Endothelin Mordulator 1
(Synonyms: N-(2-乙酰基-4,6-二甲基苯基)-3-[[(3,4-二甲基-5-异恶唑基)氨基]磺酰基]-2-噻吩甲酰胺) 目录号 : GC30577Endothelin Mordulator 1 是一种内皮素受体调节剂,用于研究内皮素介导的疾病。
Cas No.:349453-49-2
Sample solution is provided at 25 µL, 10mM.
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Endothelin Mordulator 1 is a endothelin receptor modulator, used for the research of endothelin-mediated disorders.
Endothelin Mordulator 1 is a endothelin receptor modulator, used for the research of endothelin-mediated disorders[1].
[1]. Jinling Chen, et al. Formulations of n-(2-acetyl-4,6-dimethylphenyl)-3--2-thiophenecarboxamide. US20080317858A1.
Cas No. | 349453-49-2 | SDF | |
别名 | N-(2-乙酰基-4,6-二甲基苯基)-3-[[(3,4-二甲基-5-异恶唑基)氨基]磺酰基]-2-噻吩甲酰胺 | ||
Canonical SMILES | CC(C(C)=NO1)=C1NS(=O)(C2=C(SC=C2)C(NC3=C(C=C(C)C=C3C)C(C)=O)=O)=O | ||
分子式 | C20H21N3O5S2 | 分子量 | 447.53 |
溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 2.2345 mL | 11.1724 mL | 22.3449 mL |
5 mM | 0.4469 mL | 2.2345 mL | 4.469 mL |
10 mM | 0.2234 mL | 1.1172 mL | 2.2345 mL |
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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 | |||
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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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Endothelin-1 and the regulation of vascular tone
1. In 1988, Yanagisawa et al. reported the presence of a potent peptide from the supernatant of porcine endothelial cells. This was later named endothelin-1 (ET-1) and was found to belong to a new family of vasoconstrictor peptides. There are at least three isoforms of endothelin: ET-1, endothelin-2 and endothelin-3. 2. ET-1 is produced from a larger precursor molecule by endothelin converting enzyme (ECE); there may be a number of ECE but the most physiologically relevant appears to be a membrane-bound neutral metalloprotease. The endothelin precursor is produced on demand and is regulated at the mRNA level. 3. Two subtypes of mammalian endothelin receptors have been cloned and sequenced: ETA receptors which mediate vasoconstriction and ETB receptors which mediate both vasoconstriction and vasodilatation. However, functional studies have indicated that other subtypes of endothelin receptors may exist. 4. ET-1 has a wide range of biological actions apart from its direct effects on vascular tone, including constriction of non-vascular smooth muscle, cardiac effects, mitogenesis and stimulation of the release of hormones such as atrial natriuretic peptide and prostacyclin. At low concentrations which have no direct vasoconstrictor action, ET-1 potentiates the effect of other vasoconstrictor agonists. 5. The precise role of ET-1 in health and disease is not well defined at present; however, there are indications that it may have a role in the pathogenesis of some cardiovascular disease states, including subarachnoid haemorrhage, renal ischaemia and certain types of hypertension.
Endothelin-1 and big endothelin-1 in NIDDM patients with and without microangiopathy
To examine a possible role for endothelin-1 in the pathophysiology of diabetic microangiopathy, we measured plasma levels of endothelin-1 and big endothelin-1, a precursor peptide of endothelin-1, in 33 untreated patients with non-insulin-dependent diabetes mellitus. There was no significant difference among the mean plasma endothelin-1 concentrations in 18 patients with microangiopathy, in 15 patients without microangiopathy and in 33 age-matched normal subjects. In contrast, the mean plasma big endothelin-1 concentration in patients with microangiopathy was significantly higher than in those without microangiopathy or in normal subjects. As a consequence, the mean big endothelin-1 to endothelin-1 ratio in patients with microangiopathy was significantly higher than in the other two groups. There was no significant correlation between plasma levels of endothelin-1 or big endothelin-1 and fasting blood glucose, HbA1c, mean blood pressure, or period of duration of diabetes mellitus in the patient groups. The results indicate that elevation of plasma big endothelin-1 levels with diminished conversion of big endothelin-1 to endothelin-1 is associated with diabetic microangiopathy, which may be the effect rather than the cause of endothelial dysfunction.
Themed section: endothelin
This themed section of the British Journal of Pharmacology contains reviews on recent developments in endothelin research arising from the Twelfth International Conference on Endothelin (ET-12). It includes the emerging role for endothelin-2 in the cardiovascular system, ovarian development, immunology and cancer. The action of endothelin on two key targets is discussed: the paracrine or autocrine regulation of contractility and growth in the heart and the role of endothelin in renal disease. Epidemiological studies have demonstrated cardiovascular disease and circulating levels of endothelin-1 are lower in premenopausal women than in men and evidence is presented for the contribution of sex differences in responses to the peptide. Transcription is the primary level of regulation of the endothelin gene; and current research on the epigenetic regulation of the endothelin pathway, including the silencing of the EDNRB gene encoding the ET(B) receptor during tumourigenesis, is reviewed.
Linked articles: This article is part of a themed section on Endothelin. To view the other articles in this section visit http://dx.doi.org/10.1111/bph.2013.168.issue-1. To view the previously published paper by Dhaun et al. visit http://dx.doi.org/10.1111/j.1476-5381.2012.02070.x.
Localization of endothelin-1 and endothelin-3 in the cochlea
The distribution of endothelin-1 (ET-1) and endothelin-3 (ET-3) was studied by indirect immunostaining of decalcified guinea pig and rat cochleae. No species differences were observed. Perikarya and processes of spiral ganglion cells were highly reactive for both ET-1 and ET-3. The epithelial lining of the cochlear duct stained for ET-1 and ET-3, but reactivity for ET-1 was higher in the lining cells of the inner sulcus, Claudius', and Hensen's cells, while the tympanic covering layer of the basilar membrane stained stronger for ET-3 compared to ET-1. In the stria vascularis, all cell types stained for ET-3, while marginal cells were more reactive for ET-1. Spiral ligament fibroblasts were reactive for ET-1, but not for ET-3. Connective tissue cells of the spiral limbus stained for both endothelins. The region of synapses on outer hair cells reacted for ET-1 and ET-3 but sensory cells remained unstained. Endothelins are discussed to act as modulatory peptides, possibly interfering with nitric oxide, prostaglandins, and atrial natriuretic peptide in the lateral cochlear wall (lateral cochlear wall, i.e. stria vascularis and spiral ligament). The occurrence of endothelins in cochlear neurons suggest their potential role as neurotransmitters.