| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
The primary target of Jedi2 is the mechanosensitive ion channel Piezo1. Jedi2 binds to the mouse Piezo1 proteins with a Kd of 2770 µM. It activates Piezo1 through interaction with extracellular regions of the peripheral blade-like domain. Piezo1 is a non-selective cation channel that mediates Ca2+ influx in response to mechanical stimuli. The compound shows selectivity for Piezo1 over Piezo2, as it does not induce responses in cells expressing Piezo2 channels.
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| ln Vitro |
Piezo1-mediated Ca2+ influx is caused by Jedi2. In mPiezo1-transfected cells, Jedi2 (200 μM) potential elicited quantifiable responses, but not in mPiezo2- or vector-transfected cells [1]. In mCherry HEK293T cells transfected with the mPiezo1-mCherry construct, Jedi2 (1 mM) dramatically increases Ca2+ levels; these cells are similarly responsive to Yoda1 (30 μM) [1].
In vitro, Jedi2 evokes Piezo1-mediated Ca2+ influx. The compound binds to mouse Piezo1 proteins with a Kd of 2770 µM. Jedi2 promotes the influx of calcium ions (Ca2+) into cells, and this activation has been demonstrated in HEK293 cells that express Piezo1 channels. Importantly, Jedi2's effect is selective for Piezo1 channels, as it induces responses in cells transfected with mouse Piezo1, but not in those expressing Piezo2 channels. |
| ln Vivo |
No specific in vivo activity data is publicly available for Jedi2. As a Piezo1 channel activator, it would be expected to modulate mechanosensitive signaling pathways in vivo. However, specific in vivo efficacy data from animal models is not detailed in the available sources. The compound is for research use only and not for therapeutic applications.
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| Enzyme Assay |
For Piezo1 channel activators, standard cell-free assays are not typically applicable as Piezo1 is a mechanosensitive ion channel that requires membrane environment for proper function. However, binding studies can be performed using purified Piezo1 protein or membrane preparations to measure binding affinity (Kd) using surface plasmon resonance (SPR) or other biophysical methods.
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| Cell Assay |
For Piezo1 channel activators, standard cellular assays involve the use of cells expressing recombinant Piezo1 channels (e.g., HEK293 cells transfected with mouse Piezo1). Cells are loaded with calcium-sensitive fluorescent dyes, and Ca2+ influx following compound addition is measured by fluorimetry or imaging. Jedi2 evokes Piezo1-mediated Ca2+ influx in these cells. Selectivity for Piezo1 over Piezo2 is assessed using cells expressing Piezo2 channels.
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| Animal Protocol |
No specific animal protocol is available for Jedi2. For in vivo evaluation of Piezo1 modulators, standard animal models include pain models, models of mechanotransduction, and models of vascular function. The compound is typically administered systemically, and physiological and behavioral endpoints are assessed.
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| ADME/Pharmacokinetics |
Jedi2 has a molecular weight of 208.23 and formula C10H8O3S. The IUPAC name is 2-Methyl-5-(2-thienyl)-3-furancarboxylic acid. It is soluble in DMSO. The compound should be stored dry, dark, and at 0-4°C for short term or -20°C for long term.
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| Toxicity/Toxicokinetics |
No detailed toxicology data is publicly available for Jedi2. As a research compound targeting Piezo1 channels, standard preclinical toxicology would be required for therapeutic development. The compound is for research use only and not for therapeutic applications.
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| References | |
| Additional Infomation |
2-Methyl-5-(2-thienyl)-3-furanoic acid is a type of furanoic acid.
Jedi2 is also known as 2-methyl-5-(thiophen-2-yl)furan-3-carboxylic acid. It is a synthetic small molecule classified as a chemical activator of the mechanosensitive Piezo1 ion channel. The compound has a purity of 98%. No regulatory approval for therapeutic use has been identified. |
| Molecular Formula |
C10H8O3S
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| Molecular Weight |
208.23372
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| Exact Mass |
208.019
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| CAS # |
651005-90-2
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| PubChem CID |
2796026
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| Appearance |
Light brown to brown solid powder
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| LogP |
3.014
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
14
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| Complexity |
231
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
YXDCRSXNEOKXDE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H8O3S/c1-6-7(10(11)12)5-8(13-6)9-3-2-4-14-9/h2-5H,1H3,(H,11,12)
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| Chemical Name |
2-methyl-5-thiophen-2-ylfuran-3-carboxylic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~240.12 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (12.01 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.8024 mL | 24.0119 mL | 48.0238 mL | |
| 5 mM | 0.9605 mL | 4.8024 mL | 9.6048 mL | |
| 10 mM | 0.4802 mL | 2.4012 mL | 4.8024 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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