Yoda1 |
Catalog No.GC18233 |
Yoda1 is an agonist for both human and mouse Piezo1.
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.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment [1]: | |
Cell lines |
Human coronary artery endothelial cells (HCAECs) |
Preparation Method |
Human coronary endothelial cells (HCAEC) were treated with the indicated concentration of Yoda1 for 5 min. |
Reaction Conditions |
1.5/3.0/6.0 µM for 5min |
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]: | |
Animal models |
Eight-week-old SPF male C57BL/6 mice |
Preparation Method |
Hypertensive mice were injected with GSMTX-4, Yoda1 (Yod, 4 µg/kg/day) or LY294002 through tail vein for 3 days |
Dosage form |
4 µg/kg/day Yoda1 for 3 days |
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. |
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. |
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.
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 |
Solubility | 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 | |||
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Average Rating: 5
(Based on Reviews and 16 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
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