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Submit ReviewYM 254890
说明： Gα-protein inhibitor; potent inhibitor of Gq/11 signaling
化学名： (R)-1-((3S,6S,9S,12S,18R,21S,22R)-21-acetamido-18-benzyl-3-((R)-1-methoxyethyl)-4,9,10,12,16,22-hexamethyl-15-methylene-2,5,8,11,14,17,20-heptaoxo-1,19-dioxa-4,7,10,13,16-pentaazacyclodocosan-6-yl)-2-methylpropyl (2S,3R)-2-acetamido-3-hydroxy-4-methylpentanoate
纯度： ≥95% (HPLC)
生物活性 for YM 254890
YM 254890 is a Gα-protein inhibitor. Potently inhibits Gq/11 heterotrimeric G protein signaling. Inhibits ATP/UTP-induced Ca2+ increase in HCAE cells expressing P2Y2 receptor (IC50 = 50 nM); carbachol-induced production of IP1 in CHO cells expressing M1 receptor (IC50 = 95 nM); and ADP-induced Ca2+ increase in platelets, in vitro (IC50 = 2 μM). Also inhibits Gs-induced cAMP elevation and G protein-coupled MAPK/ERK signaling.
技术数据 for YM 254890
| 分子量 | 960.09 |
| 公式 | C46H69N7O15 |
| 储存 | Store at -20°C |
| 纯度 | ≥95% (HPLC) |
| CAS Number | 568580-02-9 |
| PubChem ID | 9919454 |
| InChI Key | QVYLWCAYZGFGNF-WBWCVGBTSA-N |
| Smiles | [H][C@]1(N(C([C@H]([C@@H](C(C)C)OC([C@H]([C@@H](C(C)C)O)NC(C)=O)=O)NC([C@@H](N(C([C@@H](NC(C(N(C([C@H](OC([C@H]([C@H](OC1=O)C)NC(C)=O)=O)CC2=CC=CC=C2)=O)C)=C)=O)C)=O)C)C)=O)=O)C)[C@H](OC)C |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for YM 254890
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 9.6 | 10 |
制备储备液 for YM 254890
以下数据基于产品分子量 960.09。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 10.42 mL | 52.08 mL | 104.16 mL |
| 0.5 mM | 2.08 mL | 10.42 mL | 20.83 mL |
| 1 mM | 1.04 mL | 5.21 mL | 10.42 mL |
| 5 mM | 0.21 mL | 1.04 mL | 2.08 mL |
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产品说明书 for YM 254890
参考文献 for YM 254890
参考文献是支持产品生物活性的出版物。
Uemura et al (2006) Biological properties of a specific Gα; q/11 inhibitor, YM-254890, on platelet functions and thrombus formation under high-shear stress. Br.J.Pharmacol. 148 61 PMID: 16520742
Xiong et al (2016) Total synthesis and structure-activity relationship studies of a series of selective G protein inhibitors. Nat.Chem. 8 1035 PMID: 27768111
Xiong et al (2019) Structure-activity relationship studies of the natural product Gq/11 protein inhibitor YM-254890. Chem.Med.Chem. 14 865 PMID: 30790465
Peng et al (2021) Functional evidence for biased inhibition of G protein signaling by YM-254890 in human coronary artery endothelial cells. Eur.J.Pharmacol. 891 173706 PMID: 33152337
Schlegel et al (2021) Macrocyclic Gq protein inhibitors FR900359 and/or YM-254890-fit for translation? ACS Pharmacol.Transl.Sci. 4 888 PMID: 33860209
If you know of a relevant reference for YM 254890, please let us know.
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关键词: YM 254890, YM 254890 supplier, YM254890, heterotrimeric, g, protein, signaling, GPCRs, coupled, receptors, Galpha, Ga, Galfa, G9/11, Gi/o, potent, inhibitors, inhibits, Heterotrimeric, G-protein, GTPases, 7352, Tocris Bioscience
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