| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
IC50: GLP-1 receptor[1]
GLP-1 receptor (GLP-1R). Exendin (5-39) functions as a selective antagonist by binding to the GLP-1 receptor and blocking its activation by endogenous GLP-1 or other agonists. |
|---|---|
| ln Vitro |
Exendin (5-39) is a potent GLP-1 receptor antagonist. In cell-based assays, it effectively blocks GLP-1-induced cAMP production. The reported IC50 values for antagonizing GLP-1 responses are in the low nanomolar range, demonstrating high potency at the receptor.
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| ln Vivo |
In the hippocampal regions of male Wistar rats, the intracerebroventricular injection of exendin (5-39) (0.3 μg, once daily, 1-week) raises GLT-1 protein levels. Furthermore, hippocampus slices are made from rats that were either given with Exendin (5-39) or not. Exendin reduces the fEPSP decay time, improves the input-output relationship, and lowers the paired-pulse ratio in the dentate gyrus (DG). Moreover, Ex prevents long-term potentiation in the DG[1] but not long-term depression.
Exendin (5-39) improves memory impairment in vivo. In rats treated with beta-amyloid protein to model Alzheimer‘s disease, administration of Exendin (5-39) ameliorates memory deficits, suggesting a role for GLP-1 receptor signaling in cognitive function and neuroprotection. |
| Enzyme Assay |
A typical radioligand binding assay is performed using membranes from cells expressing human GLP-1R. Membranes are incubated with [125I]GLP-1 and various concentrations of Exendin (5-39). After incubation, the mixture is filtered through glass fiber filters, washed, and the bound radioactivity is counted to calculate the Ki value for receptor binding.
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| Cell Assay |
HEK293 cells stably expressing human GLP-1R are seeded in 96-well plates. After serum starvation, cells are pre-incubated with Exendin (5-39) followed by stimulation with GLP-1. The amount of intracellular cAMP is measured using a competitive immunoassay (e.g., HTRF or ELISA) to determine the antagonist potency (IC50) of the compound.
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| Animal Protocol |
Animal/Disease Models: Wistar rats (3 weeks old and 18 days pregnant)[1]
Doses: 0.3 μg Route of Administration: Intracerebroventricular injection; 0.3 μg; one time/day; 1-week Experimental Results: Inhibited GLT-1 protein levels and inhibited long-term depression in rats. In vivo efficacy is evaluated in male Sprague-Dawley rats infused with beta-amyloid protein (1-42) into the cerebral ventricles to induce memory impairment. Exendin (5-39) is administered intracerebroventricularly or via minipump. Memory function is assessed using the passive avoidance test or Morris water maze. |
| ADME/Pharmacokinetics |
Not reported. As a peptide antagonist, Exendin (5-39) is susceptible to rapid proteolytic degradation in plasma, resulting in a short half-life typical of unmodified peptides, which may limit its in vivo applications.
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| Toxicity/Toxicokinetics |
Not reported. As a research peptide for non-clinical use, no formal toxicology data is available. Peptide antagonists are generally considered to have low toxicity, though specific side effects depend on the extent of GLP-1R blockade and off-target interactions.
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| References |
[1]. Kazuma Kobayashi, et al. Exendin (5-39), an antagonist of GLP-1 receptor, modulates synaptic transmission via glutamate uptake in the dentate gyrus. Brain Res. 2013 Apr 10;1505:1-10.
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| Additional Infomation |
Exendin (5-39) is structurally related to exendin-4, the active ingredient in the FDA-approved drug Exenatide (Byetta). While exendin-4 is an agonist for diabetes and obesity, Exendin (5-39) serves as a potent antagonist and is an important research tool for investigating the physiological and pathological roles of the GLP-1 receptor, particularly in metabolic and neurological disorders.
