| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
IC50: 8.6 nM (Gαi1) and 166 nM (β-arrestin-2)[1]
Apelin receptor (APJ, also known as APLNR). Elabela(19-32) binds to APJ as a potent agonist (Ki = 0.93 nM), making it a key activator of this GPCR involved in cardiovascular development and function. |
|---|---|
| ln Vitro |
The radioligand apelin-13 [Glp65, Nle75 with Ki of 0.93 nM >, tyrosine 77][125I][1] is bound by Elabela (19-32) (analogue 3). When HA-hAPJ receptor is transiently expressed in HEK293 cells, Elabela (19-32) exhibits an EC50 of 36 nM. Apelin-13 and ELA are slightly more effective than Elabela (19-32) at starting receptor internalization [1]. With an EC50 of 1.5 pM, Elabela (19-32) (0.001 to 0.3 nM) alters left ventricular developed pressure (LVDP) in isolated rat hearts that are perfused with Langendorff [1].
Elabela(19-32) is an APJ agonist with high potency. It activates Galphai1 and beta-arrestin-2 signaling pathways with EC50 values of 8.6 nM and 166 nM, respectively. It also induces receptor internalization, demonstrating its ability to trigger full GPCR signaling cascades. |
| ln Vivo |
Rat plasma quickly metabolizes Elabela (19-32) (analog 3) (t1/2<2 minutes) [1].
In vivo, Elabela(19-32) reduces arterial pressure in rat hearts and produces positive inotropic effects, increasing the force of heart contraction. These effects confirm its role as a cardiovascular modulator and its potential relevance in conditions like pulmonary hypertension and heart failure. |
| Enzyme Assay |
A cell-free binding assay is performed using membranes from cells overexpressing human APJ. Membranes are incubated with [125I]Elabela(19-32) and varying concentrations of unlabeled Elabela(19-32). After incubation, bound and free ligands are separated by filtration, and radioactivity is measured to calculate the Ki (0.93 nM) for receptor binding.
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| Cell Assay |
HEK293 cells stably expressing human APJ are seeded in 96-well plates. For Galphai1 activation, cells are co-transfected with a SRE-luciferase reporter; EC50 is measured as 8.6 nM. For beta-arrestin-2 recruitment, a PathHunter beta-arrestin assay is used; EC50 is measured as 166 nM. Assays determine potency in activating different downstream pathways.
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| Animal Protocol |
Male Sprague-Dawley rats are anesthetized and instrumented for hemodynamic monitoring (arterial pressure, heart rate). Elabela(19-32) is administered intravenously as a bolus or infusion. Changes in mean arterial pressure (MAP) and cardiac contractility (dP/dt max) are recorded to assess its cardiovascular effects.
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| ADME/Pharmacokinetics |
Not reported. As a peptide agonist, Elabela(19-32) is expected to have a short plasma half-life due to proteolytic degradation and rapid renal clearance, which may limit its in vivo duration of action without chemical modification.
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| Toxicity/Toxicokinetics |
Not reported. As a research peptide not intended for clinical use, formal toxicology data is unavailable. As an endogenous peptide fragment, Elabela(19-32) is expected to have minimal toxicity, but high doses could cause hypotension or other cardiovascular side effects due to APJ activation.
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| References | |
| Additional Infomation |
Elabela(19-32) is derived from ELABELA, which is the second endogenous ligand for the APJ receptor alongside apelin. It is a critical tool for studying APJ signaling in cardiovascular biology. The fragment (19-32) represents the minimal bioactive sequence required for full receptor activation, making it a valuable probe for structure-activity relationship (SAR) studies and drug discovery targeting the apelinergic system.
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| Molecular Formula |
C75H119N25O17S2
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|---|---|
| Molecular Weight |
1707.03467202187
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| Exact Mass |
1705.865
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| CAS # |
1886973-05-2
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| Related CAS # |
Elabela(19-32) TFA
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| PubChem CID |
127043902
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| Appearance |
White to off-white solid powder
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| LogP |
-3.6
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| Hydrogen Bond Donor Count |
21
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| Hydrogen Bond Acceptor Count |
23
|
| Rotatable Bond Count |
48
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| Heavy Atom Count |
119
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| Complexity |
3580
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| Defined Atom Stereocenter Count |
14
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| SMILES |
S(C)CC[C@@H](C(N1CCC[C@H]1C(N[C@H](C(N[C@H](C(N[C@@H](CO)C(N[C@@H](CCC/N=C(\N)/N)C(N[C@@H](C(C)C)C(N1CCC[C@H]1C(N[C@@H](CC1C=CC=CC=1)C(N1CCC[C@H]1C(=O)O)=O)=O)=O)=O)=O)=O)CC1=CN=CN1)=O)CC(C)C)=O)=O)NC([C@H](CS)NC([C@H](CCC/N=C(\N)/N)NC([C@H](CCC/N=C(\N)/N)NC([C@@H]1CCC(N1)=O)=O)=O)=O)=O
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| InChi Key |
LKYSPGTYQNANFL-GYVBEWGNSA-N
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| InChi Code |
InChI=1S/C75H119N25O17S2/c1-40(2)33-49(93-67(111)54-20-12-29-98(54)69(113)48(25-32-119-5)91-66(110)53(38-118)96-60(104)45(18-10-27-84-74(78)79)88-59(103)44(17-9-26-83-73(76)77)89-61(105)47-23-24-57(102)87-47)63(107)92-50(35-43-36-82-39-86-43)64(108)95-52(37-101)65(109)90-46(19-11-28-85-75(80)81)62(106)97-58(41(3)4)71(115)99-30-13-21-55(99)68(112)94-51(34-42-15-7-6-8-16-42)70(114)100-31-14-22-56(100)72(116)117/h6-8,15-16,36,39-41,44-56,58,101,118H,9-14,17-35,37-38H2,1-5H3,(H,82,86)(H,87,102)(H,88,103)(H,89,105)(H,90,109)(H,91,110)(H,92,107)(H,93,111)(H,94,112)(H,95,108)(H,96,104)(H,97,106)(H,116,117)(H4,76,77,83)(H4,78,79,84)(H4,80,81,85)/t44-,45-,46-,47-,48-,49-,50-,51-,52-,53-,54-,55-,56-,58-/m0/s1
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| Chemical Name |
(2S)-1-[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2R)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-5-(diaminomethylideneamino)-2-[[(2S)-5-oxopyrrolidine-2-carbonyl]amino]pentanoyl]amino]pentanoyl]amino]-3-sulfanylpropanoyl]amino]-4-methylsulfanylbutanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]pentanoyl]amino]-3-methylbutanoyl]pyrrolidine-2-carbonyl]amino]-3-phenylpropanoyl]pyrrolidine-2-carboxylic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: 100 mg/mL (58.58 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (29.29 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.5858 mL | 2.9290 mL | 5.8581 mL | |
| 5 mM | 0.1172 mL | 0.5858 mL | 1.1716 mL | |
| 10 mM | 0.0586 mL | 0.2929 mL | 0.5858 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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