1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. Piezo Channel Calcium Channel
  3. Yoda2

Yoda2 (KC289), the potassium salt of Yoda1 (HY-18723), is a PIEZO1 agonist with an EC50 of 150 nM. Yoda2 evokes Ca2+ elevation and NO-dependent relaxation. Yoda2 induces relaxation in mouse arterial and cavernous tissues. Yoda2 inhibits glucocorticoid-induced osteoclast formation and bone resorptive activity, reverses glucocorticoid-induced bone density loss and architectural deterioration, and does not induce medication-related osteonecrosis of the jaw in mice. Yoda2 can be used for the researches of hypertension and osteoporosis.

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Yoda2

Yoda2 Chemical Structure

CAS No. : 3081450-95-2

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Description

Yoda2 (KC289), the potassium salt of Yoda1 (HY-18723), is a PIEZO1 agonist with an EC50 of 150 nM. Yoda2 evokes Ca2+ elevation and NO-dependent relaxation. Yoda2 induces relaxation in mouse arterial and cavernous tissues. Yoda2 inhibits glucocorticoid-induced osteoclast formation and bone resorptive activity, reverses glucocorticoid-induced bone density loss and architectural deterioration, and does not induce medication-related osteonecrosis of the jaw in mice. Yoda2 can be used for the researches of hypertension and osteoporosis[1][2][3].

IC50 & Target[1]

PIEZO1

150 nM (EC50)

In Vitro

Yoda2 (5 µM; 7 days) significantly inhibits Dexamethasone (HY-14648)-induced osteoclast formation and bone resorptive activity in mouse bone marrow-derived mononuclear cells[2].
Yoda2 (0.01-30 μM) acts as a potent agonist of endogenous human PIEZO1 in HUVECs, with an EC50 of 0.15 μM and producing more consistent concentration-dependent intracellular calcium elevations than Yoda1 (HY-18723)[3].
Yoda2 (5 μM) demonstrates high selectivity for PIEZO1 over a panel of 30 other membrane proteins, with only modest binding to adenosine A2a and prostanoid EP4 receptors at 5 μM[3].
Yoda2 can cause concentration-dependent and NO-dependent relaxation in mouse portal vein (EC50 = 1.14 μM)[3].

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

In Vivo

Yoda2 (0.4 mg/kg; s.c.; twice weekly) protects against systemic and periodontal bone loss in a mouse model of Dexamethasone (HY-14648)-induced osteoporosis by activating Piezo1 in myeloid-lineage cells, without promoting medication-related osteonecrosis of the jaw[2].

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

Animal Model: C57BL/6 wild-type (WT) (3-week-old male); Piezo1flox/flox (3-week-old male); LysM-cre/Piezo1flox/flox (Piezo1LysMD) (3-week-old male)[2]
Dosage: 0.4 mg/kg
Administration: s.c.; twice weekly
Result: Reversed significant reductions in bone mineral density and deterioration of bone architecture caused by dexamethasone in WT mice.
Preserved protective effects in Piezo1flox/flox mice but showed no protective effects in Piezo1LysMD mice.
Did not induce medication-related osteonecrosis of the jaw following tooth extraction.
Molecular Weight

435.39

Formula

C16H9Cl2KN2O2S2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O[K])C1=CC=C(C2=NN=C(SCC3=C(Cl)C=CC=C3Cl)S2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (114.84 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 2.2968 mL 11.4840 mL 22.9679 mL
5 mM 0.4594 mL 2.2968 mL 4.5936 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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: ≥ 2.5 mg/mL (5.74 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

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Please enter your animal formula composition:
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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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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.
Purity & Documentation
References

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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2968 mL 11.4840 mL 22.9679 mL 57.4198 mL
5 mM 0.4594 mL 2.2968 mL 4.5936 mL 11.4840 mL
10 mM 0.2297 mL 1.1484 mL 2.2968 mL 5.7420 mL
15 mM 0.1531 mL 0.7656 mL 1.5312 mL 3.8280 mL
20 mM 0.1148 mL 0.5742 mL 1.1484 mL 2.8710 mL
25 mM 0.0919 mL 0.4594 mL 0.9187 mL 2.2968 mL
30 mM 0.0766 mL 0.3828 mL 0.7656 mL 1.9140 mL
40 mM 0.0574 mL 0.2871 mL 0.5742 mL 1.4355 mL
50 mM 0.0459 mL 0.2297 mL 0.4594 mL 1.1484 mL
60 mM 0.0383 mL 0.1914 mL 0.3828 mL 0.9570 mL
80 mM 0.0287 mL 0.1435 mL 0.2871 mL 0.7177 mL
100 mM 0.0230 mL 0.1148 mL 0.2297 mL 0.5742 mL
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Help & FAQs
  • 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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Yoda2
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