Tacalcitol
(Synonyms: 他卡西醇; 1,24(R)-Dihydroxyvitamin D3; 1.alpha.,24R-Dihydroxyvitamin D3) 目录号 : GC10890
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Tacalcitol是骨化三醇（Calcitriol）类似物，通过刺激肠道钙吸收和影响骨骼转换来调节钙代谢。
Cas No.:57333-96-7
Sample solution is provided at 25 µL, 10mM.
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Tacalcitol is a calcitriol analogue, regulates calcium metabolism by stimulating intestinal calcium absorption and influencing bone turnover. But tacalcitol has no significant change in bone formation [1]. Tacalcitol can be used in the research of inflammation, breast cancer, and skin diseases, and prevent the osteoporosis that results from the development of cancer or from chemotherapy or hormone therapy [2-3].
In vitro, treatment of normal human keratinoeytes with tacalcitol (0.01-1μM; 48h) increased the numbers of involucrin positive cells and induced cell differentiation [4].
In vivo, tacalcitol (1.0µg/kg; s.c.; thrice weekly) decreased bone column density, transiently decreased the metastatic spread of 4T1 breast carcinoma without influencing primary tumour growth or angiogenesis in old ovariectomized (OVX) mice [2]. While tacalcitol (1.0µg/kg; s.c.; thrice weekly) increased metastatic spread in young mice bearing 4T1 breast cancer [5].
References:
[1] Yamada, S., J-P. Bonjour, and H. Fleisch. "Effect of 1α, 24 (R)-dihydroxyvitamin D3 on calcium metabolism in the rat." European Journal of Endocrinology 111.4 (1986): 572-576.
[2] Anisiewicz, Artur, et al. "Calcitriol analogues decrease lung metastasis but impair bone metabolism in aged ovariectomized mice bearing 4T1 mammary gland tumours." Aging and disease 10.5 (2019): 977.
[3] Matsumoto, Kunio, et al. "Effect of 1, 24R‐dihydroxyvitamin D3 on the growth of human keratinocytes." The Journal of Dermatology 17.2 (1990): 97-103.
[4] Kobayashi, Teruaki, et al. "1α, 24R‐dihydroxyvitamin D3 has an ability comparable to that of 1α,25‐dihydroxyvitamin D3 to induce keratinocyte differentiation." The Journal of Dermatology 17.11 (1990): 707-709.
[5] Anisiewicz, Artur, et al. "Unfavorable effect of calcitriol and its low-calcemic analogs on metastasis of 4T1 mouse mammary gland cancer." International journal of oncology 52.1 (2018): 103-126.
Tacalcitol是骨化三醇（Calcitriol）类似物，通过刺激肠道钙吸收和影响骨骼转换来调节钙代谢。但骨化醇对骨形成没有显著影响[1]。Tacalcitol可用于炎症、乳腺癌和皮肤病的研究，并能预防癌症发展、化疗或激素治疗所导致的骨质疏松症[2-3]。
在体外，用Tacalcitol（0.01 - 1μM；48小时）处理正常的人类角质形成细胞，可增加包涵蛋白阳性细胞的数量，并诱导细胞分化[4]。
在体内，Tacalcitol（1.0µg/kg；皮下注射；每周三次）可降低骨柱密度，暂时减少4T1乳腺癌的转移扩散，但不影响老年卵巢切除（OVX）小鼠的原发肿瘤生长或血管生成[2]。然而，在携带4T1乳腺癌的年轻小鼠中，Tacalcitol（1.0µg/kg；皮下注射；每周三次）会增加癌症转移扩散[5]。
| Cell experiment [1]: | |
Cell lines | Human keratinocytes |
Preparation Method | Cells were cultured in the presence or absence of tacalcitol (1,24R(OH)2D3); or 1,25(OH)2D3, for 48h. Cells were immunochemically stained using anti-involucrin antibody, and the number of cells expressing involucrin was determined by Flow cytometry using a FACScan. |
Reaction Conditions | 0.01-1μM; 48h |
Applications | The treatment with tacalcitol increased the numbers of involucrin positive cells. |
| Animal experiment [2]: | |
Animal models | 60 weeks old ovariectomized (OVX) mice bearing 4T1 tumours |
Preparation Method | Tacalcitol were administered subcutaneously (s.c.) thrice weekly starting from day 7 after tumor cell inoculation. The single dose of compounds was as follows: calcitriol, 0.5µg/kg; Tacalcitol, 1.0µg/kg; and PRI-2205, 10.0µg/kg. Control mice (both OVX and sham operated) were administered with vehicle (80% PEG) in the same volume and scheme as vitamin D compounds. |
Dosage form | 1.0µg/kg; s.c.; thrice weekly |
Applications | Tacalcitol transiently decreased the metastatic spread of 4T1 breast carcinoma without influencing primary tumour growth or angiogenesis in old OVX mice. |
References: | |
| Cas No. | 57333-96-7 | SDF | |
| 别名 | 他卡西醇; 1,24(R)-Dihydroxyvitamin D3; 1.alpha.,24R-Dihydroxyvitamin D3 | ||
| 化学名 | (1R,3S,5Z)-5-[(2E)-2-[(1R,3aS,7aR)-1-[(2R,5R)-5-hydroxy-6-methylheptan-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)C(CCC(C)C1CCC2C1(CCCC2=CC=C3CC(CC(C3=C)O)O)C)O | ||
| 分子式 | C27H44O3 | 分子量 | 416.65 |
| 溶解度 | 20mg/mL in DMSO, 20mg/mL in DMF, 20mg/mL in Ethanol | 储存条件 | Store at -20°C,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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4001 mL | 12.0005 mL | 24.001 mL |
| 5 mM | 480 μL | 2.4001 mL | 4.8002 mL |
| 10 mM | 240 μL | 1.2 mL | 2.4001 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。
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet