SERCA2a activator 1

Name: SERCA2a activator 1
Brand: MedChemExpress
SKU: HY-124873
Rating: 4.5 (1 reviews)

Cat. No.: HY-124873 Purity: 99.54%: FAQs
Data Sheet SDS COA Handling Instructions

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SERCA2a activator 1 (Compound A) is a sarco/endoplasmic reticulum Ca²⁺-dependent ATPase 2a (SERCA2a) activator. SERCA2a activator 1 attenuates phospholamban inhibition and enhances the systolic and diastolic functions of the heart. SERCA2a activator 1 can be used for heart failure.

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

SERCA2a activator 1 Chemical Structure

CAS No. : 2139330-34-8

Size	Price	Stock	Quantity
1 mg	USD 371	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 780	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1250	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 2500	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 4000	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 6400	In-stock	Estimated Time of Arrival: December 31
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500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

SERCA2a^[1]

In Vitro

SERCA2a activator 1 (Compound A) activates the Ca²⁺-dependent ATPase activity of cardiac sarcoplasmic reticulum (SR) vesicles but not that of skeletal muscle SR vesicles that lack phospholamban (PLN). The surface plasmon resonance assay reveals a direct interaction between SERCA2a activator 1 and PLN, suggesting that the binding of SERCA2a activator 1 to PLN attenuates its inhibition of SERCA2a, resulting in SERCA2a activation^[1].
SERCA2a activator 1 also increases the Ca²⁺ transients and contraction and relaxation of isolated adult rat cardiomyocytes. In isolated perfused rat hearts, the SERCA2a activator 1 enhances systolic and diastolic functions^[1].

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

In Vivo

SERCA2a activator 1 (Compound A; 30mg/kg; intravenous injection; male Wistar rats) treatment significantly enhances the diastolic function in anesthetized normal rats^[1].

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

Animal Model:	Male Wistar rats (7-8 weeks old)^[1]
Dosage:	30mg/kg
Administration:	Intravenous injection
Result:	Significantly enhanced the diastolic function in anesthetized normal rats.

Molecular Weight

551.66

Formula

C₃₂H₂₉N₃O₄S

CAS No.

2139330-34-8

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC(C(C=C2CC3=CC=CC=C3)=CN(CCCC)C2=O)=NC=C1)NS(=O)(C4=CC=C5C=CC=CC5=C4)=O

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 : 62.5 mg/mL (113.29 mM; ultrasonic and warming and heat to 80°C; 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	1.8127 mL	9.0636 mL	18.1271 mL
5 mM	0.3625 mL	1.8127 mL	3.6254 mL
10 mM	0.1813 mL	0.9064 mL	1.8127 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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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

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.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.54%

Select Batch:

Data Sheet (272 KB) SDS (251 KB)

COA (247 KB) HNMR (301 KB) LCMS (265 KB)

Handling Instructions (2659 KB)

References

[1]. Kaneko M, et al. A pyridone derivative activates SERCA2a by attenuating the inhibitory effect of phospholamban. Eur J Pharmacol. 2017 Nov 5;814:1-8. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.8127 mL	9.0636 mL	18.1271 mL	45.3178 mL
	5 mM	0.3625 mL	1.8127 mL	3.6254 mL	9.0636 mL
	10 mM	0.1813 mL	0.9064 mL	1.8127 mL	4.5318 mL
	15 mM	0.1208 mL	0.6042 mL	1.2085 mL	3.0212 mL
	20 mM	0.0906 mL	0.4532 mL	0.9064 mL	2.2659 mL
	25 mM	0.0725 mL	0.3625 mL	0.7251 mL	1.8127 mL
	30 mM	0.0604 mL	0.3021 mL	0.6042 mL	1.5106 mL
	40 mM	0.0453 mL	0.2266 mL	0.4532 mL	1.1329 mL
	50 mM	0.0363 mL	0.1813 mL	0.3625 mL	0.9064 mL
	60 mM	0.0302 mL	0.1511 mL	0.3021 mL	0.7553 mL
	80 mM	0.0227 mL	0.1133 mL	0.2266 mL	0.5665 mL
	100 mM	0.0181 mL	0.0906 mL	0.1813 mL	0.4532 mL