U 46619
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
EC50:作用于形状变化为0.035 μM、作用于MLCP为0.057 μM、作用于血清素释放为0.536 μM、作用于聚集为0.057 μM,作用于纤维蛋白原受体结合为0.53 μM [3]。
前列腺素内过氧化物类似物U46619(11,9环氧乙烷-前列腺素H2)是一种选择性的前列腺素H2(PGH2/血栓素A2(TxA2)(TP)受体激动剂。PGH2和TxA2受体都是G-蛋白偶联受体。
体外:U46619对人血小板显示双相效应。在该化合物浓度低时,发生形状变化和MLCP(EC50 = 0.035 μM和0.057 μM);而在该化合物浓度较高时,发生血清素释放和血小板聚集(EC50 = 0.536 μM和1.31 μM)。对血小板形状变化和MLCP的效应由受体介导[3]。
体内:U46619通过激活ETA和ETB受体,引起大鼠肾皮质血管收缩和髓质血管舒张[2]。在清醒SHR(自发性高血压大鼠)中,1-100 nmol/kg U-46619 (i.c.v.)诱导剂量相关性的血压增加,但对心率没有显著影响[1]。
临床试验:目前尚未进行临床研究。
参考文献:
[1] Sirén AL, SvartstrμM-Fraser M, Paakkari I. Central cardiovascular effects of the endoperoxide analogue U-46619 in rats. Prostaglandins Leukot Med. 1985 Mar;17(3):381-6.
[2] Hantz H, Adesuyi A, Adebayo O. Differential effects of U46619 on renal regional hemodynamics in the rat: involvement of endothelin. J Pharmacol Exp Ther. 2001 Oct;299(1):372-6.
[3] Morinelli TA1, Niewiarowski S, Daniel JL, Smith JB. Receptor-mediated effects of a PGH2 analogue (U 46619) on human platelets. Am J Physiol. 1987 Nov;253(5 Pt 2):H1035-43.
- 1. JQingfeng Yu, Chengjie Wu, et al. "Inhibition of LIM kinase reduces contraction and proliferation in bladder smooth muscle." Acta Pharm Sin B. 2021 Jul;11(7):1914-1930. PMID:34386328
- 2. Fengyang Li, Dan Xu, et al. "Pretreatment of Indobufen and Aspirin and their Combinations with Clopidogrel or Ticagrelor Alleviates Inflammasome Mediated Pyroptosis Via Inhibiting NF-κB/NLRP3 Pathway in Ischemic Stroke." J Neuroimmune Pharmacol. 2021 Dec;16(4):835-853. PMID:33512659
- 3. Xu Li, Gaoqing Xu, et al. "Gonadotropin-inhibiting hormone promotes apoptosis of bovine ovary granulosa cells." Life Sci. 2021 Apr 1;270:119063. PMID:33460664
- 4. Xiao J, Wang F, et al. "Targeting the COX2/MET/TOPK signaling axis induces apoptosis in gefitinib-resistant NSCLC cells." Cell Death Dis. 2019 Oct 14;10(10):777. PMID:31611604
- 5. Luo Y, Teng X, et al. "CD146-HIF-1α hypoxic reprogramming drives vascular remodeling and pulmonary arterial hypertension." Nat Commun. 2019 Aug 7;10(1):3551. PMID:31391533
- 6. Yan YY, Ao LY, et al. "Therapeutic effects of JLX001 on cerebral ischemia through inhibiting platelet activation and thrombus formation in rats." Biomed Pharmacother. 2018 Jul 7;106:805-812. PMID:29990874
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- 8. Zhang Q, Tan CN, et al. "Adsorbed hollow fiber-based biological fingerprinting for the discovery of platelet aggregation inhibitors from Danshen-Honghua decoction." J Sep Sci. 2018 Mar 23. PMID:29573136
Physical Appearance | A solution in methyl acetate, learn about Variance in Solubility |
Storage | Store at -20°C |
M.Wt | 350.5 |
Cas No. | 56985-40-1 |
Formula | C21H34O4 |
Solubility | ≥100 mg/mL in DMSO, ≥100 mg/mL in Ethanol, ≥100 mg/mL in DMF, ≥2 mg/mL in PBS pH 7.2 |
Chemical Name | (E)-7-((1R,4R,5S,6R)-6-((S,Z)-3-hydroxyoct-1-en-1-yl)-2-oxabicyclo[2.2.1]heptan-5-yl)hept-5-enoic acid |
SDF | Download SDF |
Canonical SMILES | O[C@@H](CCCCC)/C=C\[C@@H]1[C@@H](C/C=C/CCCC(O)=O)[C@H]2C[C@H]1OC2 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
人血小板 |
溶解方法 |
溶于乙酸甲酯,预先溶解为10 mg/ml。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。 |
反应条件 |
24 h |
应用 |
在人血小板中,U46619诱导血清素释放、血小板聚集和纤维蛋白原受体,EC50值分别为0.54 ± 0.13、1.31 ± 0.34和0.53 ± 0.21 μM。 |
动物实验 [2]: | |
动物模型 |
自发性高血压大鼠(SHR) |
给药剂量 |
脑室内(ICV)给药,1–100 nmol/kg |
应用 |
在有意识的自发性高血压大鼠(SHR)中,U-46619(1–100 nmol/kg i.c.v.)引起强烈剂量相关的血压升高,但对心率无明显影响。在有意识的雄性大鼠(NR)中,血压和心率都没有显著受影响。此外,U-46619(0.1–100 nmol/kg i.c.v.)对氨基甲酸酯麻醉NR的血压、心率或通气率无明显影响。 |
注意事项 |
由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。 |
References: [1]. Morinelli T A, Niewiarowski S, Daniel J L, et al. Receptor-mediated effects of a PGH2 analogue (U 46619) on human platelets[J]. American Journal of Physiology-Heart and Circulatory Physiology, 1987, 253(5): H1035-H1043. [2]. Siren A L, Svartstrm-Fraser M, Paakkari I. Central cardiovascular effects of the endoperoxide analogue U-46619 in rats[J]. Prostaglandins, Leukotrienes and Medicine, 1985, 17(3): 381-386. |