| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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Dooku1, an analog of Yoda1, is a novel, potent and selective antagonist of the endogenous Piezo1 channel. Dooku1 inhibited 2 μM Yoda1-induced Ca2+-entry with IC50 of 1.3 μM (in HEK 293 cells) and 1.5 μM (in HUVECs). Dooku1 inhibits Yoda1-induced relaxation of aorta. Yoda 1 is a novel and potent agonist of Piezo1 which is the mechanotransduction channel. Yoda 1 activates purified Piezo1 channels. Yoda1 works by eliciting Ca2+ flux in Piezo1- but not vector-transfected cells.
| ln Vitro |
In HEK 293 and CHO cells, Dooku1 (10 μM, 300 seconds) exhibits selectivity for Piezo1 channels [1]. In Piezo1 T-REx cells, Dooku1 (10 μM, 140 seconds) had no influence on constitutive Piezo1 channel activity [1]. In HEK 293 and Piezo1 T-REx cells, Dooku1 (10 μM, 40–60 seconds) blocks endogenous Yoda1-activated channels [1].
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| ln Vivo |
Dooku1 (10 μM arterial relaxation for 20 min) blockade decreases Yoda1-induced aortic relaxation in wild-type C57BL/6 mice [1].
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| Cell Assay |
Cell viability assay [1]
Cell Types: HUVECs, Piezo1 T-REx Cell Tested Concentrations: 10 μM Incubation Duration: 40-60 s Experimental Results: It has a concentration-dependent inhibitory effect on Yoda1-induced Ca2+ entry into HUVEC, with an IC50 of 1.49 μM. Potency was enhanced in HUVEC with an EC50 of 0.23 μM and in Piezo1 T-REx cells with an EC50 of 2.51 μM. |
| Animal Protocol |
Animal/Disease Models: Wild-type male C57BL/6 mouse aortic ring [1]
Doses: 10 μM Route of Administration: 20 minutes Experimental Results: Inhibition of Yoda1-induced relaxation. |
| References |
| Molecular Formula |
C13H9CL2N3OS
|
|---|---|
| Molecular Weight |
326.201059103012
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| Exact Mass |
324.984
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| CAS # |
2253744-54-4
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| PubChem CID |
137321150
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| Appearance |
White to off-white solid powder
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| LogP |
3.8
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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 |
4
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| Heavy Atom Count |
20
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| Complexity |
316
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
ClC1C=CC=C(C=1CSC1=NN=C(C2=CC=CN2)O1)Cl
|
| InChi Key |
MNPOBXLPCWFONX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H9Cl2N3OS/c14-9-3-1-4-10(15)8(9)7-20-13-18-17-12(19-13)11-5-2-6-16-11/h1-6,16H,7H2
|
| Chemical Name |
2-[(2,6-dichlorophenyl)methylsulfanyl]-5-(1H-pyrrol-2-yl)-1,3,4-oxadiazole
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| Synonyms |
Dooku1 Dooku-1 Dooku 1
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~100 mg/mL (~306.56 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0656 mL | 15.3280 mL | 30.6560 mL | |
| 5 mM | 0.6131 mL | 3.0656 mL | 6.1312 mL | |
| 10 mM | 0.3066 mL | 1.5328 mL | 3.0656 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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