipotriol and FTY720 on the expression of surface molecules and cytolytic activities of human natural killer cells and dendritic cells. Toxins (Basel). 2013 Oct 28;5(11):1932-47.

[2]Sakabe JI, et al. Calcipotriol Increases hCAP18 mRNA Expression but Inhibits Extracellular LL37 Peptide Production in IL-17/IL-22-stimulated Normal Human Epidermal Keratinocytes. Acta Derm Venereol. 2014 Sep;94(5):512-6.

[3]Pommergaard HC, et al. Combination chemoprevention with diclofenac, calcipotriol and difluoromethylornithine inhibits development of non-melanoma skin cancer in mice. Anticancer Res. 2013 Aug;33(8):3033-9.