| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Not fully elucidated, but independent of the classical GLP-1 receptor. GLP-1(32-36)amide is thought to act directly on mitochondria to reduce oxidative stress and improve cellular metabolism. It does not act on the membrane-bound GLP-1 receptor, meaning it lacks the insulinotropic and gastrointestinal effects of the full-length peptide.
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| ln Vitro |
In INS-1 cells, GLP-1(32-36)amide (0.1–10 μM; 24 h) prevents apoptosis and preserves cell viability when exposed to Streptozotocin (STZ; 1 μM)[2].
GLP-1(32-36)amide protects against oxidative stress-induced dysfunction in isolated mitochondria. It is the smallest bioactive fragment of GLP-1. It does not bind to or activate the classical GLP-1 receptor, so it does not stimulate insulin secretion or slow gastric emptying, which makes it a potential candidate for treating conditions where GLP-1's gastrointestinal side effects are undesirable. |
| ln Vivo |
In diabetic mice, GLP-1(32-36)amide (1 μmol/kg; intraperitoneally once daily for 21 days) prevents damage to the islet, prevents weight gain, and alleviates polydipsia symptoms[2]. In normal animals, GLP-1(32-36)amide (1 μmol/kg; single ip) modestly lowers the mean glucose lever 30 minutes after the glucose challenge[2]. In rats fed a high-fat diet, GLP-1(32–36)amide (50–70 nmol/kg/d; infusion for 12–16 weeks) inhibits the development of diet-induced obesity and hepatic steatosis].
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| Cell Assay |
A typical method involves isolating mitochondria from rat or mouse tissues. The mitochondria are treated with GLP-1(32-36)amide (1 pM to 1 nM) and then exposed to an oxidative stress-inducing agent (e.g., tert-butyl hydroperoxide). Mitochondrial function is assessed by measuring oxygen consumption, membrane potential, and the production of reactive oxygen species (ROS).
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| Animal Protocol |
Animal/Disease Models: Male KM mice (6-8 weeks; 18-22 g) injected with STZ[2]
Doses: 1 μmol/kg Route of Administration: Ip one time/day for 21 days Experimental Results: Dramatically lowered the cumulative values of food and water intake. Lowered fasting glucose. decreased the level of Hemoglobin A1c (HbA1c). Improved glucose tolerance. Suppressed body weight gain. In vivo, GLP-1(32-36)amide can be administered intraperitoneally (i.p.) in rodent models of Alzheimer's disease (e.g., APP/PS1 mice). The peptide is given daily for several months. Endpoints include cognitive function (Morris water maze), brain levels of amyloid-beta plaque, and markers of synaptic plasticity and neuroinflammation. It can also be used in models of cardiac ischemia-reperfusion injury. |
| ADME/Pharmacokinetics |
Not reported. Given its small size, GLP-1(32-36)amide is likely to have a very short plasma half-life (minutes). However, it may be able to cross the blood-brain barrier and exert direct effects on central nervous system. Its oral bioavailability is not known.
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| Toxicity/Toxicokinetics |
Not reported. As a naturally occurring pentapeptide and a fragment of an endogenous hormone, it is likely to be safe. It lacks the side effects (nausea, vomiting) associated with full GLP-1 agonists, which is a potential advantage for long-term use in chronic diseases.
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| References |
[1]. Elahi D, et, al. GLP-1(32-36)amide, a novel pentapeptide cleavage product of GLP-1, modulates whole body glucose metabolism in dogs. Peptides. 2014 Sep;59:20-4.
[2]. Sun L, et, al. Novel Pentapeptide GLP-1 (32-36) Amide Inhibits β-Cell Apoptosis In Vitro and Improves Glucose Disposal in Streptozotocin-Induced Diabetic Mice. Chem Biol Drug Des. 2015 Dec;86(6):1482-90. [3]. Tomas E, et, al. GLP-1(32-36)amide Pentapeptide Increases Basal Energy Expenditure and Inhibits Weight Gain in Obese Mice. Diabetes. 2015 Jul;64(7):2409-19. |
| Additional Infomation |
GLP-1(32-36)amide, along with the related nonapeptide GLP-1(28-36)amide, represents a new class of "mitochondrially targeted" peptides. Research on these peptides has revealed that the GLP-1 prohormone contains multiple bioactive sequences, some of which have functions completely independent of the classical GLP-1 receptor. This has opened up new avenues for drug discovery, focusing on the direct protection of mitochondrial function in diseases characterized by oxidative stress, such as Alzheimer's, Parkinson's, and heart failure.
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| Molecular Formula |
C25H50N10O5
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|---|---|
| Molecular Weight |
570.73
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| Exact Mass |
570.396
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| CAS # |
1417302-71-6
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| Related CAS # |
GLP-1(32-36)amide TFA
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| PubChem CID |
71497119
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
-1.9
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| Hydrogen Bond Donor Count |
9
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
20
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| Heavy Atom Count |
40
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| Complexity |
861
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC(C)C[C@@H](C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCN=C(N)N)C(=O)N)N
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| InChi Key |
VCMIHDDYZTYYJC-JPLJXNOCSA-N
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| InChi Code |
InChI=1S/C25H50N10O5/c1-14(2)12-16(27)22(38)35-20(15(3)4)24(40)34-18(8-5-6-10-26)23(39)32-13-19(36)33-17(21(28)37)9-7-11-31-25(29)30/h14-18,20H,5-13,26-27H2,1-4H3,(H2,28,37)(H,32,39)(H,33,36)(H,34,40)(H,35,38)(H4,29,30,31)/t16-,17-,18-,20-/m0/s1
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| Chemical Name |
(2S)-6-amino-N-[2-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-2-oxoethyl]-2-[[(2S)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-3-methylbutanoyl]amino]hexanamide
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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) |
DMSO: 250 mg/mL (438.04 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.64 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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: ≥ 2.08 mg/mL (3.64 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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.64 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7521 mL | 8.7607 mL | 17.5214 mL | |
| 5 mM | 0.3504 mL | 1.7521 mL | 3.5043 mL | |
| 10 mM | 0.1752 mL | 0.8761 mL | 1.7521 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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