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

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

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YM-244769 hydrochloride Chemical Structure

YM-244769 hydrochloride Chemical Structure

CAS No. : 837424-39-2

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Based on 1 publication(s) in Google Scholar

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YM-244769 hydrochloride Related Antibodies

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Description

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

IC50 & Target

IC50: 18 nM (NCX3)[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 hydrochloride Related Antibodies
In Vivo

YM-244769 (0.1-1 mg/kg; p.o.; once) exhibits dose-dependently natriuretic action in mice and significantly increased 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

479.93

Formula

C26H23ClFN3O3
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.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (208.36 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 2.0836 mL 10.4182 mL 20.8364 mL
5 mM 0.4167 mL 2.0836 mL 4.1673 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. 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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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. 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 2.0836 mL 10.4182 mL 20.8364 mL 52.0909 mL
5 mM 0.4167 mL 2.0836 mL 4.1673 mL 10.4182 mL
10 mM 0.2084 mL 1.0418 mL 2.0836 mL 5.2091 mL
15 mM 0.1389 mL 0.6945 mL 1.3891 mL 3.4727 mL
20 mM 0.1042 mL 0.5209 mL 1.0418 mL 2.6045 mL
25 mM 0.0833 mL 0.4167 mL 0.8335 mL 2.0836 mL
30 mM 0.0695 mL 0.3473 mL 0.6945 mL 1.7364 mL
40 mM 0.0521 mL 0.2605 mL 0.5209 mL 1.3023 mL
50 mM 0.0417 mL 0.2084 mL 0.4167 mL 1.0418 mL
60 mM 0.0347 mL 0.1736 mL 0.3473 mL 0.8682 mL
80 mM 0.0260 mL 0.1302 mL 0.2605 mL 0.6511 mL
100 mM 0.0208 mL 0.1042 mL 0.2084 mL 0.5209 mL
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YM-244769 hydrochloride Related Classifications

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-244769837424-39-2YM244769YM 244769Na+/Ca2+ ExchangerSH-SY5Y cellsneuroprotectivenicotinamideLLC-PK1 cellsNa+/Ca2+ exchangeanti-ischemicNCX3Inhibitorinhibitorinhibit

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