| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
The primary target of Adrenomedullin (16-31), human is the CGRP1 receptor, for which adrenomedullin has appreciable affinity. The full-length adrenomedullin is a potent vasodilator, but this fragment, Adrenomedullin (16-31), exhibits different pharmacological properties. It has been shown to have vasopressor activity in the rat systemic vasculature. This suggests that the C-terminal region of adrenomedullin may interact with a distinct receptor or binding site that mediates different effects from the full-length peptide.
|
|---|---|
| ln Vitro |
In vitro, Adrenomedullin (16-31), human is the 16-31 fragment of the amino acid residues of human adrenomedullin. Adrenomedullin has appreciable affinity for the CGRP1 receptor. The fragment is used to study the structural features of adrenomedullin that are responsible for its biological activities. It is a valuable tool for mapping the receptor binding sites and understanding the pharmacological differences between the full-length peptide and its fragments.
|
| ln Vivo |
In vivo, Adrenomedullin (16-31), human has been shown to have vasopressor activity on the rat systemic vasculature. However, it has no effect on the cat systemic vasculature, indicating species-specific differences in its activity. This is in contrast to the full-length adrenomedullin, which is a potent vasodilator. The vasopressor activity of this fragment suggests that it may act as a partial agonist or antagonist at a specific receptor subtype.
|
| Enzyme Assay |
Cell-free receptor binding assays for Adrenomedullin (16-31), human typically use membrane preparations from cells expressing the CGRP1 receptor. A standard protocol involves incubating the membranes with a radiolabeled ligand, such as [125I]-adrenomedullin, and varying concentrations of the unlabeled peptide. Bound and free ligand are separated by filtration, and the radioactivity is measured. The binding affinity (IC50 or Ki) is determined from competitive displacement curves. This assay helps characterize the interaction of the fragment with the receptor.
|
| Cell Assay |
For in vitro cellular experiments, cells expressing the CGRP1 receptor (e.g., SK-N-MC cells) are cultured in appropriate media. Cells are treated with Adrenomedullin (16-31) at various concentrations (typically 1 nM to 10 uM). Receptor activation is assessed by measuring cAMP accumulation using ELISA or radioimmunoassay. The fragment's ability to stimulate or inhibit cAMP production is measured to determine its functional activity at the receptor. These experiments help define its pharmacology.
|
| Animal Protocol |
In vivo animal experiments with Adrenomedullin (16-31), human are conducted in rodent models, typically rats, to study its vasopressor effects. A common protocol involves anesthetizing the animal and monitoring blood pressure via a carotid artery catheter. The peptide is administered intravenously at various doses (e.g., 1-100 ug/kg). The change in mean arterial pressure is recorded. This allows for the assessment of its vasopressor activity and its comparison to the full-length peptide.
|
| ADME/Pharmacokinetics |
Adrenomedullin (16-31), human is a peptide with a molecular weight of 1865.19 g/mol and a molecular formula of C82H129N25O21S2. As a peptide, it is administered by injection in experimental settings. Its half-life in vivo is short due to proteolytic degradation. It is stable as a powder and should be stored at -20degC. It is soluble in aqueous buffers. Its pharmacokinetic properties are consistent with those of a peptide, characterized by rapid clearance.
|
| Toxicity/Toxicokinetics |
The toxicity profile of Adrenomedullin (16-31), human is not extensively characterized, as it is a research tool. At the doses used in experiments, it is generally well-tolerated. However, its vasopressor activity indicates that it can have significant effects on the cardiovascular system. The compound is for research use only and not for human therapeutic use. It should be handled with standard laboratory precautions.
|
| References | |
| Additional Infomation |
Adrenomedullin (16-31), human is a synthetic peptide fragment corresponding to amino acid residues 16-31 of human adrenomedullin. Adrenomedullin has appreciable affinity for the CGRP1 receptor. This fragment is used as a research tool to study the structure-activity relationships of adrenomedullin. It has been shown to have vasopressor activity in the rat but not in the cat. It is not approved for clinical use.
|
| Molecular Formula |
C82H129N25O21S2
|
|---|---|
| Molecular Weight |
1865.18657469749
|
| Exact Mass |
1863.923
|
| CAS # |
318480-38-5
|
| Related CAS # |
Adrenomedullin (16-31), human TFA
|
| PubChem CID |
131698084
|
| Appearance |
White to off-white solid powder
|
| Density |
1.5±0.1 g/cm3
|
| Index of Refraction |
1.674
|
| LogP |
-4.67
|
| Hydrogen Bond Donor Count |
27
|
| Hydrogen Bond Acceptor Count |
27
|
| Rotatable Bond Count |
49
|
| Heavy Atom Count |
130
|
| Complexity |
3810
|
| Defined Atom Stereocenter Count |
18
|
| SMILES |
CC[C@H](C)[C@@H](C(=O)N[C@@H](CC1=CC=C(C=C1)O)C(=O)N)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CC2=CNC=N2)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](C(C)C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H]3CSSC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N3)[C@@H](C)O)CC4=CC=CC=C4)CCCNC(=N)N)N
|
| InChi Key |
UYSITIBGEJGZGX-FXMFISEGSA-N
|
| InChi Code |
InChI=1S/C82H129N25O21S2/c1-10-42(6)64(79(126)99-55(67(87)114)32-47-21-23-49(110)24-22-47)106-74(121)54(26-28-61(86)112)97-76(123)58(34-48-35-90-39-93-48)100-68(115)43(7)94-75(122)56(31-40(2)3)101-71(118)51(19-14-15-29-83)96-73(120)53(25-27-60(85)111)98-78(125)63(41(4)5)105-81(128)66(45(9)109)107-77(124)59-38-130-129-37-50(84)69(116)95-52(20-16-30-91-82(88)89)72(119)102-57(33-46-17-12-11-13-18-46)70(117)92-36-62(113)104-65(44(8)108)80(127)103-59/h11-13,17-18,21-24,35,39-45,50-59,63-66,108-110H,10,14-16,19-20,25-34,36-38,83-84H2,1-9H3,(H2,85,111)(H2,86,112)(H2,87,114)(H,90,93)(H,92,117)(H,94,122)(H,95,116)(H,96,120)(H,97,123)(H,98,125)(H,99,126)(H,100,115)(H,101,118)(H,102,119)(H,103,127)(H,104,113)(H,105,128)(H,106,121)(H,107,124)(H4,88,89,91)/t42-,43-,44+,45+,50-,51-,52-,53-,54-,55-,56-,57-,58-,59-,63-,64-,65-,66-/m0/s1
|
| Chemical Name |
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(4R,7S,13S,16S,19R)-19-amino-13-benzyl-16-(3-carbamimidamidopropyl)-7-[(1R)-1-hydroxyethyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-hydroxybutanoyl]amino]-3-methylbutanoyl]amino]-5-oxopentanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-N-[(2S,3S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]pentanediamide
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
H2O : ~100 mg/mL (~53.61 mM)
|
|---|---|
| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.5361 mL | 2.6807 mL | 5.3614 mL | |
| 5 mM | 0.1072 mL | 0.5361 mL | 1.0723 mL | |
| 10 mM | 0.0536 mL | 0.2681 mL | 0.5361 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
