| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| Other Sizes |
Purity: =95.1%
| Targets |
Human GIP receptor (hGIPR). Human GIP(3-30), amide acts as a high-affinity antagonist of the human GIP receptor, blocking GIP-induced signaling. The GIP receptor is a G protein-coupled receptor (GPCR) expressed in pancreatic β-cells, adipose tissue, bone, and the central nervous system. Upon activation by GIP(1-42), the receptor couples to Gs proteins, leading to increased cAMP levels and activation of PKA and Epac. By competitively binding to the GIP receptor, human GIP(3-30), amide blocks GIP-mediated signaling, inhibiting GIP-stimulated insulin secretion and other GIP-dependent effects.
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| ln Vitro |
GIP(3-30)NH2 is a potent competitive antagonist of the GIP receptor and effectively inhibits GIP-mediated insulin, glucagon, and somatostatin release. In vitro, human GIP(3-30), amide acts as a high-affinity antagonist of the human GIP receptor. It inhibits GIP-stimulated insulin secretion from pancreatic β-cells and cAMP production in GIP receptor-expressing cells. The peptide also inhibits GIP-induced β-arrestin recruitment. By blocking GIP receptor signaling, the peptide inhibits GIP-mediated effects on adipocytes, including lipogenesis and fat storage. Detailed IC50 or Ki values are not provided in the available literature, but the compound is described as a high-affinity antagonist.
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| ln Vivo |
Human GIP(3-30), amide has potential anti-obesity and anti-diabetic effects by blocking GIP receptor signaling. GIP plays a role in glucose homeostasis, insulin secretion, and energy balance. In obesity, GIP levels are elevated, and GIP receptor signaling promotes fat storage and adiposity. By blocking GIP receptor signaling, GIP(3-30)NH2 may reduce fat accumulation and improve glucose tolerance. In animal models of obesity and diabetes, GIP receptor antagonists have been shown to improve glucose tolerance, reduce body weight, and ameliorate insulin resistance. The peptide is used in research to investigate the role of GIP in metabolic disorders such as diabetes and obesity.
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| Enzyme Assay |
Receptor binding assays are performed using radiolabeled GIP (e.g., 125I-GIP) incubated with membranes expressing the human GIP receptor in the presence of varying concentrations of human GIP(3-30), amide. Bound radioactivity is separated from free radioligand by filtration or centrifugation, and the inhibition of specific binding is calculated. IC50 or Ki values are determined by fitting competition binding data to a sigmoidal dose-response curve.
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| Cell Assay |
cAMP accumulation assays are performed using cells expressing the human GIP receptor treated with human GIP(3-30), amide followed by GIP(1-42) stimulation. Intracellular cAMP levels are measured via ELISA or FRET-based methods. The ability of the antagonist to inhibit GIP-stimulated cAMP production demonstrates its functional antagonism. β-arrestin recruitment assays can also be performed to assess the effects of the antagonist on GIP-induced β-arrestin signaling.
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| Animal Protocol |
Animal models of obesity and diabetes are administered human GIP(3-30), amide via subcutaneous or intraperitoneal routes. Glucose tolerance tests (OGTT) are performed to assess the effects of the antagonist on glucose handling. Insulin levels are measured to evaluate the effects on insulin secretion. Body weight and food intake are monitored to assess the effects on energy balance. The peptide is used to investigate the role of GIP in metabolic disorders.
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| ADME/Pharmacokinetics |
Human GIP(3-30), amide is a naturally occurring peptide metabolite with a short half-life due to rapid renal clearance and proteolytic degradation. GIP(3-30)NH2 is a naturally occurring metabolite of GIP, and its half-life is limited by DPP-4 cleavage and renal clearance. Pharmacokinetic parameters are evaluated in rodents. The peptide is typically administered via parenteral routes for in vivo studies. Detailed PK data specific to human GIP(3-30), amide are not extensively reported in the available literature.
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| Toxicity/Toxicokinetics |
Peptide-based GIP receptor antagonists are generally well-tolerated at therapeutic doses. Potential toxicities may include gastrointestinal effects and hypoglycemia due to GIP signaling blockade. Standard toxicology studies are required for therapeutic development. As a research compound, detailed toxicology data are not publicly available.
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| References | |
| Additional Infomation |
Human GIP(3-30), amide is a research-grade peptide antagonist for metabolic research. Molecular formula: C150H226N38O44S, molecular weight: 3297.69. Soluble in DMSO (≥100 mg/mL). It is a synthetic peptide corresponding to amino acids 3-30 of human GIP with C-terminal amidation. It is a potent competitive antagonist of the GIP receptor and effectively inhibits GIP-mediated insulin, glucagon, and somatostatin release. CAS: 1884226-05-4. Synonyms: GIP(3-30)NH2. For research use only, not for human therapeutic use.
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| Molecular Formula |
C150H226N38O44S
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| Molecular Weight |
3297.69
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| CAS # |
1884226-05-4
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| Sequence |
Glu-Gly-Thr-Phe-Ile-Ser-Asp-Tyr-Ser-Ile-Ala-Met-Asp-Lys-Ile-His-Gln-Gln-Asp-Phe-Val-Asn-Trp-Leu-Leu-Ala-Gln-Lys-NH2
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| SequenceShortening |
EGTFISDYSIAMDKIHQQDFVNWLLAQK-NH2
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| Appearance |
White to off-white 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 |
| 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) |
Typically soluble in DMSO (e.g. 10 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 | 0.3032 mL | 1.5162 mL | 3.0324 mL | |
| 5 mM | 0.0606 mL | 0.3032 mL | 0.6065 mL | |
| 10 mM | 0.0303 mL | 0.1516 mL | 0.3032 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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