Calcitriol Derivatives
目录号 : GC35590
Calcitriol Derivatives是维生素D3类似物。
Cas No.:2070009-24-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Calcitriol Derivatives is a vitamin D3 analog. v
[1]. Barrera D, Noyola-MartÍnez N, Avila E, Halhali A, Larrea F, DÍaz L.Calcitriol inhibits interleukin-10 expression in cultured human trophoblasts under normal and inflammatory conditions.Cytokine. 2012 Mar;57(3):316-21. [2]. Lydia A, Asanuma K, Nonaka K, Takagi M, Jeong KH, Kodama F, Asao R, Asanuma E, Prodjosudjadi W, Tomino Y.Effects of 22-oxa-calcitriol on podocyte injury in adriamycin-induced nephrosis.Am J Nephrol. 2012;35(1):58-68. [3]. Michalak K, Wicha J.Total synthesis of a CD-ring: side-chain building block for preparing 17-epi-calcitriol derivatives from the Hajos-Parrish dione.J Org Chem. 2011 Aug 19;76(16):6906-11. [4]. Moorthi RN, Kandula P, Moe SM.Optimal vitamin D, calcitriol, and vitamin D analog replacement in chronic kidney disease: to D or not to D: that is the question.Curr Opin Nephrol Hypertens. 2011 Jul;20(4):354-9. [5]. Yu WD, Ma Y, Flynn G, Muindi JR, Kong RX, Trump DL, Johnson CS.Calcitriol enhances gemcitabine anti-tumor activity in vitro and in vivo by promoting apoptosis in a human pancreatic carcinoma model system.Cell Cycle. 2010 Aug 1;9(15):3022-9.
| Cas No. | 2070009-24-2 | SDF | |
| Canonical SMILES | O[C@H](C/1=C)C[C@@H](CC1=C\C=C2[C@@](CC[C@@H]3[C@@H](CCCC(C)(O)C)C)([H])[C@]3(C)CCC\2)OCCC#N | ||
| 分子式 | C30H47NO3 | 分子量 | 469.7 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| 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 | 2.129 mL | 10.6451 mL | 21.2902 mL |
| 5 mM | 0.4258 mL | 2.129 mL | 4.258 mL |
| 10 mM | 0.2129 mL | 1.0645 mL | 2.129 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。
Calcitriol Derivatives with two different side chains at C-20. V. Potent inhibitors of mammary carcinogenesis and inducers of leukemia differentiation
J Med Chem 2009 Sep 10;52(17):5505-19.PMID:19685888DOI:10.1021/jm900780q.
Calcitriol is implicated in many cellular functions including cellular growth and differentiation, thus explaining its antitumor effects. It was shown that gemini, the calcitriol derivative containing two side chain at C20, is also active in gene transcription with enhanced antitumor activity. We have now further optimized both the A-ring and the two side chains. The chemical structures of the resulting 18 geminis were correlated with biological activities. Those containing the 1alpha-fluoro A-ring are the least active. Those featuring 23-yne and 23(E) side-chains are generally more active in human breast cancer cell growth inhibition and human leukemia cell differentiation induction than their 23(Z) counterparts. On the basis of these evaluations, we selected as lead compound a 20(R) gemini, related to calcitriol in terms of it is A-ring, where one side chain was modified by introduction of a 23-yne function and replacement of the geminal methyl groups with trifluoromethyl groups, the other created by extension of C21 with a 3-hydroxy-3-trideuteromethyl-4,4,4-trideutero-butyl moiety.
Calcitriol Derivatives with two different side chains at C-20. II. Diastereoselective syntheses of the metabolically produced 24(R)-hydroxygemini
J Med Chem 2004 Dec 16;47(26):6476-84.PMID:15588082DOI:10.1021/jm049340b.
Vitamin D derivatives containing two side chains emanating at C-20 are known as gemini. We have recently synthesized two gemini which are related to calcitriol and 19-norcalcitriol containing two identical side chains. The metabolism of these species involves 24(R)-hydroxylation on one of the side chains. To determine the outcome of this diastereospecific transformation, we synthesized both C-20 epimeric pairs containing the 24(R)-hydroxy group in the gemini and 19-norgemini series. On the basis of the availability of these reference compounds, it was shown that the metabolic hydroxylation occurred at the pro-R side chain in both gemini compounds. In comparison to the parent compounds, the 24-hydroxygemini required higher doses to increase blood calcium levels in mice and to suppress INF-gamma release in MLR.