Incyclinide (CMT-3)
(Synonyms: CMT-3; COL-3) 目录号 : GC32823
An inhibitor of MMP-13, MMP-1, and MMP-8
Cas No.:15866-90-7
Sample solution is provided at 25 µL, 10mM.
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Incyclinide is a non-antimicrobial chemically modified tetracycline (CMT) and an inhibitor of matrix metalloproteinase-13 (MMP-13), MMP-1, and MMP-8 (IC50s = 0.3, 34, and 48 ?g/ml, respectively).1 It inhibits chick osteoclast digestion of isolated bovine bone when used at a concentration of 5 ?g/ml and inhibits IL-1-induced glycosaminoglycan release from porcine articular cartilage explants at 10 ?g/ml. Incyclinide (10 ?M) also induces cytotoxicity of HeLa and SiHa human cervical cancer cells, as well as induces apoptosis in HeLa cells and cell cycle arrest at the G0/G1 phase in SiHa cells.2
1.Greenwald, R.A., Golub, L.M., Ramamurthy, N.S., et al.In vitro sensitivity of the three mammalian collagenases to tetracycline inhibition: Relationship to bone and cartilage degradationBone22(1)33-38(1998) 2.Zhao, L., Xu, J., Yang, Y., et al.Inhibitory impacts of chemically modified tetracycline-3 and underlying mechanism in human cervical cancer cellsAnticancer Drugs24(8)799-809(2013)
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Cell experiment: |
Determination of C. albicans growth inhibition by CMT-3 is carried out by a modified turbidity assay. A series of tubes containing PDB (5 mL) and different concentrations of incyclinide (0, 0.125, 0.25, 0.5, 1.0, and 2.0 μg/mL) are each inoculated with a 100 μL suspension of C. albicans in late log phase to yield a final cell concentration of 106/mL. The tubes are aerobically incubated at 35°C, and at each time point (0, 1, 2, 4, 6, 12, and 24 h), the turbidity in each tube is determined spectrophotometrically at 600 nm[2]. |
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Animal experiment: |
Rats: Eighteen Wistar rats receive a standardized orthodontic appliance at one side of the maxilla. During 14 days, three groups of six rats receive a daily dose of 0, 6 or 30 mg/kg incyclinide, and tooth displacement is measured. Thereafter, osteoclasts are counted on histological sections using an ED-1 staining. Multi- and mononuclear ED-1-positive cells in the PDL are also counted. In addition, sections are stained for MMP-9[3]. |
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References: [1]. Lee HM, et al. CMT-3, a non-antimicrobial tetracycline (TC), inhibits MT1-MMPactivity: relevance to cancer. Curr Med Chem. 2001 Feb;8(3):257-60. |
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| Cas No. | 15866-90-7 | SDF | |
| 别名 | CMT-3; COL-3 | ||
| Canonical SMILES | O=C(C(C1=O)=C(O)C[C@]2([H])C[C@]3([H])CC4=C(C(C3=C(O)[C@@]21O)=O)C(O)=CC=C4)N | ||
| 分子式 | C19H17NO7 | 分子量 | 371.34 |
| 溶解度 | DMSO : ≥ 100 mg/mL (269.29 mM) | 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 | 2.6929 mL | 13.4647 mL | 26.9295 mL |
| 5 mM | 0.5386 mL | 2.6929 mL | 5.3859 mL |
| 10 mM | 0.2693 mL | 1.3465 mL | 2.6929 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet