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[Pyr1]-Apelin-13

[Pyr1]-Apelin-13

Catalog No. BCC7358
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1mg $186.00 Ship Within 7 Days
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Quality Control of [Pyr1]-Apelin-13

Chemical structure

[Pyr1]-Apelin-13

[Pyr1]-Apelin-13 Dilution Calculator

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Chemical Properties of [Pyr1]-Apelin-13

Cas No. 217082-60-5 SDF Download SDF
Synonyms [pGlu1]-Apelin-13
Sequence XRPRLSHKGPMPF

(Modifications: X = Glp)

Chemical Name (2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-1-[2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-1-[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-5-oxopyrrolidine-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]hexanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-4-methylsulfanylbutanoyl]pyrrolidine-2-carbonyl]amino]-3-phenylpropanoic acid
SMILES CC(C)CC(C(=O)NC(CO)C(=O)NC(CC1=CN=CN1)C(=O)NC(CCCCN)C(=O)NCC(=O)N2CCCC2C(=O)NC(CCSC)C(=O)N3CCCC3C(=O)NC(CC4=CC=CC=C4)C(=O)O)NC(=O)C(CCCN=C(N)N)NC(=O)C5CCCN5C(=O)C(CCCN=C(N)N)NC(=O)C6CCC(=O)N6
Standard InChIKey GGMAXEWLXWJGSF-PEWBXTNBSA-N
Standard InChI InChI=1S/C69H108N22O16S/c1-39(2)32-47(85-57(96)43(17-9-26-76-68(71)72)82-63(102)52-20-12-29-90(52)65(104)45(18-10-27-77-69(73)74)83-58(97)44-22-23-54(93)80-44)59(98)88-50(37-92)61(100)86-48(34-41-35-75-38-79-41)60(99)81-42(16-7-8-25-70)56(95)78-36-55(94)89-28-11-19-51(89)62(101)84-46(24-31-108-3)66(105)91-30-13-21-53(91)64(103)87-49(67(106)107)33-40-14-5-4-6-15-40/h4-6,14-15,35,38-39,42-53,92H,7-13,16-34,36-37,70H2,1-3H3,(H,75,79)(H,78,95)(H,80,93)(H,81,99)(H,82,102)(H,83,97)(H,84,101)(H,85,96)(H,86,100)(H,87,103)(H,88,98)(H,106,107)(H4,71,72,76)(H4,73,74,77)/t42-,43-,44-,45-,46-,47-,48-,49-,50-,51-,52-,53-/m0/s1
Formula C69H108N22O16S M.Wt 1533.81
Solubility Soluble to 1 mg/ml in water
Storage Desiccate at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other courier with RT , or blue ice upon request.

Preparing Stock Solutions of [Pyr1]-Apelin-13

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 0.652 mL 3.2599 mL 6.5197 mL 13.0394 mL 16.2993 mL
5 mM 0.1304 mL 0.652 mL 1.3039 mL 2.6079 mL 3.2599 mL
10 mM 0.0652 mL 0.326 mL 0.652 mL 1.3039 mL 1.6299 mL
50 mM 0.013 mL 0.0652 mL 0.1304 mL 0.2608 mL 0.326 mL
100 mM 0.0065 mL 0.0326 mL 0.0652 mL 0.1304 mL 0.163 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

References on [Pyr1]-Apelin-13

[Pyr1]Apelin-13(1-12) Is a Biologically Active ACE2 Metabolite of the Endogenous Cardiovascular Peptide [Pyr1]Apelin-13.[Pubmed: 28293165]


Aims: Apelin is a predicted substrate for ACE2, a novel therapeutic target. Our aim was to demonstrate the endogenous presence of the putative ACE2 product [Pyr1]apelin-13(1-12) in human cardiovascular tissues and to confirm it retains significant biological activity for the apelin receptor in vitro and in vivo. The minimum active apelin fragment was also investigated. Methods and Results: [Pyr1]apelin-13 incubated with recombinant human ACE2 resulted in de novo generation of [Pyr1]apelin-13(1-12) identified by mass spectrometry. Endogenous [Pyr1]apelin-13(1-12) was detected by immunostaining in human heart and lung localized to the endothelium. Expression was undetectable in lung from patients with pulmonary arterial hypertension. In human heart [Pyr1]apelin-13(1-12) (pKi = 8.04 ± 0.06) and apelin-13(F13A) (pKi = 8.07 ± 0.24) competed with [125I]apelin-13 binding with nanomolar affinity, 4-fold lower than for [Pyr1]apelin-13 (pKi = 8.83 ± 0.06) whereas apelin-17 exhibited highest affinity (pKi = 9.63 ± 0.17). The rank order of potency of peptides to inhibit forskolin-stimulated cAMP was apelin-17 (pD2 = 10.31 ± 0.28) > [Pyr1]apelin-13 (pD2 = 9.67 ± 0.04) ≥ apelin-13(F13A) (pD2 = 9.54 ± 0.05) > [Pyr1]apelin-13(1-12) (pD2 = 9.30 ± 0.06). The truncated peptide apelin-13(R10M) retained nanomolar potency (pD2 = 8.70 ± 0.04) but shorter fragments exhibited low micromolar potency. In a β-arrestin recruitment assay the rank order of potency was apelin-17 (pD2 = 10.26 ± 0.09) >> [Pyr1]apelin-13 (pD2 = 8.43 ± 0.08) > apelin-13(R10M) (pD2 = 8.26 ± 0.17) > apelin-13(F13A) (pD2 = 7.98 ± 0.04) ≥ [Pyr1]apelin-13(1-12) (pD2 = 7.84 ± 0.06) >> shorter fragments (pD2 < 6). [Pyr1]apelin-13(1-12) and apelin-13(F13A) contracted human saphenous vein with similar sub-nanomolar potencies and [Pyr1]apelin-13(1-12) was a potent inotrope in paced mouse right ventricle and human atria. [Pyr1]apelin-13(1-12) elicited a dose-dependent decrease in blood pressure in anesthetized rat and dose-dependent increase in forearm blood flow in human volunteers. Conclusions: We provide evidence that ACE2 cleaves [Pyr1]apelin-13 to [Pyr1]apelin-13(1-12) and this cleavage product is expressed in human cardiovascular tissues. We have demonstrated biological activity of [Pyr1]apelin-13(1-12) at the human and rodent apelin receptor in vitro and in vivo. Our data show that reported enhanced ACE2 activity in cardiovascular disease should not significantly compromise the beneficial effects of apelin based therapies for example in PAH.

