| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Apelin receptor (APJ). ELA-21 (human) is a potent APJ agonist, activating both G protein-dependent (e.g., cAMP inhibition) and beta-arrestin-dependent signaling pathways. It binds with high affinity (pKi = 8.52) to APJ in human left ventricular tissue.
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|---|---|
| ln Vitro |
ELA-21 (human) is a potent APJ agonist. It completely inhibits forskolin-induced cAMP production (an indicator of Gi activation) and stimulates beta-arrestin recruitment at subnanomolar potencies. It binds to APJ receptors in left ventricle from normal and PAH hearts with pKi values of 9.31 and 9.46, respectively.
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| ln Vivo |
Not reported. As a high-affinity APJ agonist, ELA-21 is expected to have in vivo cardiovascular effects similar to other APJ agonists, such as vasodilation, increased cardiac contractility (positive inotropy), and regulation of fluid homeostasis. It is a bioactive fragment of ELA-32, which is known to be active in vivo.
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| Enzyme Assay |
A cell-free binding assay is conducted using membranes prepared from human left ventricular tissue (normal or from PAH patients). Membranes are incubated with [125I]apelin-13 or a labeled ELA peptide and varying concentrations of unlabeled ELA-21. Bound and free ligands are separated by filtration, and radioactivity is counted to calculate pKi values (9.31 and 9.46).
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| Cell Assay |
HEK293 cells expressing human APJ are seeded in 96-well plates. For G protein signaling, cells are stimulated with forskolin in the presence or absence of ELA-21, and cAMP levels are measured using HTRF. For beta-arrestin recruitment, a PathHunter beta-arrestin assay is used. EC50 values are calculated to assess the compound‘s potency in activating both pathways.
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| Animal Protocol |
In vivo studies are conducted in rodent models of pulmonary arterial hypertension (PAH). ELA-21 may be administered intravenously or via osmotic minipump. Hemodynamic parameters (e.g., right ventricular pressure) are measured, and cardiac function is assessed via echocardiography. Tissue samples are collected for histological and molecular analysis.
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| ADME/Pharmacokinetics |
Not reported. As a peptide agonist, ELA-21 is expected to have a short plasma half-life in vivo due to rapid proteolytic degradation. This is typical for unmodified peptide therapeutics and limits its duration of action, often requiring continuous infusion for sustained effects.
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| Toxicity/Toxicokinetics |
Not reported. No formal toxicology data is available as ELA-21 is a research-grade peptide not intended for clinical use. Given its mechanism as an APJ agonist, potential toxicity could include hypotension or cardiac arrhythmias due to excessive vasodilation or positive inotropy.
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| References | |
| Additional Infomation |
ELA-21 (human) is a 21-amino acid peptide derived from ELA-32, the endogenous APJ ligand. It represents a key bioactive fragment and is a crucial research tool for studying the apelinergic system, which is involved in cardiovascular development, fluid homeostasis, and angiogenesis. Unlike apelin, ELABELA-derived peptides often show distinct signaling bias and receptor internalization profiles, making them important for dissecting biased agonism at the APJ receptor.
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| Molecular Formula |
C112H184N40O25S3
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|---|---|
| Molecular Weight |
2587.14
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| Exact Mass |
2586.355
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| CAS # |
2245073-05-4
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| PubChem CID |
146018951
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| Appearance |
White to off-white solid powder
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| LogP |
-8
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| Hydrogen Bond Donor Count |
37
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| Hydrogen Bond Acceptor Count |
36
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| Rotatable Bond Count |
74
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| Heavy Atom Count |
180
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| Complexity |
5670
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| Defined Atom Stereocenter Count |
21
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| SMILES |
CC(C)C[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CSSC[C@@H](C(=O)N1)NC(=O)[C@H](CC(=O)N)NC(=O)[C@H](CC2=CNC=N2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)N)C(=O)N[C@@H](CCSC)C(=O)N3CCC[C@H]3C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC4=CNC=N4)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C(C)C)C(=O)N5CCC[C@H]5C(=O)N[C@@H](CC6=CC=CC=C6)C(=O)N7CCC[C@H]7C(=O)O)CCCNC(=N)N)CCCNC(=N)N)CCC(=O)N
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| InChi Key |
DITOSSSIQUUZEP-FMGZCOAKSA-N
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| InChi Code |
InChI=1S/C112H184N40O25S3/c1-58(2)44-65(114)88(156)133-67(25-15-36-127-109(117)118)89(157)134-66(24-13-14-35-113)91(159)141-75(48-63-51-125-56-131-63)97(165)143-77(50-86(116)155)99(167)148-81-55-180-179-54-80(147-92(160)69(27-17-38-129-111(121)122)135-90(158)68(26-16-37-128-110(119)120)136-93(161)71(32-33-85(115)154)138-95(163)73(45-59(3)4)140-102(81)170)101(169)139-72(34-43-178-9)105(173)150-40-19-29-82(150)103(171)144-74(46-60(5)6)96(164)142-76(49-64-52-126-57-132-64)98(166)146-79(53-153)100(168)137-70(28-18-39-130-112(123)124)94(162)149-87(61(7)8)107(175)151-41-20-30-83(151)104(172)145-78(47-62-22-11-10-12-23-62)106(174)152-42-21-31-84(152)108(176)177/h10-12,22-23,51-52,56-61,65-84,87,153H,13-21,24-50,53-55,113-114H2,1-9H3,(H2,115,154)(H2,116,155)(H,125,131)(H,126,132)(H,133,156)(H,134,157)(H,135,158)(H,136,161)(H,137,168)(H,138,163)(H,139,169)(H,140,170)(H,141,159)(H,142,164)(H,143,165)(H,144,171)(H,145,172)(H,146,166)(H,147,160)(H,148,167)(H,149,162)(H,176,177)(H4,117,118,127)(H4,119,120,128)(H4,121,122,129)(H4,123,124,130)/t65-,66-,67-,68-,69-,70-,71-,72-,73-,74-,75-,76-,77-,78-,79-,80-,81-,82-,83-,84-,87-/m0/s1
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| Chemical Name |
(2S)-1-[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(4R,7S,10S,13S,16S,19R)-19-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-4-oxobutanoyl]amino]-13-(3-amino-3-oxopropyl)-7,10-bis(3-carbamimidamidopropyl)-16-(2-methylpropyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-4-methylsulfanylbutanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-5-carbamimidamidopentanoyl]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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.3865 mL | 1.9326 mL | 3.8653 mL | |
| 5 mM | 0.0773 mL | 0.3865 mL | 0.7731 mL | |
| 10 mM | 0.0387 mL | 0.1933 mL | 0.3865 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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