Corynoxeine
(Synonyms: 去氢钩藤碱) 目录号 : GN10481An alkaloid with diverse biological activities
Cas No.:630-94-4
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >99.50%
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- SDS (Safety Data Sheet)
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Cell experiment: | Cell proliferation and DNA synthesis are measured. For cell counting, VSMCs are seeded in 12-well culture plates at 5-6×104 cells/mL and cultured in DMEM with 10% FBS at 37°C for 24 h. Under these conditions, the cells reach 70% confluence. The medium is then replaced by serum-free medium with Corynoxeine (5-50 μM). The cells are stimulated with 50 ng/mL PDGF-BB, then trypsinized with trypsin-EDTA and counted using a hemocytometer under a microscope. For [3H]-thymidine incorporation experiments, VSMCs are seeded in 24-well culture plates 5000 cells/well and then allowed to grow for 3-4 d in DMEM, and 2 μCi/mL of [3H]-thymidine are added to the medium. The reactions are terminated after 4 h by aspirating the medium and subjecting the cultures to sequential washes on ice with PBS containing 10% trichloroacetic acid and ethanol/ether (1 : 1, v/v). Acid-insoluble [3H]-thymidine is extracted into 250 μL of 0.5 M NaOH/well; this solution is then mixed with 3ml of scintillation cocktail and quantified using a liquid scintillation counter[1]. |
References: [1]. Kim TJ, et al. Corynoxeine isolated from the hook of Uncaria rhynchophylla inhibits rat aortic vascular smooth muscle cell proliferation through the blocking of extracellular signal regulated kinase 1/2 phosphorylation. Biol Pharm Bull. 2008 Nov;31(11):2073-8. |
Corynoxeine, isolated from the hook of Uncaria rhynchophylla, is a potent ERK1/ERK2 inhibitor of key PDGF-BB-induced vascular smooth muscle cells (VSMCs) proliferation.
Corynoxeine is able to inhibit the PDGF-BB-stimulated proliferation of VSMCs through downregulation of PDGF-BB-induced ERK1/2 activation. Pre-incubation of VSMCs with Corynoxeine significantly inhibits PDGF-BB-induced extracellular signal-regulated kinase 1/2 (ERK1/2) activation, whereas Corynoxeine has no effects on mitogen-activated protein kinase (MAPK/ERK)-activating kinase 1 and 2 (MEK1/2), Akt, or phospholipase C (PLC) γ 1 activation or on PDGF receptor beta (PDGF-Rβ) phosphorylation. Corynoxeine inhibits PDGF-BB-induced ERK1/2 activation, in the same concentration range that inhibits VSMC proliferation and DNA synthesis. Corynoxeine inhibits VSMC numbers in response to PDGF-BB with 50% inhibitory concentrations (IC50) of 13.7 μM. Corynoxeine inhibits DNA synthesis in response to PDGF-BB (24 h) with IC50 of 9.2 μM. Pre-treatment of VSMCs with Corynoxeine (5-50 μM) for 24 h results in significant decreases in cell number without any cytotoxicity; the inhibition percentages are 25.0±12.5, 63.0±27.5 and 88.0±12.5% at 5, 20 and 50 μM, respectively. Corynoxeine also significantly inhibits the 50 ng/mL PDGF-BB-induced DNA synthesis of VSMCs in a concentration-dependent manner without any cytotoxicity; the inhibitions are 32.8±11.0, 51.8±8.0 and 76.9±7.4% at concentrations of 5, 20 and 50 μM, respectively[1].
References:
[1]. Kim TJ, et al. Corynoxeine isolated from the hook of Uncaria rhynchophylla inhibits rat aortic vascular smooth muscle cell proliferation through the blocking of extracellular signal regulated kinase 1/2 phosphorylation. Biol Pharm Bull. 2008 Nov;31(11):2073-8.
Cas No. | 630-94-4 | SDF | |
别名 | 去氢钩藤碱 | ||
化学名 | methyl (E)-2-[(3R,6'R,7'S,8'aS)-6'-ethenyl-2-oxospiro[1H-indole-3,1'-3,5,6,7,8,8a-hexahydro-2H-indolizine]-7'-yl]-3-methoxyprop-2-enoate | ||
Canonical SMILES | COC=C(C1CC2C3(CCN2CC1C=C)C4=CC=CC=C4NC3=O)C(=O)OC | ||
分子式 | C22H26N2O4 | 分子量 | 382.19 |
溶解度 | ≥ 36.9mg/mL in DMSO | 储存条件 | |
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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.6165 mL | 13.0825 mL | 26.165 mL |
5 mM | 0.5233 mL | 2.6165 mL | 5.233 mL |
10 mM | 0.2616 mL | 1.3082 mL | 2.6165 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。