| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Adrenomedullin receptor and CGRP (calcitonin gene-related peptide) receptor. Adrenomedullin (AM) (22-52), human is an NH2-terminal truncated adrenomedullin analogue that acts as an adrenomedullin receptor antagonist. It also antagonizes the calcitonin gene-related peptide (CGRP) receptor in the hindlimb vascular bed of the cat. The peptide competitively inhibits the binding of adrenomedullin in a dose-dependent manner.
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| ln Vitro |
Adrenomedullin (AM) (22-52), Humans have no influence on the hindlimb perfusion pressure response to 120 nmol adrenomedullin (ADM). However, human adrenomedullin (AM) (22-52) at 30 nmol specifically and reversibly decreases the vasodilatory response to human calcitonin gene-related peptide (hCGRP) with effects similar to those of CGRP antagonists [1]. Human adrenomedullin (AM) (22-52) competitively inhibits adrenomedullin binding in a dose-dependent manner and decreases adrenomedullin-induced cAMP buildup in rat vascular smooth muscle cells [1].
In vitro, Adrenomedullin (AM) (22-52), human shows no effect on hindlimb perfusion pressure responses to adrenomedullin (ADM) at 120 nmol. However, it selectively and reversibly decreases vasodilator responses to human calcitonin gene-related peptide (hCGRP) at 30 nmol, with a similar effect to that of a CGRP antagonist. The peptide competitively inhibits the binding of adrenomedullin in a dose-dependent manner and inhibits adrenomedullin-induced cAMP accumulation in rat vascular smooth muscle cells. |
| ln Vivo |
In vivo, Adrenomedullin (AM) (22-52), human has been studied in animal models to characterize its antagonist effects. In the cat hindlimb vascular bed, the peptide antagonizes vasodilator responses to CGRP but not to adrenomedullin. It has been reported that 30 nmol of the peptide can selectively and reversibly decrease vasodilator responses to human CGRP. The compound is used as a research tool to study the physiological roles of adrenomedullin and CGRP in cardiovascular regulation.
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| Enzyme Assay |
In vitro receptor binding assays for Adrenomedullin (AM) (22-52), human measure its affinity for adrenomedullin and CGRP receptors. The assay uses membrane preparations from cells expressing recombinant adrenomedullin or CGRP receptors and a radiolabeled ligand. Varying concentrations of the peptide are incubated with membranes and radioligand. Non-specific binding is determined in the presence of excess unlabeled ligand. After incubation, bound and free radioligands are separated by filtration, and radioactivity is counted. IC50 and Ki values are calculated from competition curves using nonlinear regression analysis.
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| Cell Assay |
In vitro cell-based assays for Adrenomedullin (AM) (22-52), human use rat vascular smooth muscle cells or cells expressing adrenomedullin receptors. Cells are seeded in multi-well plates and pre-incubated with varying concentrations of the peptide antagonist for 30-60 minutes, followed by stimulation with a fixed concentration of adrenomedullin. Functional readouts include cAMP accumulation measured by ELISA or HTRF. Antagonist potency is expressed as IC50 or pKB values. The reversible nature of the antagonist allows for washout experiments to confirm competitive binding kinetics.
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| Animal Protocol |
In vivo animal studies with Adrenomedullin (AM) (22-52), human are commonly conducted in cat or rat models. A typical protocol involves intravenous administration of the peptide at doses ranging from 10-120 nmol, followed by assessment of hemodynamic parameters such as hindlimb perfusion pressure. Vasodilator responses to adrenomedullin and CGRP are measured before and after peptide administration. Blood pressure, heart rate, and vascular resistance are monitored at various time points post-administration.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Adrenomedullin (AM) (22-52), human are characteristic of peptide antagonists. With a molecular weight of 3575.98 and a 31-amino-acid sequence, the peptide is susceptible to proteolytic degradation and has a short half-life in biological fluids. It is soluble in DMSO (100 mg/mL) and water (50 mg/mL). The peptide is typically stored as a powder at -80degC for up to 2 years or at -20degC for up to 1 year. In solution, it should be stored at -80degC for up to 6 months or at -20degC for up to 1 month.
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| Toxicity/Toxicokinetics |
Adrenomedullin (AM) (22-52), human is intended for research use only and is not for human therapeutic use. As a peptide antagonist, it is generally well-tolerated at pharmacological doses in animal studies. Standard safety precautions for handling peptides apply. The compound is not approved for clinical use.
