Yoda1 |
| カタログ番号GC18233 |
Yoda1は、ヒトおよびマウスのPiezo1のアゴニストである。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 448947-81-7
Sample solution is provided at 25 µL, 10mM.
Yoda1は、ヒトおよびマウスのPiezo1のアゴニストである。Yoda1は精製したPiezo1チャネルを活性化する。マウスのEC50は17.1μm、ヒトのEC50は26.6μmであった。Yoda1はPiezoのゲート機構や様々なPIEzO関連の生物学的プロセスの研究に広く用いられている。
Yoda1は内皮細胞（EC）においてAktとERK1/2の活性化を誘導するが、これはPiezo1には依存しない。Yoda1はAktとERK1/2の活性化を誘導し、それぞれのリン酸化レベルの増加は、Yoda1濃度の増加とともに2つのシグナル分子のリン酸化も増加することを反映していた。 Piezo1アゴニストであるYoda1によるPiezo1の活性化は、HK2細胞にカルシウム流入とプロフィブロティック応答を引き起こし、カルシウム依存性プロテアーゼであるカルパイン2の活性化を誘導し、次いで接着複合タンパク質であるタリン1の切断とインテグリンβ1のアップレギュレーションを引き起こした。また、Yoda1は、ECMとインテグリンβ1の間のリンクを促進した.Yoda1は、MDA-MB-231乳がん細胞の移動制御における骨細胞上の低倍率高周波振動を増強した。
アゴニストYoda1は、高血圧によるカルシウム流入を効果的に抑制した。抗血栓研究では、Piezo1の阻害が高血圧マウスの動脈血栓症を効果的に抑制し、脳卒中の梗塞サイズを縮小させることが証明された。Yoda1様運動ピルは、運動中のPiezo1活性を特異的に標的化して増強する。
References:
[1]: Syeda R, Xu J, et,al. Chemical activation of the mechanotransduction channel Piezo1. Elife. 2015 May 22;4:e07369. doi: 10.7554/eLife.07369. PMID: 26001275; PMCID: PMC4456433.
[2]:Dela Paz NG, Frangos JA. Yoda1-induced phosphorylation of Akt and ERK1/2 does not require Piezo1 activation. Biochem Biophys Res Commun. 2018 Feb 26;497(1):220-225. doi: 10.1016/j.bbrc.2018.02.058. Epub 2018 Feb 8. PMID: 29428723; PMCID: PMC5835220.
[3]:Beech DJ. Endothelial Piezo1 channels as sensors of exercise. J Physiol. 2018 Mar 15;596(6):979-984. doi: 10.1113/JP274396. Epub 2018 Jan 9. PMID: 29194632; PMCID: PMC5851887.
[4]: Kuriyama M, Hirose H, et,al. Piezo1 activation using Yoda1 inhibits macropinocytosis in A431 human epidermoid carcinoma cells. Sci Rep. 2022 Apr 15;12(1):6322. doi: 10.1038/s41598-022-10153-8. Erratum in: Sci Rep. 2022 May 12;12(1):7873. PMID: 35428847; PMCID: PMC9012786.
[5]: Douguet D, Patel A, et,al. Piezo Ion Channels in Cardiovascular Mechanobiology. Trends Pharmacol Sci. 2019 Dec;40(12):956-970. doi: 10.1016/j.tips.2019.10.002. Epub 2019 Nov 5. PMID: 31704174.
[6]: Zhao W, Wei Z, et,al.Piezo1 initiates platelet hyperreactivity and accelerates thrombosis in hypertension. J Thromb Haemost. 2021 Dec;19(12):3113-3125. doi: 10.1111/jth.15504. Epub 2021 Oct 8. PMID: 34411418.
[7]: Zhao X, Kong Y, et,al. Mechanosensitive Piezo1 channels mediate renal fibrosis. JCI Insight. 2022 Apr 8;7(7):e152330. doi: 10.1172/jci.insight.152330. PMID: 35230979; PMCID: PMC9057604.
