[Pyr1]-Apelin-13 (Synonyms: [pGlu1]-Apelin-13)

Name: [Pyr1]-Apelin-13
Brand: MedChemExpress
SKU: HY-P1033
Rating: 4.5 (1 reviews)

Cat. No.: HY-P1033 Purity: 99.92%: FAQs
Data Sheet SDS COA Handling Instructions Technical Support

[Pyr1]-Apelin-13 is a highly potent, selective endogenous apelin receptor (APJ) agonist.

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

Custom Peptide Synthesis

[Pyr1]-Apelin-13 Chemical Structure

CAS No. : 217082-60-5

Size	Stock	Quantity
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	Get quote
100 mg	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of [Pyr1]-Apelin-13:

[Pyr1]-Apelin-13, Gly(15N) TFA Get quote
[Pyr1]-Apelin-13, Pro(¹³C₅,¹⁵N) TFA Get quote

1 Publications Citing Use of MCE [Pyr1]-Apelin-13

•Research Square Print. 2023 Jan 23.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity
Purity & Documentation
References
Customer Review

Description

[Pyr1]-Apelin-13 is a highly potent, selective endogenous apelin receptor (APJ) agonist.

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	0.0003 μM Compound: Pyr-Apelin-13	Agonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay Agonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay	[PMID: 31948845]
CHO	EC₅₀	0.002 μM Compound: Pyr-Apelin-13	Agonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assay Agonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assay	[PMID: 31948845]
CHO-K1	EC₅₀	0.001 μM Compound: Pyr-Apelin-13	Agonist activity at human APJ receptor stably expressed in CHOK1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay Agonist activity at human APJ receptor stably expressed in CHOK1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay	[PMID: 31948845]
HEK293	EC₅₀	0.047 nM Compound: 1; (Pyr1)apelin-13	Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay	[PMID: 31724863]
HEK293	EC₅₀	0.062 nM Compound: 1; (Pyr1)apelin-13	Agonist activity at rat APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay Agonist activity at rat APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay	[PMID: 31724863]
HEK293	EC₅₀	0.84 nM Compound: Ape13	Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of Galphai1 subunit dissociation incubated for 5 mins by BRET assay Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of Galphai1 subunit dissociation incubated for 5 mins by BRET assay	[PMID: 25668242]
HEK293	EC₅₀	1.1 nM Compound: Ape13	Activity at human APJ receptor expressed in HEK293 cells assessed as dissociation of Galphai1 from Gbetagamma subunit after 5 mins by BRET assay Activity at human APJ receptor expressed in HEK293 cells assessed as dissociation of Galphai1 from Gbetagamma subunit after 5 mins by BRET assay	[PMID: 29461833]
HEK293	IC₅₀	1.2 nM Compound: Ape13	Displacement of [125I]apelin-13[Glp65,Nle75,Tyr77] from YFP epitope-tagged human APJ receptor expressed in HEK293 cell membranes incubated for 1 hr by gamma counting method Displacement of [125I]apelin-13[Glp65,Nle75,Tyr77] from YFP epitope-tagged human APJ receptor expressed in HEK293 cell membranes incubated for 1 hr by gamma counting method	[PMID: 25668242]
HEK293	EC₅₀	1.4 nM Compound: Ape13	Agonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assay Agonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assay	[PMID: 25668242]
HEK293	EC₅₀	12.2 pM Compound: [pyr1]-apelin-13	Agonist activity at APJ receptor in HEK293 cells assessed as inhibition of forskolin-induced cAMP level incubated for 5 mins prior to forskolin challenge measured after 30 mins by TR-FRET assay Agonist activity at APJ receptor in HEK293 cells assessed as inhibition of forskolin-induced cAMP level incubated for 5 mins prior to forskolin challenge measured after 30 mins by TR-FRET assay	[PMID: 25241924]
HEK293	EC₅₀	24 nM Compound: Ape13	Induction of human HA-tagged APJ receptor internalization expressed in HEK293 cells after 30 mins by ELISA Induction of human HA-tagged APJ receptor internalization expressed in HEK293 cells after 30 mins by ELISA	[PMID: 29461833]
HEK293	EC₅₀	26 nM Compound: Ape13	Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of beta-arrestin-1 recruitment subunit dissociation incubated for 30 mins by BRET assay Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of beta-arrestin-1 recruitment subunit dissociation incubated for 30 mins by BRET assay	[PMID: 25668242]
HEK293	EC₅₀	29 nM Compound: Ape13	Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of beta-arrestin-2 recruitment subunit dissociation incubated for 30 mins by BRET assay Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of beta-arrestin-2 recruitment subunit dissociation incubated for 30 mins by BRET assay	[PMID: 25668242]
HEK293	EC₅₀	5.9 nM Compound: Ape13	Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of GalphaoA subunit dissociation incubated for 5 mins by BRET assay Agonist activity at human APJ receptor expressed in HEK293 cells assessed as induction of GalphaoA subunit dissociation incubated for 5 mins by BRET assay	[PMID: 25668242]
HEK293	EC₅₀	60 nM Compound: Ape13	Activity at GFP10-tagged human APJ receptor expressed in HEK293 cells assessed as induction of RlucII-tagged beta-arrestin-2 recruitment after 30 mins by BRET assay Activity at GFP10-tagged human APJ receptor expressed in HEK293 cells assessed as induction of RlucII-tagged beta-arrestin-2 recruitment after 30 mins by BRET assay	[PMID: 29461833]

