中文名称: 卡泊三醇一水合物
英文名称: Calcipotriol monohydrate
CAS No: 147657-22-5
分子式: C27H42O4
分子量: 430.62
C10665 卡泊三醇一水合物 ≥98% (psaitong)
包装规格:
10mg 50mg 100mg in glass bottle
溶解性:
溶于DMSO(100 mg/mL 超声)
产品描述:

基本信息

产品编号:

C10665 

产品名称:

Calcipotriol monohydrate

CAS:

147657-22-5

 

储存条件

粉末

2-8℃

四年

 

 

分子式:

C27H42O4

溶于液体

 

 

分子量

430.62

 

 

化学名: 

1,3-Cyclohexanediol,5-[(2E)-2-[(1R,3aS,7aR)-1-[(1R,2E,4S)-4-cyclopropyl-4-hydroxy-1-methyl-2-buten-1-yl]octahydro-7a-methyl-4H-inden-4-ylidene]ethylidene]-4-methylene-,hydrate (1:1), (1R,3S,5Z)-

Solubility (25°C):

 

体外:

 

DMSO

100 mg/mL (232.22mM; Need ultrasonic)

Water

 

Ethanol

100 mg/mL (232.22mM; Need ultrasonic)

体内(现配现用):

1.请依序添加每种溶剂: 10% EtOH40% PEG3005% Tween-8045% saline

Solubility: 5 mg/mL (11.61mM); Suspended solution; Need ultrasonic

此方案可获得 5 mg/mL (11.61mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

1mL 工作液为例,取 100μL 50.0 mg/mL 的澄清 EtOH 储备液加到 400μL PEG300 中,混合均匀;向上述体系中加入50μL Tween-80,混合均匀;然后继续加入 450μL生理盐水定容至 1mL。

2.请依序添加每种溶剂: 10% EtOH90% (20% SBE-β-CD in saline)

Solubility: ≥ 5 mg/mL (11.61mM); Clear solution

此方案可获得 ≥ 5 mg/mL (11.61mM,饱和度未知) 的澄清溶液。

1mL 工作液为例,取 100μL 50.0 mg/mL 的澄清 EtOH 储备液加到 900μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

3.请依序添加每种溶剂: 10% EtOH90% corn oil

Solubility: ≥ 5 mg/mL (11.61mM); Clear solution

此方案可获得 ≥ 5 mg/mL (11.61mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

1mL 工作液为例,取 100μL 50.0 mg/mL 的澄清 EtOH 储备液加到 900μL玉米油中,混合均匀。

4.请依序添加每种溶剂: 10% DMSO40% PEG3005% Tween-80→45% saline

Solubility: ≥ 2.5 mg/mL (5.81mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.81mM,饱和度未知) 的澄清溶液。

1 mL 工作液为例,取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50μL Tween-80,混合均匀;然后继续加入 450μL生理盐水定容至 1mL。

5.请依序添加每种溶剂: 10% DMSO90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.81mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.81mM,饱和度未知) 的澄清溶液。

1mL 工作液为例,取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

6.请依序添加每种溶剂: 10% DMSO90% corn oil

Solubility: ≥ 2.5 mg/mL (5.81mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.81mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

1mL 工作液为例,取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900μL玉米油中,混合均匀。

7.请依序添加每种溶剂: 5% DMSO40% PEG3005% Tween-8050% saline

Solubility: 2.5 mg/mL (5.81mM); Suspended solution; Need ultrasonic

8.请依序添加每种溶剂: 5% DMSO95% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.81mM); Clear solution

1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。

 

制备储备液

 

浓度

 

溶液体积

质量

 

1mg

 

5mg

 

10mg

1mM

2.3222mL

11.6112mL

23.2223mL

5mM

0.4644mL

2.3222mL

4.6445mL

10mM

0.2322mL

1.1611mL

2.3222mL

 

生物活性

产品描述

1,25-Dihydroxyvitamin D3类似物,可作用于银屑病。

靶点

vitamin D receptor

体外研究

When NHEK cells are not stimulated with IL-17A or IL-22, Calcipotriol slightly enhances (0.2nM) IL-8 mRNA expression or has no effect (2-20nM). The addition of IL-17A and IL-22 markedly increased the mRNA expression of IL-8, confirming our previous study. This enhanced IL-8 mRNA expression is suppressed by Calcipotriol at 2, 20 and 40nM in a dose dependent manner. Treatment of natural killer (NK) cells with drugs modulates their expression of NK cytotoxicity receptors or KIR. Human NK cells are pre-treated with 100, 10 or 1ng/mL of 1,25(OH)2D3, Calcipotriol or FTY720 for 4 h. All three concentrations of 1,25(OH)2D3, Calcipotriol and FTY720 significantly up-regulate the expression of NKp30 on the surface of NK cells after 4 h incubation.

体内研究

One out of the 32 animals in each of the groups has died, except for the Diclofenac plus DFMO plus Calcipotriol group, where all animals survived. Survival is equally distributed between the groups. The weight gain is significantly smaller in the groups treated with Diclofenac plus Calcipotriol (p=0.018) and Diclofenac plus DFMO plus Calcipotriol (p=0.002) compare with placebo (linear regression model)

特征

 

 

推荐实验方法(仅供参考)

Cell Assay

Normal human epidermal keratinocytes (NHEK) are grown in serum-free keratinocyte growth medium Epilife and used at third passage in all experiments. Growth supplement is omitted 48 h before experiments. As a control, IL-17A and IL-22 are either added or not added to the cells. Cultured NHEK cells are stimulated with IL-17A (200ng/mL) and/or IL-22 (200 ng/mL) followed by co-incubation in the presence or absence of Calcipotriol at 0.2-40nM to test its modulatory effect. Cells are harvested 3 days later and subjected to real-time quantitative PCR (qPCR). Culture supernatants are also collected and frozen at -80°C until use for ELISA

 

Animal Administration

Mice
The 160 female SKH-1 hairless mice (6-7 weeks of age) are used. After UV treatment, mice without tumors are randomly divided into five groups, four chemoprevention groups (Diclofenac plus DFMO; Diclofenac plus Calcipotriol; DFMO plus calcitriol; and Diclofenac plus DFMO plus Calcipotriol) and one placebo group (skin lotion). The placebo group used in this study is the same as the one used in an earlier study. The mice are treated with test mixtures once a day, five days a week, for a total of 17 weeks. The test mixtures are applied topically on the dorsal surface of the mice. Ten microliters are applied by a pipette after which the mixture is rubbed onto the skin. This corresponded to the following doses of each active substance in the treatments: 100μg/week for Diclofenac (30 mg/g undiluted), 0.166 μg/week for Calcitriol (50μg/g undiluted), and 463.3μg/week for difluoromethylornithine (DFMO) (139 mg/g undiluted).

保存条件:
2-8℃ 充氮保存
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

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    *选择对应的单位 *空出希望得到的变量,填写另外两个变量

用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )

  • * = *

连续稀释计算器方程

  • 连续稀释

  • 初始浓度:
  • 稀释倍数:
  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):