![[D-Ala2]-GIP (human)](/upload/1124/V69511.png)
| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
GIP receptor. [D-Ala2]-GIP (human) is a GIP receptor agonist with an EC50 of 630 +/- 119 pM. It activates the GIP receptor, leading to cAMP accumulation, insulin secretion, and improvement of glucose tolerance.
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| ln Vitro |
[D-Ala2]-GIP (human) is a highly potent GIP receptor agonist (EC50 = 630 +/- 119 pM) in cells expressing the wild-type GIP receptor. It displays equivalent cAMP stimulating properties and improved resistance to enzymatic degradation compared to native GIP. It improves glucose tolerance and insulin release.
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| ln Vivo |
[D-Ala2]-GIP (human) improves glucose tolerance, insulin release, and cognitive function in various animal models of obesity and diabetes. It also shows neuroprotective activity in the MPTP-induced Parkinson's disease model. It is a valuable tool for studying GIP receptor pharmacology and its potential in metabolic and neurodegenerative diseases.
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| Enzyme Assay |
Cell-free GIP receptor binding assays are performed using membranes from cells expressing the human GIP receptor. The membranes are incubated with a radiolabeled GIP ligand (e.g., 125I-GIP) and increasing concentrations of [D-Ala2]-GIP (human). After 60-90 minutes, bound radioactivity is separated by filtration, and binding affinity (Ki) is calculated.
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| Cell Assay |
Cells expressing the human GIP receptor (e.g., CHO-K1 cells) are loaded with a cAMP detection kit (HTRF). [D-Ala2]-GIP (human) is added at increasing concentrations (0.1 pM to 1 uM), and cAMP accumulation is measured. EC50 (630 +/- 119 pM) is determined from a dose-response curve. The effect on insulin secretion can be assessed in pancreatic beta-cell lines.
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| Animal Protocol |
For in vivo studies, [D-Ala2]-GIP (human) is administered via intraperitoneal or subcutaneous injection to mice or rats. Doses typically range from 1-100 nmol/kg. Glucose tolerance tests (oral or intraperitoneal glucose load) are performed 15-30 min post-injection. Blood glucose levels are measured, and plasma insulin is quantified by ELISA. For neuroprotection studies, it is administered in the MPTP Parkinson's disease model.
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| ADME/Pharmacokinetics |
No specific PK data are reported for [D-Ala2]-GIP (human). As a synthetic peptide, it is not orally bioavailable and has a relatively short half-life (minutes to hours) despite improved enzymatic resistance compared to native GIP. For in vivo studies, it is typically administered by injection. The molecular weight is 4977.6. Solubility: water (≥10 mg/mL).
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| Toxicity/Toxicokinetics |
No specific toxicity data are reported for [D-Ala2]-GIP (human). As a GIP receptor agonist, potential adverse effects may include hypoglycemia at high doses. Preclinical studies have not reported significant toxicity at the doses used for metabolic studies. The compound is for research use only and is not a therapeutic agent.
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| References |
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| Additional Infomation |
Other information: [D-Ala2]-GIP (human) (CAS 444073-04-5) is a research-grade peptide, not FDA-approved. It is a highly potent GIP receptor agonist with an EC50 of 630 pM and improved resistance to enzymatic degradation compared to native GIP. It is a valuable tool for studying GIP receptor function in metabolic diseases and neuroprotection. For research use only.
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| Molecular Formula |
C22H27NO11
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|---|---|
| Molecular Weight |
481.158417
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| Exact Mass |
481.158
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| CAS # |
444073-04-5
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| PubChem CID |
168006474
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| Sequence |
Tyr-{d-Ala}-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-Gly-Lys-Lys-Asn-Asp-Trp-Lys-His-Asn-Ile-Thr-GlnY-{d-Ala}-EGTFISDYSIAMDKIHQQDFVNWLLAQKGKKNDWKHNITQ
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| SequenceShortening |
Y-{d-Ala}-EGTFISDYSIAMDKIHQQDFVNWLLAQKGKKNDWKHNITQ
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| Appearance |
White to off-white solid powder
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| LogP |
2.5
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
34
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| Complexity |
747
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC=C1O[C@H]1[C@@H]([C@@H]([C@@H]([C@@H](COC(C)=O)O1)OC(C)=O)OC(C)=O)OC(C)=O)/C=N\OC
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| InChi Key |
OXLRMRDQILKNCS-AUEPDCJTSA-N
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| InChi Code |
InChI=1S/C22H27NO11/c1-12(24)29-11-18-19(30-13(2)25)20(31-14(3)26)21(32-15(4)27)22(34-18)33-17-8-6-16(7-9-17)10-23-28-5/h6-10,18-22H,11H2,1-5H3/b23-10+
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| Chemical Name |
[3,4,5-triacetyloxy-6-[4-[(E)-methoxyiminomethyl]phenoxy]oxan-2-yl]methyl acetate
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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) |
DMSO: 50 mg/mL (10.03 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (0.50 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (0.50 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (0.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0783 mL | 10.3916 mL | 20.7831 mL | |
| 5 mM | 0.4157 mL | 2.0783 mL | 4.1566 mL | |
| 10 mM | 0.2078 mL | 1.0392 mL | 2.0783 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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