Structure of Dooku1
CAS No.: 2253744-54-4
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Dooku1 is a reversible Yoda1 antagonist that effectively disrupts Yoda1-induced Piezo1 channel activity, making it potentially valuable in vascular physiology and related disease research.
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Batch number can be found on the product's label following the word 'Batch'.
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Batch number can be found on the product's label following the word 'Batch'.
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CAS No. : | 2253744-54-4 |
Formula : | C13H9Cl2N3OS |
M.W : | 326.20 |
SMILES Code : | ClC1=C(C(Cl)=CC=C1)CSC2=NN=C(C3=CC=CN3)O2 |
MDL No. : | MFCD32174346 |
InChI Key : | MNPOBXLPCWFONX-UHFFFAOYSA-N |
Pubchem ID : | 137321150 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P280-P301+P312-P302+P352-P305+P351+P338 |
Description |
Dooku1 acts as a reversible antagonist of Yoda1, with IC50 values of 1.3 μM and 1.5 μM for Yoda1-induced Ca2+ entry in HEK 293 cells and HUVECs at a Yoda1 concentration of 2 μM, respectively. It interferes with Yoda1-induced Piezo1 channel activity and inhibits Yoda1-induced relaxation of the aorta. Dooku1 is applicable for research in vascular physiology and disease[1].
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In Vitro:
Cell Line
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Concentration | Treated Time | Description | References |
BRIN-BD11 cells | 10 μM | 15 minutes | inhibited Yoda1-induced Ca2+ influx | Sci Rep. 2019 Nov 14;9(1):16876 |
INS-1 cells | 10 μM | 15 minutes | inhibited Yoda1-induced Ca2+ influx | Sci Rep. 2019 Nov 14;9(1):16876 |
HUVECs | 10 μM | 30 minutes | To test the inhibitory effect of Dooku1 on endogenous Piezo1 channels in HUVECs, results showed that Dooku1 inhibited Yoda1-induced Ca2+ entry | Br J Pharmacol. 2018 May;175(10):1744-1759 |
MLO-Y4 cells | 40 μM | 30 minutes | Dooku1 inhibited fluid flow shear stress (FFSS)-induced intracellular Ca2+ signaling and Cx43 hemichannels activation | Cell Biosci. 2022 Dec 1;12(1):191 |
human red blood cells | 1 µM to 100 µM | immediately observed | Study the dose-dependent effect of Dooku1, found that Dooku1 has a direct dose-dependent effect in the range of 1-10 µM, triggering calcium entry and activating the Gárdos channel. | Front Physiol. 2023 Jul 10;14:1222983 |
human red blood cells | 10 µM | 15 minutes | Investigate the inhibitory effect of Dooku1 on Yoda1-induced effects, found that Dooku1 itself can trigger calcium entry and activate the Gárdos channel. | Front Physiol. 2023 Jul 10;14:1222983 |
human eosinophil cell line AML14.3D10 | 10 µM | 3 minutes | Inhibited Yoda1-induced Piezo1 activity, significantly reducing Ca2+ elevation | Biomolecules. 2024 Sep 14;14(9):1157 |
Human aortic smooth muscle cells (HAoSMC) | 5 μmol/L | 7 days | Dooku1 inhibited Yoda1-induced calcification in HAoSMCs, reducing calcium deposition in the extracellular matrix. | Front Physiol. 2022 Nov 10;13:1037230 |
HEK 293 cells | 10 μM | 30 minutes | To test the inhibitory effect of Dooku1 on Yoda1-induced Piezo1 channel activity, results showed that Dooku1 effectively inhibited Yoda1-induced Ca2+ entry | Br J Pharmacol. 2018 May;175(10):1744-1759 |
In Vivo:
Species
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Animal Model
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Administration | Dosage | Frequency | Description | References |
C57BL/6 mice | Mouse thoracic aorta rings | In vitro culture | 10 μM | Single administration, lasting 20 minutes | To test the inhibitory effect of Dooku1 on Yoda1-induced aortic relaxation, results showed that Dooku1 effectively inhibited Yoda1-induced aortic relaxation | Br J Pharmacol. 2018 May;175(10):1744-1759 |
Sprague Dawley rats | Thoracic aorta rings | Tissue bath | 10 μM | 1-hour incubation | Dooku1 caused direct contraction in thoracic aorta rings without PVAT but did not alter PE-induced contraction. | Pharmacol Res. 2022 Jan;175:105995 |
C57BL/6 mice | Intracerebral hemorrhage model | Intraperitoneal injection | 5, 10, and 20 mg/kg | Four administrations at 0.5, 12, 24, and 48 hours post-operation | Dooku1 significantly alleviated brain edema, myelin sheath loss, and degeneration in injured tissue, substantially reduced oligodendrocyte apoptosis, and significantly improved neurological function. Additionally, Dooku1-mediated Piezo1 suppression reduced intracellular endoplasmic reticulum stress and cell apoptosis through the PERK-ATF4-CHOP and inositol-requiring enzyme 1 signaling pathway. | Neural Regen Res. 2023 Aug;18(8):1750-1756 |
C57BL/6J mice | Tibial compression model | Intraperitoneal injection | 5 mg/kg | Single injection, 4 hours before mechanical loading | Dooku1 inhibited mechanical loading-induced opening of Cx43 hemichannels | Cell Biosci. 2022 Dec 1;12(1):191 |
Mice | Murine neocortex | In vitro administration | 10 µM and 20 µM | Dooku1 significantly reduced the SIC frequency and activity induced by Yoda1, and when applied alone, it significantly decreased the rise time of SICs. | Int J Mol Sci. 2024 Apr 3;25(7):3994 |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
3.07mL 0.61mL 0.31mL |
15.33mL 3.07mL 1.53mL |
30.66mL 6.13mL 3.07mL |
Tags: Dooku1 | Dooku 1 | Dooku-1 | Piezo Channel | vascular physiology | inhibitor | 2253744-54-4 |
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