| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
Exendin-3 targets VIP (vasoactive intestinal peptide) receptors and a putative exendin receptor on pancreatic acinar cells. VIP receptors are G protein-coupled receptors that are activated by vasoactive intestinal peptide and related peptides. In the pancreas, these receptors regulate exocrine and endocrine secretion. Exendin-3 also interacts with a newly described receptor on dispersed acini from guinea pig pancreas. The peptide's mechanism of action involves binding to these receptors and activating signaling pathways that regulate pancreatic secretion. Exendin-3 is a member of the glucagon family of peptides and shares sequence similarity with glucagon, GLP-1, and other related peptides. Its receptor interactions have been characterized in various in vitro systems.
|
|---|---|
| ln Vitro |
Exendin-3 interacts with guinea pig pancreatic acini through at least two receptors; at high concentrations(>100 nM), the peptide interacts with VIP receptors, resulting in a significant increase in cAMP and stimulating the release of amylase; at higher concentrations This peptide interacts with putative exendin receptors at low concentrations (0.1-3 nM) and causes a slight increase in cAMP with unknown function [1].
Exendin-3 demonstrates potent in vitro activity in stimulating pancreatic secretion. The peptide interacts with vasoactive intestinal peptide receptors and a newly described receptor on dispersed acini from guinea pig pancreas. In pancreatic acinar cell preparations, exendin-3 stimulates amylase secretion and other pancreatic enzymes. The peptide's activity is concentration-dependent, with effects observed at nanomolar concentrations. Exendin-3's effects on pancreatic secretion have been well-characterized in vitro. The peptide is closely related to exendin-4, which is a potent GLP-1 receptor agonist. However, exendin-3 has different receptor selectivity compared to exendin-4. |
| ln Vivo |
In vivo, exendin-3 has been studied for its effects on pancreatic secretion and glucose metabolism. As a member of the glucagon family, exendin-3 may have effects on glucose homeostasis similar to those of GLP-1 and exendin-4. However, exendin-3 has different receptor selectivity compared to exendin-4. The peptide has been studied in animal models to evaluate its effects on pancreatic exocrine and endocrine function. Exendin-3's in vivo activity has been described in the literature. The peptide is primarily used as a research tool for studying VIP receptor biology and pancreatic secretion. Comprehensive in vivo efficacy studies using exendin-3 as a therapeutic agent have not been extensively reported.
|
| Enzyme Assay |
In vitro receptor binding assays for exendin-3 involve measuring binding affinity to VIP receptors and other receptors. Membranes from cells expressing VIP receptors or pancreatic acinar cells are incubated with a radiolabeled ligand (e.g., [¹2⁵I]-VIP) and varying concentrations of the test peptide. Bound and free radioligand are separated by filtration, and radioactivity is measured. Binding affinity (Ki) is calculated from competition curves using non-linear regression analysis. Alternatively, functional assays can measure receptor activation. For example, cAMP accumulation can be measured in cells expressing VIP receptors following treatment with exendin-3. EC50 values are calculated from dose-response curves. Each concentration is typically tested in duplicate or triplicate.
|
| Cell Assay |
In vitro cellular assays for exendin-3 are performed using pancreatic acinar cells or cells expressing VIP receptors. Dispersed acini from guinea pig pancreas are prepared and treated with varying concentrations of exendin-3. Amylase secretion is measured as a marker of pancreatic exocrine function. Alternatively, cells expressing VIP receptors can be used to measure cAMP accumulation or other second messenger responses. The peptide's effects on intracellular signaling pathways can be assessed by Western blot or immunoassay. Cytotoxicity is assessed using standard viability assays to ensure that observed effects are not due to cell death. EC50 values for stimulation of secretion or signaling are calculated from dose-response curves.
|
| Animal Protocol |
In vivo animal studies for exendin-3 are conducted using rodent models. The peptide is typically administered by injection (intraperitoneal, intravenous, or subcutaneous). In studies of pancreatic secretion, the peptide's effects on amylase secretion or other pancreatic parameters can be assessed. In studies of glucose metabolism, blood glucose and insulin levels can be measured. Pharmacokinetic studies assess peptide concentrations in plasma. Animals are monitored for clinical signs and body weight. The peptide's in vivo effects are mediated through VIP receptor activation and other receptor interactions.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of exendin-3 are characteristic of a peptide. The peptide has a molecular formula of C184H282N50O61S and a molecular weight of 4202.57 g/mol. As a peptide, exendin-3 is susceptible to proteolytic degradation and has a short half-life in circulation. The peptide is soluble in water. Comprehensive pharmacokinetic parameters including half-life, volume of distribution, clearance, and bioavailability have been characterized in preclinical studies. The peptide is typically administered by injection due to poor oral bioavailability. Its pharmacokinetic profile supports its use as a research tool.
|
| Toxicity/Toxicokinetics |
Exendin-3 is intended for laboratory research use only and has not undergone comprehensive toxicology testing. As a peptide from the glucagon family, the compound may have effects on glucose metabolism and gastrointestinal function. Standard in vitro cytotoxicity assays in cell lines are typically performed alongside efficacy studies to rule out nonspecific toxicity. In vivo, animals are monitored for signs of toxicity including body weight changes, behavioral abnormalities, and clinical observations. Comprehensive toxicological characterization including genotoxicity and repeated-dose toxicity studies has not been reported for exendin-3. The peptide is not approved for human use and is strictly intended for research purposes.
|
| References | |
| Additional Infomation |
Exendin-3 is a biologically active peptide from the glucagon family, isolated from the venom of the Gila monster lizard, Heloderma horridum. It has a molecular formula of C184H282N50O61S and a molecular weight of 4202.57 g/mol. Exendin-3 interacts with VIP receptors and a putative exendin receptor on pancreatic acinar cells. The peptide stimulates pancreatic secretion and has been studied for its effects on glucose metabolism. Exendin-3 is closely related to exendin-4, which is the active ingredient in the FDA-approved drug exenatide for type 2 diabetes. Exendin-3 has not entered clinical trials and has not received regulatory approval for any indication. It is available from research chemical suppliers for non-clinical research purposes only. Exendin-3 is a valuable research tool for studying VIP receptor biology and pancreatic secretion.
|
| Molecular Formula |
C184H282N50O61S
|
|---|---|
| Molecular Weight |
4202.57
|
| Exact Mass |
4201.025
|
| CAS # |
130357-25-4
|
| PubChem CID |
131636564
|
| Appearance |
White to off-white solid powder
|
| LogP |
-22
|
| Hydrogen Bond Donor Count |
59
|
| Hydrogen Bond Acceptor Count |
67
|
| Rotatable Bond Count |
135
|
| Heavy Atom Count |
296
|
| Complexity |
10300
|
| Defined Atom Stereocenter Count |
38
|
| SMILES |
S(C([H])([H])[H])C([H])([H])C([H])([H])[C@@]([H])(C(N([H])[C@@]([H])(C([H])([H])C([H])([H])C(=O)O[H])C(N([H])[C@@]([H])(C([H])([H])C([H])([H])C(=O)O[H])C(N([H])[C@@]([H])(C([H])([H])C([H])([H])C(=O)O[H])C(N([H])[C@@]([H])(C([H])([H])[H])C(N([H])[C@]([H])(C(N([H])[C@]([H])(C(N([H])[C@]([H])(C(N([H])[C@@]([H])(C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H])C(N([H])[C@]([H])(C(N([H])[C@@]([H])(C([H])([H])C([H])([H])C(=O)O[H])C(N([H])[C@@]([H])(C([H])([H])C1=C([H])N([H])C2=C([H])C([H])=C([H])C([H])=C12)C(N([H])[C@@]([H])(C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])C(N([H])[C@@]([H])(C([H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])[H])C(N([H])[C@@]([H])(C([H])([H])C(N([H])[H])=O)C(N([H])C([H])([H])C(N([H])C([H])([H])C(N1C([H])([H])C([H])([H])C([H])([H])[C@@]1([H])C(N([H])[C@@]([H])(C([H])([H])O[H])C(N([H])[C@@]([H])(C([H])([H])O[H])C(N([H])C([H])([H])C(N([H])[C@@]([H])(C([H])([H])[H])C(N1C([H])([H])C([H])([H])C([H])([H])[C@@]1([H])C(N1C([H])([H])C([H])([H])C([H])([H])[C@@]1([H])C(N1C([H])([H])C([H])([H])C([H])([H])[C@@]1([H])C(N([H])[C@]([H])(C(N([H])[H])=O)C([H])([H])O[H])=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)[C@@]([H])(C([H])([H])[H])C([H])([H])C([H])([H])[H])=O)=O)C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