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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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
Purity & Documentation
References
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YM-244769 hydrochloride Related Classifications

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

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