(Pro³)-Gastric Inhibitory Polypeptide (human) (Synonyms: (Pro3) Gastric Inhibitory Peptide, human) |
Catalog No.GA20278
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(Pro3)-Gastric Inhibitory Polypeptide (human) is an analog of human glucose-dependent insulinotropic polypeptide (GIP), distinguished by the substitution of proline for glutamate at the third amino acid position. (Pro3)-Gastric Inhibitory Polypeptide acts as a potent, stable, and specific full agonist of the human GIP receptor (hGIPR), exhibiting high binding affinity (Ki/Kd=0.90nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 299898-52-5
Sample solution is provided at 25 µL, 10mM.
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(Pro3)-Gastric Inhibitory Polypeptide (human) is an analog of human glucose-dependent insulinotropic polypeptide (GIP), distinguished by the substitution of proline for glutamate at the third amino acid position. (Pro3)-Gastric Inhibitory Polypeptide acts as a potent, stable, and specific full agonist of the human GIP receptor (hGIPR), exhibiting high binding affinity (Ki/Kd=0.90nM)[1-2]. (Pro3)-Gastric Inhibitory Polypeptide is used in research related to obesity-associated diabetes and type 2 diabetes[3-4].
In vitro, using isolated human atrial preparations, simultaneous stimulation with (Pro3)-Gastric Inhibitory Polypeptide (100nM) and Tirzepatide (100nM) was performed. (Pro3)-Gastric Inhibitory Polypeptide attenuated the positive inotropic effect induced by Tirzepatide. (Pro3)-Gastric Inhibitory Polypeptide antagonized the GIP receptor-mediated enhancement of myocardial contractility[5]. COS-7 cells transiently transfected with the human GIP receptor were stimulated with (Pro3)-Gastric Inhibitory Polypeptide (4.7nM to 92nM) for 30 minutes. (Pro3)-Gastric Inhibitory Polypeptide acted as a full agonist with similar efficacy to native human GIP at the human GIP receptor[6].
In vivo, (Pro3)-Gastric Inhibitory Polypeptide (25nmol/kg) was administered via intraperitoneal injection once or twice daily to high-fat diet-induced obese diabetic mice for 48 days. (Pro3)-Gastric Inhibitory Polypeptide significantly improved glucose tolerance and insulin sensitivity, and reduced weight gain and hyperinsulinemia[7]. In fasted obese diabetic (ob/ob) mice, a single intraperitoneal injection of (Pro3)-Gastric Inhibitory Polypeptide (25nmol/kg) was administered. (Pro3)-Gastric Inhibitory Polypeptide significantly reduced the plasma insulin response 15 minutes after re-feeding, decreasing overall insulin release by 42%. In non-fasted ob/ob mice, a single intraperitoneal injection of (Pro3)-Gastric Inhibitory Polypeptide (25nmol/kg) ameliorated the basal hyperinsulinemia[8].
References:
[1] Rosenkilde MM, Lindquist P, Kizilkaya HS, et al. GIP-derived GIP receptor antagonists - a review of their role in GIP receptor pharmacology. Peptides. 2024 Jul;177:171212.
[2] McClean PL, Irwin N, Cassidy RS, et al. GIP receptor antagonism reverses obesity, insulin resistance, and associated metabolic disturbances induced in mice by prolonged consumption of high-fat diet. Am J Physiol Endocrinol Metab. 2007 Dec;293(6):E1746-55.
[3] McClean PL, Gault VA, Irwin N, et al. Daily administration of the GIP-R antagonist (Pro3)GIP in streptozotocin-induced diabetes suggests that insulin-dependent mechanisms are critical to anti-obesity-diabetes actions of (Pro3)GIP. Diabetes Obes Metab. 2008 Apr;10(4):336-42.
[4] Cassidy RS, Irwin N, Flatt PR. Effects of gastric inhibitory polypeptide (GIP) and related analogues on glucagon release at normo- and hyperglycaemia in Wistar rats and isolated islets. Biol Chem. 2008 Feb;389(2):189-93.
[5] Neumann J, Hofmann B, Kirchhefer U, et al. Tirzepatide increased force of contraction in the isolated human atrium. Naunyn Schmiedebergs Arch Pharmacol. 2025 Oct;398(10):14451-14459.
[6] Sparre-Ulrich AH, Hansen LS, Svendsen B, et al. Species-specific action of (Pro3)GIP - a full agonist at human GIP receptors, but a partial agonist and competitive antagonist at rat and mouse GIP receptors. Br J Pharmacol. 2016 Jan;173(1):27-38.
[7] McClean PL, Irwin N, Hunter K, et al. (Pro(3))GIP[mPEG]: novel, long-acting, mPEGylated antagonist of gastric inhibitory polypeptide for obesity-diabetes (diabesity) therapy. Br J Pharmacol. 2008 Nov;155(5):690-701.
[8] Gault VA, O'Harte FP, Harriott P, et al. Effects of the novel (Pro3)GIP antagonist and exendin(9-39)amide on GIP- and GLP-1-induced cyclic AMP generation, insulin secretion and postprandial insulin release in obese diabetic (ob/ob) mice: evidence that GIP is the major physiological incretin. Diabetologia. 2003 Feb;46(2):222-30.
| Cell experiment [1]: | |
Cell lines | COS-7 cells (African green monkey kidney fibroblast-like cell line) transiently transfected with human GIP receptor cDNA |
Preparation Method | Transfected COS-7 cells were assayed for cAMP accumulation. Cells were stimulated with species-specific (Pro3)-Gastric Inhibitory Polypeptide (4.7nM to 92nM) at the indicated concentration range for 30 minutes. |
Reaction Conditions | 4.7nM to 92nM; 30 minutes. |
Applications | (Pro3)-Gastric Inhibitory Polypeptide acted as a full agonist with similar efficacy as native human GIP at the human GIP receptor. |
| Animal experiment [2]: | |
Animal models | Obese diabetic (ob/ob) mice |
Preparation Method | Mice were fasted for 18 hours, then intraperitoneally administered a single dose of (Pro3)-Gastric Inhibitory Polypeptide (25nmol/kg). Following injection, the mice were allowed to re-feed for 15 minutes. Blood samples were collected at 0, 15, 30, 60, and 120 minutes post-injection for plasma insulin and glucose analysis. |
Dosage form | 25nmol/kg; i.p.; single injection. |
Applications | Administration of (Pro3)-Gastric Inhibitory Polypeptide significantly decreased the postprandial plasma insulin response in fasted mice, reducing the overall insulin release. (Pro3)-Gastric Inhibitory Polypeptide also lowered the basal hyperinsulinaemia in non-fasted mice. Accompanying changes in plasma glucose concentrations were minimal. |
References: | |
| Cas No. | 299898-52-5 | SDF | |
| Synonyms | (Pro3) Gastric Inhibitory Peptide, human | ||
| Formula | C226H338N60O64S | M.Wt | 4951.6 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 202 μL | 1.0098 mL | 2.0195 mL |
| 5 mM | 40.4 μL | 202 μL | 403.9 μL |
| 10 mM | 20.2 μL | 101 μL | 202 μL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
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Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)