Calcipotriol
(Synonyms: 卡泊三醇; MC 903; Calcipotriene) 目录号 : GC17682
A vitamin D3 analog
Cas No.:112965-21-6
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
|
Cell lines |
Human HL-60 and MCF-7 cell lines |
|
Preparation method |
Soluble in DMSO > 16.7mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
1, 10, 100, 1000 nM for 24 h |
|
Applications |
Calcipotriol revealed a strong proliferation inhibition in HL-60 cells, the potentiation of the antiproliferative effect of CIS(cisplatin) could be observed. In MCF-7 cells, a lower dose of TX (tamoxifen) in combination with calcipotriol caused an increase in the G0/G1 and a decrease in the G2/M stage as compared to TX alone. |
| Clinical experiment [2]: | |
|
Diseases models |
Patients with vulgaris psoriasis aged ≥18 years |
|
Dosage form |
Foam of calcipotriol 50μg/g plus betamethasone 0.5 mg/g, 4, 8, 12 weeks, topical treatment |
|
Application |
A greater proportion of patients achieved modified Psoriasis Area and Severity Index 75 and 90 at weeks 4, 8, and 12 with the calcipotriol 50μg/g plus betamethasone 0.5 mg/g (Cal/BD) foam. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1]. Milczarek M1, Chodyński M, et al, Synthesis and Biological Activity of Diastereomeric and Geometric Analogs of Calcipotriol, PRI-2202 and PRI-2205, Against Human HL-60 Leukemia and MCF-7 Breast Cancer Cells. Cancers (Basel). 2013 Oct 31;5(4):1355-78. doi: 10.3390/cancers5041355. [2]. Paul C1, Leonardi C2, et al, Calcipotriol Plus Betamethasone Dipropionate Aerosol Foam in Patients with Moderate-to-Severe Psoriasis: Sub-Group Analysis of the PSO-ABLE Study. Am J Clin Dermatol. 2017 Jun;18(3):405-411. doi: 10.1007/s40257-017-0258-0. |
|
Calcipotriol is an analogue of vitamin D3. [1]
Calcipotriol is a ligand of VDR-like receptors and is used as a first-line topical agent in the treatment of psoriasis.[1-2] Calcipotriol is much less effective in causing hypercalcemia.[3] The vitamin D receptor is found on the cells of many different tissues including T cells of the immune system. T cells are known to play a role in psoriasis, and the binding of calcipotriol to VDR modulates the T cells gene transcription of cell differentiation and proliferation related genes. Calcipotriol induced apoptosis in eratinocytes isolated from psoriatic plaques at 100 nM for 20 h.[4] Calcipotriol also induced autophagy in both HeLa cells and keratinocytes.[2] Calcipotriol inhibited the proliferation of HL-60 and MCF-7 cells dose-dependently from 1 nM-1000 nM.[5] Calcipotriol is a potent inducer of terminal differentiation in cultured human keratinocytes.[3] Calcipotriol also decreased the mRNA expression/production of human cathelicidin antimicrobial protein (hCAP18) and LL37 peptide by IL-17A/IL-22-stimulated keratinocytes at 40 nM.[6]
References:
1. M. R. Klaber, P. E. Hutchinson, A. Pedvis-Leftick, K. Kragballe, T. L. Reunala, P. C. Van de Kerkhof, M. K. Johnsson, L. Molin, M. S. Corbett and N. Downess, Br J Dermatol 1994, 131, 678-683.
2. R. C. Wang and B. Levine, J Invest Dermatol 2011, 131, 990-993.
3. K. Kragballe and I. L. Wildfang, Arch Dermatol Res 1990, 282, 164-167.
4. R. Tiberio, C. Bozzo, G. Pertusi, F. Graziola, M. Gattoni, P. Griffanti, P. Boggio, E. Colombo and G. Leigheb, Clin Exp Dermatol 2009, 34, e972-974.
5. M. Milczarek, M. Chodynski, B. Filip-Psurska, A. Martowicz, M. Krupa, K. Krajewski, A. Kutner and J. Wietrzyk, Cancers (Basel) 2013, 5, 1355-1378.
6. J. Sakabe, T. Umayahara, M. Hiroike, T. Shimauchi, T. Ito and Y. Tokura, Acta Derm Venereol 2014, 94, 512-516.
| Cas No. | 112965-21-6 | SDF | |
| 别名 | 卡泊三醇; MC 903; Calcipotriene | ||
| 化学名 | (1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(E,2R,5S)-5-cyclopropyl-5-hydroxypent-3-en-2-yl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol | ||
| Canonical SMILES | CC(C=CC(C1CC1)O)C2CCC3C2(CCCC3=CC=C4CC(CC(C4=C)O)O)C | ||
| 分子式 | C27H40O3 | 分子量 | 412.62 |
| 溶解度 | ≥ 16.7 mg/mL in DMSO, ≥ 87.6 mg/mL in EtOH with gentle warming | 储存条件 | -20°C, protect from light, stored under nitrogen,unstable in solution, ready to use. |
| General tips | 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。 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。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4235 mL | 12.1177 mL | 24.2354 mL |
| 5 mM | 0.4847 mL | 2.4235 mL | 4.8471 mL |
| 10 mM | 0.2424 mL | 1.2118 mL | 2.4235 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。