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| Molecular Formula |
C169H262N44O54S
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|---|---|
| Molecular Weight |
3806.27
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| Exact Mass |
3804.886
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| CAS # |
196109-27-0
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| PubChem CID |
46866279
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| Appearance |
Typically exists as solid at room temperature
|
| LogP |
-18.4
|
| Hydrogen Bond Donor Count |
52
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| Hydrogen Bond Acceptor Count |
59
|
| Rotatable Bond Count |
122
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| Heavy Atom Count |
268
|
| Complexity |
9180
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| Defined Atom Stereocenter Count |
35
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| SMILES |
CC[C@H](C)[C@@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC1=CNC2=CC=CC=C21)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)N)C(=O)NCC(=O)NCC(=O)N3CCC[C@H]3C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N4CCC[C@H]4C(=O)N5CCC[C@H]5C(=O)N6CCC[C@H]6C(=O)N[C@@H](CO)C(=O)N)NC(=O)[C@H](CC7=CC=CC=C7)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC8=CC=CC=C8)NC(=O)[C@H]([C@@H](C)O)N
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| InChi Key |
ULKZLNJITZELGU-DCLPRNCFSA-N
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| InChi Code |
InChI=1S/C169H262N44O54S/c1-16-87(10)135(164(263)193-104(51-56-131(232)233)148(247)198-111(71-94-74-179-96-39-24-23-38-95(94)96)153(252)195-106(66-83(2)3)150(249)185-98(41-26-28-59-171)143(242)199-112(72-124(173)222)139(238)181-75-125(223)180-77-127(225)210-61-30-43-119(210)160(259)205-117(81-217)159(258)203-115(79-215)140(239)182-76-126(224)183-89(12)166(265)212-63-32-45-121(212)168(267)213-64-33-46-122(213)167(266)211-62-31-44-120(211)161(260)202-114(78-214)137(175)236)208-155(254)109(69-92-34-19-17-20-35-92)197-151(250)107(67-84(4)5)194-144(243)99(42-29-60-178-169(176)177)192-163(262)134(86(8)9)207-138(237)88(11)184-141(240)101(48-53-128(226)227)188-146(245)102(49-54-129(228)229)189-147(246)103(50-55-130(230)231)190-149(248)105(57-65-268-15)191-145(244)100(47-52-123(172)221)187-142(241)97(40-25-27-58-170)186-157(256)116(80-216)204-152(251)108(68-85(6)7)196-154(253)113(73-132(234)235)200-158(257)118(82-218)206-165(264)136(91(14)220)209-156(255)110(70-93-36-21-18-22-37-93)201-162(261)133(174)90(13)219/h17-24,34-39,74,83-91,97-122,133-136,179,214-220H,16,25-33,40-73,75-82,170-171,174H2,1-15H3,(H2,172,221)(H2,173,222)(H2,175,236)(H,180,223)(H,181,238)(H,182,239)(H,183,224)(H,184,240)(H,185,249)(H,186,256)(H,187,241)(H,188,245)(H,189,246)(H,190,248)(H,191,244)(H,192,262)(H,193,263)(H,194,243)(H,195,252)(H,196,253)(H,197,250)(H,198,247)(H,199,242)(H,200,257)(H,201,261)(H,202,260)(H,203,258)(H,204,251)(H,205,259)(H,206,264)(H,207,237)(H,208,254)(H,209,255)(H,226,227)(H,228,229)(H,230,231)(H,232,233)(H,234,235)(H4,176,177,178)/t87-,88-,89-,90+,91+,97-,98-,99-,100-,101-,102-,103-,104-,105-,106-,107-,108-,109-,110-,111-,112-,113-,114-,115-,116-,117-,118-,119-,120-,121-,122-,133-,134-,135-,136-/m0/s1
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| Chemical Name |
(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-amino-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-4-carboxybutanoyl]amino]-4-carboxybutanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-4-amino-1-[[2-[[2-[(2S)-2-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[(2S)-2-[(2S)-2-[(2S)-2-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-oxopentanoic acid
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 0.2627 mL | 1.3136 mL | 2.6272 mL | |
| 5 mM | 0.0525 mL | 0.2627 mL | 0.5254 mL | |
| 10 mM | 0.0263 mL | 0.1314 mL | 0.2627 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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