In Vitro

[Pyr1]-apelin-13 encapsulation in lipoPEG particles (lipoPEG-PA13) results in sustained and extended drug release under physiological conditions^[1].

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

In Vivo

[Pyr1]-apelin-13 nanocarriers in a mouse model of pressure-overload induced heart failure demonstrate a sustainable long-term effect of [Pyr1]-apelin-13 in preventing cardiac dysfunction^[1]. [Pyr1] apelin-13 (1, 5 μg) improves locomotor activity and reduces pain symptoms, cavity size and caspase-3 levels in rats. [Pyr1] apelin-13 (1, 5 μg) significantly increases thermal paw withdrawal latency. [Pyr1] apelin-13 in 5 μg dose also produces significant attenuation in paw withdrawal threshold compared to SCI animals from the second week post SCI^[2].

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

Molecular Weight

1533.80

Formula

C₆₉H₁₀₈N₂₂O₁₆S

CAS No.

217082-60-5

Appearance

Solid

Color

White to off-white

Sequence Shortening

{Glp}-RPRLSHKGPMPF

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture

Powder	-80°C	2 years
	-20°C	1 year

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

Solvent & Solubility

In Vitro:

H₂O : 100 mg/mL (65.20 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	0.6520 mL	3.2599 mL	6.5198 mL
5 mM	0.1304 mL	0.6520 mL	1.3040 mL
10 mM	0.0652 mL	0.3260 mL	0.6520 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 100 mg/mL (65.20 mM); Clear solution; Need ultrasonic

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

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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).

Purity & Documentation

Purity: 99.92%

Select Batch:

Data Sheet (276 KB) SDS (394 KB)

COA (252 KB) LCMS (86 KB)

Handling Instructions (2659 KB)

References

[1]. Serpooshan V, et al. [Pyr1]-Apelin-13 delivery via nano-liposomal encapsulation attenuates pressure overload-induced cardiac dysfunction. Biomaterials. 2015 Jan;37:289-98. [Content Brief]

[2]. Hajimashhadi Z, et al. Chronic administration of [Pyr1] apelin-13 attenuates neuropathic pain after compression spinal cord injury in rats. Neuropeptides. 2017 Feb;61:15-22. [Content Brief]

Complete Stock Solution Preparation Table

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

H₂O	1 mM	0.6520 mL	3.2599 mL	6.5198 mL	16.2994 mL
	5 mM	0.1304 mL	0.6520 mL	1.3040 mL	3.2599 mL
	10 mM	0.0652 mL	0.3260 mL	0.6520 mL	1.6299 mL
	15 mM	0.0435 mL	0.2173 mL	0.4347 mL	1.0866 mL
	20 mM	0.0326 mL	0.1630 mL	0.3260 mL	0.8150 mL
	25 mM	0.0261 mL	0.1304 mL	0.2608 mL	0.6520 mL
	30 mM	0.0217 mL	0.1087 mL	0.2173 mL	0.5433 mL
	40 mM	0.0163 mL	0.0815 mL	0.1630 mL	0.4075 mL
	50 mM	0.0130 mL	0.0652 mL	0.1304 mL	0.3260 mL
	60 mM	0.0109 mL	0.0543 mL	0.1087 mL	0.2717 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

[Pyr1]-Apelin-13 Related Classifications

Cardiovascular Disease

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:

[Pyr1]-Apelin-13217082-60-5[pGlu1]-Apelin-13Apelin Receptor (APJ)Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

[Pyr1]-Apelin-13 (Synonyms: [pGlu1]-Apelin-13)

Customer Review

Other Forms of [Pyr1]-Apelin-13:

[Pyr1]-Apelin-13 Related Antibodies

1 Publications Citing Use of MCE [Pyr1]-Apelin-13

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

[Pyr1]-Apelin-13 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

[Pyr1]-Apelin-13 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report