])=O)C([H])([H])C([H])([H])C([H])([H])N([H])/C(=N/[H])/N([H])[H])=O)C([H])(C([H])([H])[H])C([H])([H])[H])=O)=O)=O)=O)=O)N([H])C([C@]([H])(C([H])([H])C([H])([H])C(N([H])[H])=O)N([H])C([C@]([H])(C([H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])[H])N([H])C([C@]([H])(C([H])([H])O[H])N([H])C([C@]([H])(C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])N([H])C([C@]([H])(C([H])([H])C(=O)O[H])N([H])C([C@]([H])(C([H])([H])O[H])N([H])C([C@]([H])([C@@]([H])(C([H])([H])[H])O[H])N([H])C([C@]([H])(C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H])N([H])C([C@]([H])([C@@]([H])(C([H])([H])[H])O[H])N([H])C(C([H])([H])N([H])C([C@]([H])(C([H])([H])C(=O)O[H])N([H])C([C@]([H])(C([H])([H])O[H])N([H])C([C@]([H])(C([H])([H])C1=C([H])N([H])C([H])=N1)N([H])[H])=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O
|
| InChi Key |
LMHMJYMCGJNXRS-IEQINRSDSA-N
|
| InChi Code |
InChI=1S/C184H282N50O61S/c1-16-93(10)146(178(290)211-112(51-56-142(255)256)162(274)216-119(71-100-76-195-104-39-24-23-38-102(100)104)167(279)213-114(66-89(2)3)164(276)203-106(41-26-28-59-186)157(269)217-120(73-134(189)244)152(264)197-78-135(245)196-81-138(248)231-61-30-43-129(231)175(287)225-127(86-239)174(286)223-124(83-236)154(266)199-79-136(246)201-95(12)181(293)233-63-32-45-131(233)183(295)234-64-33-46-132(234)182(294)232-62-31-44-130(232)176(288)221-123(82-235)149(190)261)229-169(281)117(69-98-34-19-17-20-35-98)215-165(277)115(67-90(4)5)212-158(270)107(42-29-60-194-184(191)192)210-177(289)145(92(8)9)228-150(262)94(11)202-155(267)109(48-53-139(249)250)206-160(272)110(49-54-140(251)252)207-161(273)111(50-55-141(253)254)208-163(275)113(57-65-296-15)209-159(271)108(47-52-133(188)243)205-156(268)105(40-25-27-58-185)204-171(283)126(85-238)224-166(278)116(68-91(6)7)214-168(280)122(75-144(259)260)219-173(285)128(87-240)226-180(292)148(97(14)242)230-170(282)118(70-99-36-21-18-22-37-99)220-179(291)147(96(13)241)227-137(247)80-198-153(265)121(74-143(257)258)218-172(284)125(84-237)222-151(263)103(187)72-101-77-193-88-200-101/h17-24,34-39,76-77,88-97,103,105-132,145-148,195,235-242H,16,25-33,40-75,78-87,185-187H2,1-15H3,(H2,188,243)(H2,189,244)(H2,190,261)(H,193,200)(H,196,245)(H,197,264)(H,198,265)(H,199,266)(H,201,246)(H,202,267)(H,203,276)(H,204,283)(H,205,268)(H,206,272)(H,207,273)(H,208,275)(H,209,271)(H,210,289)(H,211,290)(H,212,270)(H,213,279)(H,214,280)(H,215,277)(H,216,274)(H,217,269)(H,218,284)(H,219,285)(H,220,291)(H,221,288)(H,222,263)(H,223,286)(H,224,278)(H,225,287)(H,226,292)(H,227,247)(H,228,262)(H,229,281)(H,230,282)(H,249,250)(H,251,252)(H,253,254)(H,255,256)(H,257,258)(H,259,260)(H4,191,192,194)/t93-,94-,95-,96+,97+,103-,105-,106-,107-,108-,109-,110-,111-,112-,113-,114-,115-,116-,117-,118-,119-,120-,121-,122-,123-,124-,125-,126-,127-,128-,129-,130-,131-,132-,145-,146-,147-,148-/m0/s1
|
| Chemical Name |
(4S)-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]-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-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-(1H-imidazol-4-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]acetyl]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-oxopentanoic acid
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 0.2379 mL | 1.1897 mL | 2.3795 mL | |
| 5 mM | 0.0476 mL | 0.2379 mL | 0.4759 mL | |
| 10 mM | 0.0238 mL | 0.1190 mL | 0.2379 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
