YM-244769 dihydrochloride

Name: YM-244769 dihydrochloride
Brand: MedChemExpress
SKU: HY-136182
Rating: 4.5 (1 reviews)

Cat. No.: HY-136182 Purity: 99.02%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

For research use only. We do not sell to patients.

YM-244769 dihydrochloride Chemical Structure

CAS No. : 1780390-65-9

Size	Price	Stock	Quantity
5 mg	USD 95	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 320	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 520	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 830	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of YM-244769 dihydrochloride:

YM-244769 hydrochloride Get quote
YM-244769 Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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 (I_NCX) in a concentration- and [Na⁺]_i-dependent manner, the IC₅₀ against the unidirectional outward I_NCX (Ca²⁺ entry mode) is 0.05 μM. The IC₅₀ values against the bidirectional outward and inward I_NCX 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.

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

516.39

Formula

C₂₆H₂₄Cl₂FN₃O₃

CAS No.

1780390-65-9

Appearance

Solid

Color

Off-white to pink

SMILES

O=C(C1=CC=C(OC2=CC=C(OCC3=CC=CC(F)=C3)C=C2)N=C1)NCC4=CC=CC(N)=C4.Cl.Cl

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 : 100 mg/mL (193.65 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	1.9365 mL	9.6826 mL	19.3652 mL
5 mM	0.3873 mL	1.9365 mL	3.8730 mL
10 mM	0.1937 mL	0.9683 mL	1.9365 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.03 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.03 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)

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

Purity: 99.02%

Select Batch:

Data Sheet (273 KB) SDS (251 KB)

COA (243 KB) HNMR (445 KB) RP-HPLC (235 KB) LCMS (82 KB)

Handling Instructions (2659 KB)

References

[1]. Takahiro Iwamoto , et al. YM-244769, a Novel Na⁺/Ca²⁺ Exchange Inhibitor That Preferentially Inhibits NCX3, Efficiently Protects Against hypoxia/reoxygenation-induced SH-SY5Y Neuronal Cell Damage. Mol Pharmacol. 2006 Dec;70(6):2075-83. [Content Brief]

[2]. Gotoh Y, et al. Genetic knockout and pharmacologic inhibition of NCX2 cause natriuresis and hypercalciuria. Biochem Biophys Res Commun. 2015 Jan 9;456(2):670-5. [Content Brief]

[3]. Yamashita K, et al. Inhibitory effect of YM-244769, a novel Na+/Ca2+ exchanger inhibitor on Na+/Ca2+ exchange current in guinea pig cardiac ventricular myocytes. Naunyn Schmiedebergs Arch Pharmacol. 2016 Nov;389(11):1205-1214. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9365 mL	9.6826 mL	19.3652 mL	48.4130 mL
	5 mM	0.3873 mL	1.9365 mL	3.8730 mL	9.6826 mL
	10 mM	0.1937 mL	0.9683 mL	1.9365 mL	4.8413 mL
	15 mM	0.1291 mL	0.6455 mL	1.2910 mL	3.2275 mL
	20 mM	0.0968 mL	0.4841 mL	0.9683 mL	2.4207 mL
	25 mM	0.0775 mL	0.3873 mL	0.7746 mL	1.9365 mL
	30 mM	0.0646 mL	0.3228 mL	0.6455 mL	1.6138 mL
	40 mM	0.0484 mL	0.2421 mL	0.4841 mL	1.2103 mL
	50 mM	0.0387 mL	0.1937 mL	0.3873 mL	0.9683 mL
	60 mM	0.0323 mL	0.1614 mL	0.3228 mL	0.8069 mL
	80 mM	0.0242 mL	0.1210 mL	0.2421 mL	0.6052 mL
	100 mM	0.0194 mL	0.0968 mL	0.1937 mL	0.4841 mL