2. Membrane Transporter/Ion Channel
  3. Na+/Ca2+ Exchanger
  4. YM-244769

YM-244769 is a potent, selective and orally active Na+/Ca2+ exchanger (NCX) inhibitor. YM-244769 preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca2+ entry mode), with IC50s of 18 nM and 50 nM, respectively. YM-244769 efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 can also increase urine volume and urinary excretion of electrolytes in mice.

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YM-244769 Chemical Structure

YM-244769 Chemical Structure

CAS No. : 838819-70-8

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Based on 1 publication(s) in Google Scholar

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Description

YM-244769 is a potent, selective and orally active Na+/Ca2+ exchanger (NCX) inhibitor. YM-244769 preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca2+ entry mode), with IC50s of 18 nM and 50 nM, respectively. YM-244769 efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 can also increase urine volume and urinary excretion of electrolytes in mice[1][2][3].

IC50 & Target

IC50: 18 nM (NCX3), 68 nM (NCX1), 96 nM (NCX2)[1]
In Vitro

YM-244769 (0.003-1 μM) inhibits dose dependently the initial rates of 45Ca2+ uptake into NCX1, NCX2, and NCX3 transfectants with IC50 values of 68 ± 2.9, 96 ± 3.5, and 18 ± 1.0 nM, respectively[1].
YM-244769 (0.3 or 1 μM) efficiently protects against the hypoxia/reoxygenation-induced lactate dehydrogenase (LDH) release in SH-SY5Y cells and in LLC-PK1 cells (1 μM)[1].
YM-244769 possesses reverse mode-selectivity[1].
YM-244769 (1 and 10 μM) inhibits NCX current (INCX) in a concentration- and [Na+]i-dependent manner, the IC50 against the unidirectional outward INCX (Ca2+ entry mode) is 0.05 μM. The IC50 values against the bidirectional outward and inward INCX are similar and approximately 100 nM with a Hill coefficient of about 1[3].
YM-244769 is trypsin-insensitive[3].

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

YM-244769 Related Antibodies

Cell Viability Assay[1]

Cell Line: SH-SY5Y cells treated with NCX1 or NCX3 antisense
Concentration: 0.3 and 1 μM
Incubation Time:
Result: Hypoxia/reoxygenation-induced LDH release was significantly attenuated: reduction in cell damage was greater in cells treated with NCX3 antisense (by 61%) than in cells treated with NCX1 antisense (by 35%). 0.3 or 1 μM efficiently suppressed the hypoxia/reoxygenation-induced cell damage in SH-SY5Y cells treated with NCX1 antisense more than in those treated with NCX3 antisense.
In Vivo

YM-244769 (0.1-1 mg/kg; p.o.; once) exhibits dose-dependently natriuretic action in mice and significantly increases urinary excretion of Ca2+ as well as Ca2+/Cr ratio[2].

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

Animal Model: Wild-type C57BL/6J mice and NCX-KO mice[2]
Dosage: 0.1, 0.3 and 1 mg/kg
Administration: Oral administration, once
Result: Caused a dose-dependent increase (up to approximately 200%) in urine volume and urinary excretion of electrolytes (Na+, K+ and Cl-). Natriuretic actions were equivalently observed in NCX1-KO and WT, but disappeared in NCX2-KO and double KO.
Molecular Weight

443.47

Formula

C26H22FN3O3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=CN=C(C=C1)OC2=CC=C(C=C2)OCC3=CC(F)=CC=C3)NCC4=CC(N)=CC=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 120 mg/mL (270.59 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 2.2549 mL 11.2747 mL 22.5494 mL
5 mM 0.4510 mL 2.2549 mL 4.5099 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). 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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  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 2.08 mg/mL (4.69 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, 6 months; -20°C, 1 month (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.
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). 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 2.2549 mL 11.2747 mL 22.5494 mL 56.3736 mL
5 mM 0.4510 mL 2.2549 mL 4.5099 mL 11.2747 mL
10 mM 0.2255 mL 1.1275 mL 2.2549 mL 5.6374 mL
15 mM 0.1503 mL 0.7516 mL 1.5033 mL 3.7582 mL
20 mM 0.1127 mL 0.5637 mL 1.1275 mL 2.8187 mL
25 mM 0.0902 mL 0.4510 mL 0.9020 mL 2.2549 mL
30 mM 0.0752 mL 0.3758 mL 0.7516 mL 1.8791 mL
40 mM 0.0564 mL 0.2819 mL 0.5637 mL 1.4093 mL
50 mM 0.0451 mL 0.2255 mL 0.4510 mL 1.1275 mL
60 mM 0.0376 mL 0.1879 mL 0.3758 mL 0.9396 mL
80 mM 0.0282 mL 0.1409 mL 0.2819 mL 0.7047 mL
100 mM 0.0225 mL 0.1127 mL 0.2255 mL 0.5637 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.

Keywords:

YM-244769838819-70-8YM244769YM 244769Na+/Ca2+ ExchangerSH-SY5Y cellsneuroprotectivenicotinamideLLC-PK1 cellsNa+/Ca2+ exchangeanti-ischemicNCX3Inhibitorinhibitorinhibit

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