Endothelin 3 (human, rat)
(Synonyms: 人内皮素3,Endothelin 3 (Rat,Human)) 目录号 : GC13924
A peptide vasoconstrictor
Cas No.:117399-93-6
Sample solution is provided at 25 µL, 10mM.
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Endothelin-3, human, mouse, rabbit, rat is a 21-amino acid vasoactive peptide that binds to G-protein-linked transmembrane receptors, ET-RA and ET-RB.
The endothelins (ETs) are a family of 21-amino-acid vasoconstrictor peptides comprising three distinct isoforms: ET-1, ET2 and Endothelin-3. Endothelin-3 is detected in plasma, heart, brain and vascular smooth muscle cells (VSMCs). The surface enzymes of VSMCs break down big Endothelin-3 to the corresponding mature peptide, Endothelin-3. Endothelin-3 down-regulate endothelin ETA receptor expression in coronary artery VSMCs without affecting receptor density or functional ETA receptor responses. By contrast, high concentrations of Endothelin-3 (100 nM) increase the expression of ETB receptors but abolish the vasoconstrictor response of the receptors, possibly due to the desensitizing effect of Endothelin-3[1]. Endothelin-3 stimulates ENCC adhesion to various ECM components. Endothelin-3 induces rapid changes in ENCC shape and protrusion dynamics favouring sustained growth and stabilization of lamellipodia, a process coincident with the increase in the number of focal adhesions and activated β1-integrins[2].
Endothelin-3 at low concentrations may attenuate inflammatory responses via ETB2 activation and NO production. Endothelin-3, which acts mainly on ETB, at low concentrations specifically inhibited platelet-activating factor (PAF)-induced paw oedema, whereas neither ET-1 nor Endothelin-2, both of which act on ETA and ETB, showed inhibitory activity. The inhibition by ET-1 and Endothelin-3 (each 0.5 pmol/paw) in the presence of BQ-123 (66.4 ± 6.7 % and 65.4 ± 22.6 %, respectively), is comparable to that by Endothelin-3 (0.5 pmol/paw) alone (65.4 ± 10.9 %), whereas neither ET-1 nor Endothelin-3 in the presence of BQ-788 showed inhibitory activity[3].
References:
[1]. Skovsted GF, et al. Endothelin-1 and Endothelin-3 Regulate Endothelin Receptor Expression in Rat Coronary Arteries. Basic Clin Pharmacol Toxicol. 2015 Nov;117(5):297-305.
[2]. Gazquez E, et al. Endothelin-3 stimulates cell adhesion and cooperates with β1-integrins during enteric nervous system ontogenesis. Sci Rep. 2016 Dec 1;6:37877. doi: 10.1038/srep37877.
[3]. Sato A, et al. Endothelin-3 at low concentrations attenuates inflammatory responses via the endothelin B2 receptor. Inflamm Res. 2013 Apr;62(4):417-24.
| Cas No. | 117399-93-6 | SDF | |
| 别名 | 人内皮素3,Endothelin 3 (Rat,Human) | ||
| 化学名 | (1Z,3S,4Z,6S,7Z,9S,10Z,12S,13Z,15S,16Z,18S)-3-((1H-imidazol-5-yl)methyl)-18-((1H-indol-3-yl)methyl)-1-((1R,2Z,4S,5Z,7S,8Z,10S,11E,13S,14Z,16S,17Z,19S,20Z,22S,23Z,25R,26Z,28S,29Z,31R,36R,37Z,39S,40Z,42S,43Z,45S,46Z)-31-amino-7,13-bis(4-aminobutyl)-22-benzy | ||
| Canonical SMILES | CC[C@]([C@@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@]1([H])CSSC[C@@](N)([H])/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N\[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/2)([H])CCC(O)=O)([H]) | ||
| 分子式 | C121H168N26O33S4 | 分子量 | 2643.04 |
| 溶解度 | Soluble to 1 mg/ml in Water | 储存条件 | Desiccate 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 | 0.3784 mL | 1.8918 mL | 3.7835 mL |
| 5 mM | 0.0757 mL | 0.3784 mL | 0.7567 mL |
| 10 mM | 0.0378 mL | 0.1892 mL | 0.3784 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