Yoda1
目录号 : GC18233
Yoda1 是人和小鼠 Piezo1 的激动剂。
Cas No.:448947-81-7
Sample solution is provided at 25 µL, 10mM.
Yoda1 is an agonist for both human and mouse Piezo1. Yoda 1 activates purified Piezo1 channels。The EC50 of mouse was 17.1 μm, and that of human was 26.6 μm[1].Yoda1 has been widely used to study the gating mechanism of Piezo and various PIEzO-related biological processes[5].
Yoda1 induces activation of both Akt and ERK1/2 in endothelial cells (ECs), which is not dependent on Piezo1[2].Yoda1 induced the activation of Akt and ERK1/2, and the increase of their respective phosphorylation levels reflected that the phosphorylation of the two signaling molecules also increased with the increase of Yoda1 concentration[4].Activation of Piezo1 by Yoda1, a Piezo1 agonist, caused calcium influx and profibrotic responses in HK2 cells and induced calcium-dependent protease calpain2 activation, followed by adhesion complex protein talin1 cleavage and upregulation of integrin β1. Also, Yoda1 promoted the link between ECM and integrin β1[7].Yoda1 Enhanced Low-Magnitude High-Frequency Vibration on Osteocytes in Regulation of MDA-MB-231 Breast Cancer Cell Migration[8].
Agonist Yoda1 effectively inhibited calcium influx caused by hypertension. Antithrombotic studies proved that the inhibition of Piezo1 effectively inhibited arterial thrombosis and reduced the infarct size of stroke in hypertensive mice[6].A Yoda1-like exercise pill has the ability to specifically target and enhance Piezo1 activity during exercise[3].
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.
Yoda1 是人和小鼠 Piezo1 的激动剂。 Yoda 1激活纯化的Piezo1通道。小鼠EC50为17.1 μm，人为26.6 μm[1]。Yoda1已被广泛用于研究Piezo的门控机制和各种PIEzO相关生物过程[5].
Yoda1 诱导内皮细胞 (EC) 中 Akt 和 ERK1/2 的激活，这不依赖于 Piezo1[2]。Yoda1 诱导 Akt 和 ERK1/2 的激活，并且它们各自磷酸化水平的增加反映了两种信号分子的磷酸化也随着 Yoda1 浓度的增加而增加[4]。Yoda1 激活 Piezo1，一种 Piezo1 激动剂，导致钙流入和促纤维化反应在 HK2 细胞中诱导钙依赖性蛋白酶钙蛋白酶 2 激活，然后是粘附复合蛋白 talin1 裂解和整合素 β1 的上调。此外，Yoda1 还促进了 ECM 与整合素 β1[7] 之间的联系。Yoda1 增强了骨细胞的低幅度高频振动以调节 MDA-MB-231 乳腺癌细胞迁移[8 ].
激动剂 Yoda1 可有效抑制高血压引起的钙内流。抗血栓研究证明，抑制 Piezo1 可有效抑制高血压小鼠的动脉血栓形成并减少卒中的梗死面积[6]。练习[3]。
| Cell experiment [1]: | |
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Cell lines |
Human coronary artery endothelial cells (HCAECs) |
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Preparation Method |
Human coronary endothelial cells (HCAEC) were treated with the indicated concentration of Yoda1 for 5 min. |
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Reaction Conditions |
1.5/3.0/6.0 µM for 5min |
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Applications |
Yoda1 induced the activation of Akt and ERK1/2, and the increase of their respective phosphorylation levels reflected that the phosphorylation of the two signaling molecules also increased with the increase of Yoda1 concentration. |
| Animal experiment [2]: | |
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Animal models |
Eight-week-old SPF male C57BL/6 mice |
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Preparation Method |
Hypertensive mice were injected with GSMTX-4, Yoda1 (Yod, 4 µg/kg/day) or LY294002 through tail vein for 3 days |
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Dosage form |
4 µg/kg/day Yoda1 for 3 days |
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Applications |
Agonist Yoda1 effectively inhibited calcium influx caused by hypertension. Antithrombotic studies proved that the inhibition of Piezo1 effectively inhibited arterial thrombosis and reduced the infarct size of stroke in hypertensive mice. |
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References: [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. |
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| Cas No. | 448947-81-7 | SDF | |
| 化学名 | 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 | ||
| 分子式 | C13H8Cl2N4S2 | 分子量 | 355.3 |
| 溶解度 | DMSO : 25 mg/mL (70.37 mM) | 储存条件 | Store 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 | 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 |
| 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
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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