TEI-9647
目录号 : GC61768TEI-9647是一种维生素D3内酯类似物，可特异性抑制维生素D受体活性。TEI-9647具有抑制炎症反应的功能，还被用于探索治疗佩吉特病的研究中。
Cas No.:173388-20-0
Sample solution is provided at 25 µL, 10mM.
TEI-9647 is a vitamin D3 lactone analog that specifically inhibits vitamin D receptor activity[1-2]. TEI-9647 has anti-inflammatory effects and has also been used in research exploring the treatment of Paget's disease[3-4].
In vitro, when human promyelocytic leukemia cells (HL-60) were pretreated with TEI-9647 (1nM–1μM) for 24–96 hours, TEI-9647 significantly inhibited HL-60 cell differentiation[5].
In vivo, a single intravenous co-administration of TEI-9647 (2–50μg/kg) with 1α,25(OH)₂D₃ (0.25μg/kg) to vitamin D-deficient rats significantly suppressed the genomic effects of 1α,25(OH)₂D₃ on intestinal calcium transport and bone calcium mobilization 24 hours after treatment[6].
References:
[1] Takenouchi K, Sogawa R, Manabe K, et al. Synthesis and structure-activity relationships of TEI-9647 derivatives as Vitamin D3 antagonists. J Steroid Biochem Mol Biol. 2004 May;89-90(1-5):31-4.
[2] Miura D, Manabe K, Ozono K, et al. Antagonistic action of novel 1alpha,25-dihydroxyvitamin D3-26, 23-lactone analogs on differentiation of human leukemia cells (HL-60) induced by 1alpha,25-dihydroxyvitamin D3. J Biol Chem. 1999 Jun 4;274(23):16392-9.
[3] Dixon KM, Deo SS, Wong G, et al. Skin cancer prevention: a possible role of 1,25dihydroxyvitamin D3 and its analogs. J Steroid Biochem Mol Biol. 2005 Oct;97(1-2):137-43.
[4] Díaz L, Noyola-Martínez N, Barrera D, et al. Calcitriol inhibits TNF-alpha-induced inflammatory cytokines in human trophoblasts. J Reprod Immunol. 2009 Jul;81(1):17-24.
[5] Ishizuka S, Kurihara N, Hiruma Y, et al. 1alpha,25-Dihydroxyvitamin D(3)-26,23-lactam analogues function as vitamin D receptor antagonists in human and rodent cells. J Steroid Biochem Mol Biol. 2008 Jun;110(3-5):269-77.
[6] Ishizuka S, Miura D, Ozono K, et al. Antagonistic Actions in Vivo of (23S)-25-Dehydro-1alpha-Hydroxyvitamin D(3-)26,23-Lactone on Calcium Metabolism Induced by 1alpha,25-Dihydroxyvitamin D(3). Endocrinology. 2001 Jan;142(1):59-67.
TEI-9647是一种维生素D3内酯类似物，可特异性抑制维生素D受体活性[1-2]。TEI-9647具有抑制炎症反应的功能，还被用于探索治疗佩吉特病的研究中[3-4]。
在体外，TEI-9647（1nM-1μM）预处理人早幼粒白血病细胞（HL-60）24-96小时，TEI-9647显著抑制HL-60细胞分化[5]。
在体内，TEI-9647（2–50μg/kg）与1α,25(OH)₂D₃（0.25μg/kg）联合静脉单次注射至维生素D缺乏大鼠体内，24小时后显著抑制由1α,25(OH)₂D₃介导的肠道钙转运和骨钙动员的基因组效应[6]。
| Cell experiment [1]: | |
Cell lines | HL-60 cells (human promyelocytic leukemia cell line) |
Preparation Method | HL-60 cells were cultured in RPMI-1640 medium supplemented with 10% heat-inactivated fetal bovine serum (FBS) at 37°C, 5% CO₂. Cells were treated with TEI-9647 (1nM-1μM) for 24 hours (gene expression) or 96 hours (differentiation). |
Reaction Conditions | 1nM-1μM for 24 hours (gene expression), 96 hours (HL-60 differentiation). |
Applications | TEI-9647 significantly inhibited differentiation of HL-60 cells. |
| Animal experiment [2]: | |
Animal models | Vitamin D-deficient (-D) rats |
Preparation Method | -D rats were fed a vitamin D-deficient, low calcium diet for 7 weeks. Rats received single intravenous (iv) doses of TEI-9647 (2–50μg/kg) alone or in combination with 1α,25(OH)₂D₃ (0.25–0.5μg/kg). |
Dosage form | 2–50μg/kg; iv; Single injection. |
Applications | TEI-9647 alone weakly stimulated intestinal calcium transport and bone calcium mobilization at 8 hours but not at 24 hours in -D rats. When co-administered with 1α,25(OH)₂D₃, TEI-9647 dose-dependently antagonized 1α,25(OH)₂D₃-induced hypercalcemia, intestinal calcium absorption, and bone calcium mobilization at 24 hours. TEI-9647 also reversed 1α,25(OH)₂D₃-mediated suppression of serum PTH levels. |
References: | |
| Cas No. | 173388-20-0 | SDF | |
| Canonical SMILES | O=C1O[C@@H](C[C@H]([C@H]2CC[C@@]3([H])/C(CCC[C@]23C)=C/C=C4C([C@@H](O)C[C@H](O)C\4)=C)C)CC1=C | ||
| 分子式 | C27H38O4 | 分子量 | 426.59 |
| 溶解度 | DMSO : 100 mg/mL (234.42 mM; Need ultrasonic) | 储存条件 | 4°C, protect from light, stored under nitrogen |
| 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 | 2.3442 mL | 11.7209 mL | 23.4417 mL |
| 5 mM | 468.8 μL | 2.3442 mL | 4.6883 mL |
| 10 mM | 234.4 μL | 1.1721 mL | 2.3442 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。
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Quality Control & SDS
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- Purity: >98.00%
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