| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Insulin receptor, GIP receptor (GIPR)
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| ln Vitro |
Chinese hamster lung fibroblasts transfected with human GIP receptors produce cyclic adenosine 3'5' monophosphate (cAMP) in response to acetyl Gastric Inhibitory Peptide (human) TFA, with an EC50 value of 1.9 nM [1]. Acetyl Gastric Inhibitory Peptide (human) TFA (10-13-10-8 nM) exhibits a potent effect in increasing insulin release when compared to natural GIP [1]. Beta cell glucose insensitivity, insulin resistance, glucose intolerance, type 2 diabetes, and decreased insulin production can all be improved with acetyl gastric inhibitory peptide (human) TFA [2]. Acetyl Gastric Inhibitory Peptide (human) TFA has been studied both in vitro and in vivo [3]. It possesses the hypoglycemic, insulin-modulating, and metabolic stability of two fatty acid-derived N-terminally acetylated GIP analogues.
Acetyl Gastric Inhibitory Peptide (human) TFA acts as a GIP receptor agonist. In vitro studies show that it stimulates cAMP production in Chinese hamster lung fibroblasts expressing the human GIP receptor, with an EC50 value of 1.9 nM. It also exhibits a potent effect on increasing insulin release compared to native GIP. |
| ln Vivo |
The human version of Acetyl Gastric Inhibitory Peptide (TFA) (25 nmol/kg; i.p. ; single dosage) is more bioactive and has better antidiabetic potential in vivo because it is resistant to degradation by plasma dipeptidyl peptidase IV [1].
In vivo, this acetylated GIP analog has improved antidiabetic potential. At 25 nmol/kg (i.p., single dose), it effectively lowers blood glucose levels. Its enhanced bioactivity is due to its resistance to degradation by plasma dipeptidyl peptidase IV (DPP-IV). It is used in diabetes, insulin resistance, and obesity research. |
| Enzyme Assay |
In a receptor binding assay, the compound is first dissolved in assay buffer. CHO-K1 cells stably expressing the human GIP receptor are homogenized to prepare membrane fractions. These membranes are then incubated with a radiolabeled GIP tracer (e.g., [125I]-GIP) and increasing concentrations of the test compound. After incubation, the mixture is filtered, and the bound radioactivity is measured. The Ki or IC50 values are calculated from the competition curves.
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| Cell Assay |
For the cell-based cAMP assay, CHO-K1 cells expressing the human GIP receptor are seeded into a 96-well plate and grown to confluence. The cells are then treated with various concentrations of Acetyl Gastric Inhibitory Peptide (human) TFA for 30 minutes at 37degC. The cells are then lysed, and the amount of cAMP is quantified using a specific ELISA or HTRF kit. The EC50 value is calculated from the dose-response curve.
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| Animal Protocol |
In an animal experiment, male Wistar rats are fasted overnight and then administered the test compound at a dose of 25 nmol/kg via intraperitoneal injection. Blood samples are collected from the tail vein at various time points (e.g., 0, 15, 30, 60, 90, 120 minutes). Plasma glucose levels are measured using a glucose meter or an enzymatic assay kit. The area under the curve (AUC) for glucose is calculated to assess the compound's antihyperglycemic effect.
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| ADME/Pharmacokinetics |
Peptide-based therapeutics, such as this GIP analog, generally have a short half-life due to rapid renal clearance and enzymatic degradation. The acetylation and fatty acid derivatization in this analog are specifically designed to improve metabolic stability. Resistance to DPP-IV degradation extends its in vivo half-life, allowing for once-daily or less frequent dosing.
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| Toxicity/Toxicokinetics |
No specific toxicology data is available for this research compound. Given its mechanism as an incretin mimetic, potential long-term toxicities could be similar to other GLP-1 receptor agonists, including gastrointestinal disturbances (nausea, vomiting) and a potential risk of pancreatitis. This product is for research purposes only.
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| References |
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| Additional Infomation |
Fatty acid derivatization is a common strategy to prolong the action of peptide drugs by promoting albumin binding. This approach is clinically used in GLP-1 analogs like liraglutide (Victoza®). Acetyl Gastric Inhibitory Peptide (human) TFA is a research tool to study the potential of GIP analogs for treating diabetes and obesity. It is not approved for clinical use.
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| Molecular Formula |
C228H340N60O67S.C2HF3O2
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|---|---|
| Molecular Weight |
5139.62
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| Related CAS # |
Acetyl Gastric Inhibitory Peptide (human);299898-33-2
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| Appearance |
Solid powder
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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 :~50 mg/mL (~9.73 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 | 0.1946 mL | 0.9728 mL | 1.9457 mL | |
| 5 mM | 0.0389 mL | 0.1946 mL | 0.3891 mL | |
| 10 mM | 0.0195 mL | 0.0973 mL | 0.1946 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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