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| 1mg |
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| 5mg |
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| Targets |
The primary target of GIP is the GIP receptor (GIPR), a G protein-coupled receptor expressed on pancreatic beta cells, adipocytes, and other tissues. GIP is a high-affinity agonist of its receptor with an EC₅₀ of 0.81 nM. Activation of GIPR stimulates glucose-dependent insulin secretion from pancreatic beta cells and promotes glucose uptake in peripheral tissues.
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| ln Vitro |
The peripheral effects of gastric inhibitory polypeptide (GIP) on lipid metabolism and adipose tissue lead to enhanced fat accumulation in the postprandial state [1]. GIP, lipid metabolism and the onset of obesity are major human factors.
GIP exhibits potent incretin activity in both rodent and human subjects, with the primary action being the stimulation of glucose-dependent insulin secretion. In vitro studies have shown that GIP enhances glucose absorption in enterocytes, potentiates endogenous glucose-dependent insulin release from islet beta-cells, increases glucose uptake while inhibiting lipolysis in adipocytes, and increases nutrient uptake into bone while inhibiting bone resorption. |
| ln Vivo |
GIP lowers blood glucose levels by stimulating an increase in insulin levels in vivo. It is an essential regulator of insulin secretion and glucose homeostasis. In rodent and human subjects, GIP exhibits potent incretin activity, enhancing glucose-dependent insulin secretion in response to nutrient ingestion. GIP may also play a role in adipocyte biology.
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| Enzyme Assay |
For in vitro receptor binding assays, GIP is typically evaluated using cell lines expressing the human GIP receptor. Competitive binding experiments are performed using radiolabeled GIP (e.g., ¹²⁵I-GIP) incubated with varying concentrations of unlabeled GIP at 4°C for 2-4 hours. Non-specific binding is determined in the presence of excess unlabeled peptide. Binding affinity (Kd or IC₅₀) is calculated from displacement curves.
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| Cell Assay |
For in vitro cell-based assays, GIP is typically tested on pancreatic beta-cell lines (such as MIN6 or INS-1) or primary human islets. Cells are serum-starved and then stimulated with glucose (e.g., 5-20 mM) in the presence or absence of GIP at various concentrations (typically 0.01-100 nM). Insulin secretion is measured by ELISA or radioimmunoassay. Signaling pathway activation (e.g., cAMP accumulation) can also be quantified.
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| Animal Protocol |
For in vivo animal experiments, GIP is typically administered via intravenous or intraperitoneal injection in mice or rats. Glucose tolerance tests (OGTT or IPGTT) are performed to assess the incretin effect, with GIP administered prior to or concurrently with glucose challenge. Blood glucose and plasma insulin levels are measured at multiple time points post-administration to evaluate the insulinotropic response.
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| ADME/Pharmacokinetics |
GIP is a peptide hormone with a short half-life in circulation due to rapid degradation by the enzyme dipeptidyl peptidase-4 (DPP-4). The in vivo half-life of native GIP is approximately 2-5 minutes in humans. This rapid clearance necessitates continuous infusion or the use of DPP-4-resistant analogs for prolonged therapeutic effect. The peptide is administered via injection and is not orally bioavailable.
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| Toxicity/Toxicokinetics |
As an endogenous peptide hormone, GIP is generally well-tolerated at physiological concentrations. However, at supraphysiological doses, potential side effects may include hypoglycemia due to excessive insulin stimulation. GIP is classified as a research-grade peptide and is not approved for human therapeutic use. Standard laboratory safety practices should be followed when handling the compound.
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| References |
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| Additional Infomation |
GIP (1-42) is a 42-amino acid peptide with a molecular weight of approximately 4980.49 Da. It is typically supplied as a TFA salt with purity >95%. The peptide sequence is well-characterized and is available from various research suppliers. GIP is also known as glucose-dependent insulinotropic polypeptide. It is for research use only and has not been approved for clinical applications.
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| Molecular Formula |
C226H338N60O66S
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| Molecular Weight |
4983.52937078476
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| CAS # |
100040-31-1
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| Related CAS # |
GIP, human TFA
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| PubChem CID |
131954558
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
70
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| Hydrogen Bond Acceptor Count |
75
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| Rotatable Bond Count |
168
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| Heavy Atom Count |
353
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| Complexity |
12400
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C)CCC(C(NC(CC(=O)O)C(NC(C(NC(C(NC(C(NC(C(NC(C(NC(CC(=O)O)C(NC(CC1C=CC=CC=1)C(NC(C(NC(CC(N)=O)C(NC(C(NC(C(NC(C(NC(C)C(NC(C(NC(C(NCC(NC(C(NC(C(NC(CC(N)=O)C(NC(CC(=O)O)C(NC(C(NC(C(NC(CC1=CNC=N1)C(NC(CC(N)=O)C(NC(C(NC(C(NC(C(=O)O)CCC(N)=O)=O)C(C)O)=O)C(C)CC)=O)=O)=O)CCCCN)=O)CC1=CNC2C=CC=CC1=2)=O)=O)=O)CCCCN)=O)CCCCN)=O)=O)CCCCN)=O)CCC(N)=O)=O)=O)CC(C)C)=O)CC(C)C)=O)CC1=CNC2C=CC=CC1=2)=O)=O)C(C)C)=O)=O)=O)CCC(N)=O)=O)CCC(N)=O)=O)CC1=CNC=N1)=O)C(C)CC)=O)CCCCN)=O)=O)NC(C(C)NC(C(C(C)CC)NC(C(CO)NC(C(CC1C=CC(=CC=1)O)NC(C(CC(=O)O)NC(C(CO)NC(C(C(C)CC)NC(C(CC1C=CC=CC=1)NC(C(C(C)O)NC(CNC(C(CCC(=O)O)NC(C(C)NC(C(CC1C=CC(=CC=1)O)N)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O
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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) |
H2O : ~25 mg/mL (~5.02 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 | 0.2007 mL | 1.0033 mL | 2.0066 mL | |
| 5 mM | 0.0401 mL | 0.2007 mL | 0.4013 mL | |
| 10 mM | 0.0201 mL | 0.1003 mL | 0.2007 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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