[8]: Lin CY, Song X, et,al. Yoda1 Enhanced Low-Magnitude High-Frequency Vibration on Osteocytes in Regulation of MDA-MB-231 Breast Cancer Cell Migration. Cancers (Basel). 2022 Jul 13;14(14):3395. doi: 10.3390/cancers14143395. PMID: 35884459; PMCID: PMC9324638.
| 細胞実験[1]: | |
細胞株 | ヒト冠動脈内皮細胞（HCAECs） |
準備方法 | ヒト冠動脈内皮細胞（HCAEC）を指示濃度のYoda1で5分間処理した。 |
反応条件 | 1.5/3.0/6.0 µM、5分間 |
アプリケーション | Yoda1はAktおよびERK1/2の活性化を誘導し、それぞれのリン酸化レベルの上昇は、Yoda1濃度の上昇とともに2つのシグナル分子のリン酸化も上昇することを反映した。 |
| 動物実験 [2]: | |
動物モデル | 8週齢SPF雄性C57BL/6マウス |
準備方法 | 高血圧マウスにGSMTX-4、Yoda1（Yod、4μg/kg/day）またはLY294002を尾静脈より3日間注射した。 |
投与形態 | Yoda1 4μg/kg/日を3日間投与 |
アプリケーション | アゴニストYoda1は、高血圧によるカルシウム流入を効果的に抑制した。抗血栓試験において、Piezo1の阻害が高血圧マウスの動脈血栓症を効果的に抑制し、脳梗塞の梗塞サイズを縮小させることが証明された。 |
参考文献: [1]: Dela Paz NG, Frangos JA. Yoda1-induced phosphorylation of Akt and ERK1/2 does not require Piezo1 activation. Biochem Biophys Res Commun. 2018 Feb 26;497(1):220-225. doi: 10.1016/j.bbrc.2018.02.058. Epub 2018 Feb 8. PMID: 29428723; PMCID: PMC5835220. [2]: Zhao W, Wei Z, et,al. Piezo1 initiates platelet hyperreactivity and accelerates thrombosis in hypertension. J Thromb Haemost. 2021 Dec;19(12):3113-3125. doi: 10.1111/jth.15504. Epub 2021 Oct 8. PMID: 34411418. | |
| Cas No. | 448947-81-7 | SDF | |
| Chemical Name | 2-[5-[[(2,6-dichlorophenyl)methyl]thio]-1,3,4-thiadiazol-2-yl]-pyrazine | ||
| Canonical SMILES | ClC(C=CC=C1Cl)=C1CSC2=NN=C(C3=CN=CC=N3)S2 | ||
| Formula | C13H8Cl2N4S2 | M.Wt | 355.3 |
| 溶解度 | DMSO : 25 mg/mL (70.37 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8145 mL | 14.0726 mL | 28.1452 mL |
| 5 mM | 0.5629 mL | 2.8145 mL | 5.629 mL |
| 10 mM | 0.2815 mL | 1.4073 mL | 2.8145 mL |
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Quality Control & SDS
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- Purity: >98.00%
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Related Biological Data
Mechano-stress upregulates the transcription of POSTN via NF-κB p65 (L) ChIP-qPCR assay was performed with anti-NF-κB p65 using hNPCs treated with PBS, TNF-α, or Yoda1 for 24 h to identify the binding between NF-κB p65 and the POSTN promoter.
Quantitation of Ca2+ influx changes in hNPCs after 5 μM Yoda1(GLPBIO) stimulation (left panel), and representative fluorescence images at indicated time points(right panel). Yoda1 was administrated at 10 s.
Molecular therapy S1525-0016. PMID: 35619555 IF: 11.4545 -
Related Biological Data
The correlation between trans-differentiation and PIEZO1/YAP expression in MSCs. (G) Densitometric analysis of blots showing the values of relevant proteins in MSCs after being treated with Yoda1 and GsMTx4.
PIEZO1 agonist Yoda1 (26.6 μM)(GLPBIO) or antagonist GsMTx4 (2.5 μM) were respectively added in the chambers.
Materials Today Advances 17 (2023): 100325. IF: 9.9176 -
Related Biological Data
FI of intracellular Ca2+ and intracellular Ca2+ levels increased by Yoda1. (a) FIbefore in EC109shRNA‑piezo1 and EC109shRNA‑control cells.
Then, 1 mL of Piezo1 agonist Yoda1 (26.6 μM, Glpbio, USA) was added, and cells were incubated for 10 min.
ACS Omega (2021). PMID: 34056174 IF: 3.51
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