Vasopressin V1a receptors mediate the hypertensive effects of [Pyr1 ]apelin-13 in the rat rostral ventrolateral medulla.[Pubmed: 28255983]


Apelin is a ubiquitous peptide that can elevate arterial blood pressure (ABP) yet understanding of the mechanisms involved remain incomplete. Bilateral microinjection of [Pyr1 ]apelin-13 into the rostral ventrolateral medulla (RVLM), a major source of sympathoexcitatory neurones, increases ABP and sympathetic nerve activity. We sought to investigate the potential involvement of neurotransmitter systems through which the apelin pressor response may occur within the RVLM. Adult male Wistar rats were anaesthetised and ABP was monitored via a femoral arterial catheter. Bilateral RVLM microinjection of [Pyr1 ]apelin-13 significantly increased ABP (9 ± 1 mmHg) compared to saline (-1 ± 2mmHg; P < 0.001) which was blocked by pretreatment with the apelin receptor antagonist, F13A (0 ± 1 mmHg; P < 0.01). The rise in ABP was associated with an increase in the low frequency spectra of systolic BP (LFSBP) (13.9 ± 4.3% total power; P < 0.001), indicative of sympathetic vasomotor activation. The [Pyr1 ]apelin-13-mediated pressor response and the increased LFSBP response were fully maintained despite RVLM pretreatment with the angiotensin (ANG) II type 1 receptor (AT1) antagonist losartan, the oxytocin (OT) receptor antagonist dOVT, the ionotropic glutamate receptor antagonist kynurenate or the GABAA antagonist bicuculline (P > 0.05). In contrast, the [Pyr1 ]apelin-13 induced pressor and sympathoexcitatory effects were abolished by pretreatment of the RVLM with the vasopressin (VP) V1a receptor antagonist, SR 49059 (-1 ± 1 mmHg; 1.1 ± 1.1% total power respectively; P < 0.001). These findings suggest that the pressor action of [Pyr1 ]apelin-13 in the RVLM of normotensive rats is not mediated via AT1, OT, ionotropic glutamate or GABAA receptors but involves a close relationship with the neuropeptide modulator VP. This article is protected by copyright. All rights reserved.

Post-infarct treatment with [Pyr1]apelin-13 exerts anti-remodeling and anti-apoptotic effects in rats heart.[Pubmed: 28181211]


Ischemic heart disease (IHD) is the main cause of mortality in the world. After myocardial infarction (MI) cardiomyocytes apoptosis and ventricular remodeling have been occurred. Apelin is a peptide that has been shown to exert cardioprotective effects.

[Effects of (Pyr1)apelin-13 on the proliferation and activation of Jarkat T lymphocyte].[Pubmed: 27916097]


Objective To investigate the effect of (Pyr1)apelin-13 on the proliferation and activation of Jurkat T lymphocytes. Methods Jurkat T cells were treated by 0, 10, 50 nmol/L (Pyr1)apelin-13 for 24 hours and cell proliferation ability was detected by CCK-8 assay. The effect of (Pyr1)apelin-13 on the activation of Jurkat T lymphocytes with anti-CD3 and anti-CD28 antibodies was observed and the molecular mechanism was investigated. Quantitative real-time PCR was applied to detect the expressions of CD69, CD25, cytotoxic T lymphocyte antigen-4 (CTLA-4) and programmed death-1 (PD-1) mRNAs. Results The proliferation of Jurkat T cells was not affected by (Pyr1) apelin-13. However, (Pyr1)apelin-13 increased the expressions of CD69 and CD25 and then activated Jurkat T lymphocytes. Furthermore, the expressions of CTLA-4 and PD-1 had no difference between activation group and (Pyr1)apelin-13 group. Conclusion (Pyr1)apelin-13 promotes Jurkat T lymphocyte activation by increasing the expressions of CD69 and CD25.

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