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| References |
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| Additional Infomation |
Adrenomedullin (AM) (22-52), human is a research-grade peptide antagonist of adrenomedullin and CGRP receptors. It is an NH2-terminal truncated adrenomedullin analogue with the sequence TVQKLAHQIYQFTDKDKDNVAPRSKISPQGY-NH2. The peptide has a molecular formula of C159H252N46O48 and a molecular weight of 3575.98. It is used as a research tool to study the physiological roles of adrenomedullin and CGRP in cardiovascular regulation. Not approved for clinical use.
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| Molecular Formula |
C121H193N33O31S
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|---|---|
| Molecular Weight |
2638.09464621544
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| Exact Mass |
2637.429
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| CAS # |
159899-65-7
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| Related CAS # |
Adrenomedullin (AM) (22-52), human TFA
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| PubChem CID |
44208916
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| Appearance |
White to off-white solid powder
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| LogP |
-5.6
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| Hydrogen Bond Donor Count |
40
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| Hydrogen Bond Acceptor Count |
38
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| Rotatable Bond Count |
90
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| Heavy Atom Count |
186
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| Complexity |
5620
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C)CC[C@@H](C(N[C@@H](C)C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@@H](C)C(N[C@@H](C)C(N[C@H](C(N[C@H](C(N)=O)CC(C)C)=O)C(C)C)=O)=O)=O)CC(C)C)=O)CC1C=CC(=CC=1)O)=O)CCCCN)=O)CCCCN)=O)C(C)C)=O)=O)NC([C@H](CCC(N)=O)NC([C@H](CCCCN)NC([C@H](CCCNC(=N)N)NC([C@H](CC1C=CC(=CC=1)O)NC([C@H](CCCNC(=N)N)NC([C@H](CO)NC([C@H](CC1C=CC(=CC=1)O)NC([C@H](CO)NC([C@H](CC(=O)O)NC([C@H]([C@@H](C)O)NC([C@H](CC1C=CC=CC=1)N)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O
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| InChi Key |
MMCDBQGTKNYEHP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C121H193N33O31S/c1-62(2)53-85(98(127)164)144-118(184)96(65(7)8)153-100(166)67(10)134-99(165)66(9)136-110(176)86(54-63(3)4)145-112(178)88(57-72-34-40-75(159)41-35-72)147-107(173)79(28-18-21-48-123)138-105(171)80(29-19-22-49-124)143-117(183)95(64(5)6)152-101(167)68(11)135-103(169)84(46-52-186-13)142-109(175)83(44-45-93(126)161)141-104(170)78(27-17-20-47-122)137-106(172)81(30-23-50-132-120(128)129)139-111(177)87(56-71-32-38-74(158)39-33-71)146-108(174)82(31-24-51-133-121(130)131)140-115(181)91(60-155)150-113(179)89(58-73-36-42-76(160)43-37-73)148-116(182)92(61-156)151-114(180)90(59-94(162)163)149-119(185)97(69(12)157)154-102(168)77(125)55-70-25-15-14-16-26-70/h14-16,25-26,32-43,62-69,77-92,95-97,155-160H,17-24,27-31,44-61,122-125H2,1-13H3,(H2,126,161)(H2,127,164)(H,134,165)(H,135,169)(H,136,176)(H,137,172)(H,138,171)(H,139,177)(H,140,181)(H,141,170)(H,142,175)(H,143,183)(H,144,184)(H,145,178)(H,146,174)(H,147,173)(H,148,182)(H,149,185)(H,150,179)(H,151,180)(H,152,167)(H,153,166)(H,154,168)(H,162,163)(H4,128,129,132)(H4,130,131,133)
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| Chemical Name |
4-[[1-[[1-[[1-[[1-[[1-[[1-[[6-amino-1-[[5-amino-1-[[1-[[1-[[1-[[6-amino-1-[[6-amino-1-[[1-[[1-[[1-[[1-[[1-[(1-amino-4-methyl-1-oxopentan-2-yl)amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-[[2-[(2-amino-3-phenylpropanoyl)amino]-3-hydroxybutanoyl]amino]-4-oxobutanoic 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) |
DMSO : ~100 mg/mL (~27.96 mM)
H2O : ~50 mg/mL (~13.98 mM) |
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.3791 mL | 1.8953 mL | 3.7906 mL | |
| 5 mM | 0.0758 mL | 0.3791 mL | 0.7581 mL | |
| 10 mM | 0.0379 mL | 0.1895 mL | 0.3791 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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