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| Targets |
HAEGTFTSDVS targets the GLP-1 receptor (GLP-1R), a G protein-coupled receptor that mediates the effects of GLP-1. As the N-terminal fragment of GLP-1, this peptide contains the region critical for receptor binding and activation. The full-length GLP-1 (7-36) amide promotes insulin secretion from pancreatic beta cells in a glucose-dependent manner and inhibits glucagon secretion from alpha cells. HAEGTFTSDVS is used to study the structure-activity relationships of GLP-1 and its interaction with the GLP-1 receptor.
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| ln Vitro |
In response to food intake, intestinal L cells secrete GLP-1 (7-36) amide, which is the result of the proglucagon gene. By promoting insulin secretion from pancreatic beta cells in a glucose-dependent manner, GLP-1 has a variety of effects (insulinotropic effect). GLP-1 suppresses alpha cell secretion, which lowers the amounts of circulating plasma glucagon. In addition, GLP-1 has the ability to promote insulin sensitivity, suppress appetite, delay stomach emptying, and promote beta cell growth [1]. GLP-1 peptide analogues function as agonists of the glucagon-like peptide 1 receptor [2].
In vitro studies have characterized HAEGTFTSDVS as the N-terminal fragment of GLP-1. The peptide is used to study the interaction of GLP-1 with its receptor and to understand the structural requirements for GLP-1 activity. As a fragment of the incretin hormone, it is relevant to the study of glucose metabolism and pancreatic function. The peptide's ability to bind to the GLP-1 receptor and activate downstream signaling pathways has been investigated in various assay systems. |
| ln Vivo |
In vivo studies of HAEGTFTSDVS are limited, as the peptide is primarily used as a research tool for in vitro studies. As a fragment of GLP-1, it could potentially have effects on glucose metabolism and insulin secretion in vivo, but its shorter sequence may result in reduced potency and rapid degradation. The peptide is not intended for therapeutic use. Its utility is in understanding the structure-function relationships of GLP-1 and its receptor.
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| Enzyme Assay |
The in vitro binding assay for HAEGTFTSDVS involves measuring the interaction of the peptide with the GLP-1 receptor. Competitive binding studies are performed using membrane preparations from cells expressing the GLP-1 receptor and a radiolabeled or fluorescently labeled GLP-1 ligand. Varying concentrations of HAEGTFTSDVS are incubated with the receptor and the labeled ligand. The displacement of the ligand is measured, and binding affinity is determined. Alternatively, functional assays measuring cAMP accumulation in response to peptide treatment can be performed to assess receptor activation.
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| Cell Assay |
In vitro cellular assays for HAEGTFTSDVS are conducted using cells expressing the GLP-1 receptor, such as pancreatic beta-cell lines (e.g., INS-1, MIN6) or transfected HEK293 cells. Cells are treated with varying concentrations of HAEGTFTSDVS. Receptor activation is assessed by measuring cAMP accumulation using ELISA or HTRF assays. The peptide's ability to stimulate insulin secretion can be measured in insulin-secreting cell lines. The potency of the peptide is compared to full-length GLP-1 to assess the contribution of the N-terminal region to receptor activation. All experiments are performed in triplicate with appropriate controls.
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| Animal Protocol |
In vivo animal studies for HAEGTFTSDVS are not extensively reported. As a GLP-1 fragment, it could be evaluated in animal models of diabetes for its effects on glucose tolerance and insulin secretion. Typical study designs would involve administration of the peptide via intravenous or intraperitoneal routes in mice or rats, followed by glucose tolerance tests. However, specific published in vivo protocols for HAEGTFTSDVS are not available in the provided sources. The compound is primarily used as an in vitro research tool.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for HAEGTFTSDVS are not applicable as the compound is a peptide research tool rather than a therapeutic candidate. The peptide has a molecular weight of approximately 1150.18 g/mol and a molecular formula of C48H71N13O20. As a peptide, it would be susceptible to rapid proteolytic degradation and would have poor oral bioavailability. It is not intended for in vivo administration in pharmacokinetic studies. For in vitro use, it is typically dissolved in aqueous buffers. The compound is for research use only.
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| Toxicity/Toxicokinetics |
Toxicology data for HAEGTFTSDVS are not applicable as the compound is a peptide research tool. The peptide is not administered to animals or humans for therapeutic purposes. Standard safety precautions for handling peptides should be followed. No specific toxicity data are available. The compound is for research use only and is not intended for human therapeutic applications.
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| References |
[1]. US20120264685
[2]. US9738697 |
| Additional Infomation |
HAEGTFTSDVS is a synthetic peptide corresponding to the first N-terminal 1-11 residues of glucagon-like peptide-1 (GLP-1). The sequence is His-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser. It has a molecular weight of approximately 1150.18 g/mol and a molecular formula of C48H71N13O20. GLP-1 is an incretin hormone that promotes insulin secretion and regulates glucose metabolism. HAEGTFTSDVS is used as a research tool for studying GLP-1 biology and receptor interactions.
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| Molecular Formula |
C48H71N13O20
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|---|---|
| Molecular Weight |
1150.15245175362
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| Exact Mass |
1149.493
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| CAS # |
864915-61-7
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| PubChem CID |
168013604
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
-8.3
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| Hydrogen Bond Donor Count |
19
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| Hydrogen Bond Acceptor Count |
22
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| Rotatable Bond Count |
35
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| Heavy Atom Count |
81
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| Complexity |
2220
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| Defined Atom Stereocenter Count |
12
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| SMILES |
C[C@H]([C@@H](C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CO)C(=O)O)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CC2=CN=CN2)N)O
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| InChi Key |
DVFFCJRYQFXVGO-QZDJTBDFSA-N
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| InChi Code |
InChI=1S/C48H71N13O20/c1-21(2)36(45(77)58-32(19-63)48(80)81)60-43(75)30(15-35(69)70)55-44(76)31(18-62)57-47(79)38(24(5)65)61-42(74)29(13-25-9-7-6-8-10-25)56-46(78)37(23(4)64)59-33(66)17-51-41(73)28(11-12-34(67)68)54-39(71)22(3)53-40(72)27(49)14-26-16-50-20-52-26/h6-10,16,20-24,27-32,36-38,62-65H,11-15,17-19,49H2,1-5H3,(H,50,52)(H,51,73)(H,53,72)(H,54,71)(H,55,76)(H,56,78)(H,57,79)(H,58,77)(H,59,66)(H,60,75)(H,61,74)(H,67,68)(H,69,70)(H,80,81)/t22-,23+,24+,27-,28-,29-,30-,31-,32-,36-,37-,38-/m0/s1
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| Chemical Name |
(4S)-4-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]propanoyl]amino]-5-[[2-[[(2S,3R)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-3-carboxy-1-[[(2S)-1-[[(1S)-1-carboxy-2-hydroxyethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-5-oxopentanoic 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 Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 0.8695 mL | 4.3473 mL | 8.6945 mL | |
| 5 mM | 0.1739 mL | 0.8695 mL | 1.7389 mL | |
| 10 mM | 0.0869 mL | 0.4347 mL | 0.8695 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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