1. Membrane Transporter/Ion Channel
  2. Piezo Channel
  3. Dooku1

Dooku1 is a reversibly Yoda1 antagonist with IC50 value of 1.3 μM and 1.5 μM for 2 μM Yoda1-induced Ca2+ entry HEK 293 cells and HUVECs, respectively. Dooku1 can disrupt Yoda1-induced Piezo1 channel activity and inhibit Yoda1-induced relaxation of aorta. Dooku1 can be used for vascular physiology and disease research.

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Dooku1 Chemical Structure

Dooku1 Chemical Structure

CAS No. : 2253744-54-4

Size Prix Stock Quantité
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 121 En stock
Solution
10 mM * 1 mL in DMSO USD 121 En stock
Solid
5 mg USD 110 En stock
10 mg USD 176 En stock
25 mg USD 352 En stock
50 mg USD 649 En stock
100 mg USD 1155 En stock
200 mg   Obtenir un devis  
500 mg   Obtenir un devis  

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Based on 5 publication(s) in Google Scholar

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  • Activité biologique

  • Pureté et documentation

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Description

Dooku1 is a reversibly Yoda1 antagonist with IC50 value of 1.3 μM and 1.5 μM for 2 μM Yoda1-induced Ca2+ entry HEK 293 cells and HUVECs, respectively. Dooku1 can disrupt Yoda1-induced Piezo1 channel activity and inhibit Yoda1-induced relaxation of aorta. Dooku1 can be used for vascular physiology and disease research[1].

In Vitro

Dooku1 (10 μM, 300 s) has selectivity for Piezo1 channels in HEK 293 and CHO cells.[1].
Dooku1 (10 μM, 140 s) has no effect on constitutive Piezo1 channel activity in Piezo1 T-REx cells[1].
Dooku1 (10 μM, 40-60 s) inhibits endogenous Yoda1-activated channels in HUVECs and Piezo1 T-REx cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: HUVECs, Piezo1 T-REx cells
Concentration: 10 μM
Incubation Time: 40-60 s
Result: Had a concentration-dependent inhibitory effect against Yoda1-induced Ca2+ entry in HUVECs, acting with an IC50 of 1.49 μM.
Increased potency in HUVECs with an EC50 of 0.23 μM, compared with 2.51 μM in Piezo1 T-REx cells.
In Vivo

Dooku1 (10 μM incubate 20 min) selectively inhibits Yoda1-induced relaxation of aorta of wild-type male C57BL/6 mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: wild-type male C57BL/6 mice’s aortic rings[1]
Dosage: 10 μM
Administration: 20 min
Result: Suppressed the Yoda1-induced relaxation.
Masse moléculaire

326.20

Formule

C13H9Cl2N3OS

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=C(C(Cl)=CC=C1)CSC2=NN=C(C3=CC=CN3)O2

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Solvant et solubilité
In Vitro: 

DMSO : 100 mg/mL (306.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Calculateur de molarité

  • Calculateur de dilution

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (6.38 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation

Purity: 99.89%

Références

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0656 mL 15.3280 mL 30.6560 mL 76.6401 mL
5 mM 0.6131 mL 3.0656 mL 6.1312 mL 15.3280 mL
10 mM 0.3066 mL 1.5328 mL 3.0656 mL 7.6640 mL
15 mM 0.2044 mL 1.0219 mL 2.0437 mL 5.1093 mL
20 mM 0.1533 mL 0.7664 mL 1.5328 mL 3.8320 mL
25 mM 0.1226 mL 0.6131 mL 1.2262 mL 3.0656 mL
30 mM 0.1022 mL 0.5109 mL 1.0219 mL 2.5547 mL
40 mM 0.0766 mL 0.3832 mL 0.7664 mL 1.9160 mL
50 mM 0.0613 mL 0.3066 mL 0.6131 mL 1.5328 mL
60 mM 0.0511 mL 0.2555 mL 0.5109 mL 1.2773 mL
80 mM 0.0383 mL 0.1916 mL 0.3832 mL 0.9580 mL
100 mM 0.0307 mL 0.1533 mL 0.3066 mL 0.7664 mL
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Dooku1 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Dooku1
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