| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
Exendin(9-39) amide acetate targets the glucagon-like peptide-1 (GLP-1) receptor. It acts as a competitive antagonist, binding to the receptor and blocking the effects of endogenous GLP-1. This makes it a valuable tool for studying GLP-1-related diseases and for counteracting excessive GLP-1 secretion in conditions like postbariatric hypoglycemia.
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|---|---|
| ln Vitro |
In vitro, Exendin(9-39) amide acetate acts as a potent and specific GLP-1 receptor antagonist. It competes with endogenous GLP-1 for binding to the GLP-1 receptor, thereby blocking downstream signaling. Its antagonist activity has been characterized in various cell-based assays measuring cAMP production or other GLP-1-mediated responses.
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| ln Vivo |
In vivo, Exendin(9-39) amide acetate is used in research on postbariatric hypoglycemia (PBH). By blocking GLP-1 receptor signaling, it can counteract the effects of excessive GLP-1 secretion that contribute to hypoglycemia following bariatric surgery. Its efficacy in this condition is being investigated.
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| Enzyme Assay |
The non-cellular assay for Exendin(9-39) amide acetate involves assessing its binding affinity to the GLP-1 receptor using radioligand binding assays. Membrane preparations from cells expressing the GLP-1 receptor are incubated with the compound and a radiolabeled GLP-1 ligand. Ki values are determined from competition binding curves.
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| Cell Assay |
In vitro cell-based assays for Exendin(9-39) amide acetate involve culturing cells expressing the GLP-1 receptor. Cells are treated with the compound in the presence or absence of GLP-1 stimulation. Antagonist activity is assessed by measuring inhibition of GLP-1-induced signaling (e.g., cAMP accumulation). IC50 values are determined from dose-response curves.
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| Animal Protocol |
In vivo animal study protocols for Exendin(9-39) amide acetate involve models of postbariatric hypoglycemia or other conditions involving GLP-1 signaling. The compound is administered via appropriate routes. Endpoints include blood glucose levels, GLP-1 levels, and assessment of hypoglycemia prevention.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Exendin(9-39) amide acetate are not extensively characterized. As a peptide with a molecular weight of 3549.91, it would be expected to have limited oral bioavailability and would likely require parenteral administration. Its sequence is Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2.
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| Toxicity/Toxicokinetics |
Toxicological data for Exendin(9-39) amide acetate are not extensively reported. As a research compound, it is intended for laboratory use only. Standard safety precautions should be observed during handling. The compound is not approved for human therapeutic use.
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| References | |
| Additional Infomation |
Exendin(9-39) amide acetate (Avexitide acetate) is a GLP-1 receptor antagonist used in research on postbariatric hypoglycemia. It competes with endogenous GLP-1 for receptor binding. It is a research compound and is not an FDA-approved drug.
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| Molecular Formula |
C155H246N40O53S
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|---|---|
| Molecular Weight |
3549.91
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| Exact Mass |
3548.754
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| CAS # |
2051593-46-3
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| PubChem CID |
137331909
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| Appearance |
Typically exists as solids at room temperature
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| Hydrogen Bond Donor Count |
48
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| Hydrogen Bond Acceptor Count |
58
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| Rotatable Bond Count |
109
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| Heavy Atom Count |
249
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| Complexity |
8030
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| Defined Atom Stereocenter Count |
29
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| SMILES |
S(C)CC[C@@H](C(N[C@@H](CCC(=O)O)C(N[C@@H](CCC(=O)O)C(N[C@@H](CCC(=O)O)C(N[C@@H](C)C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@@H](CC1C=CC=CC=1)C(N[C@H](C(N[C@H](C(N[C@@H](CC1=CNC2C=CC=CC1=2)C(N[C@H](C(N[C@@H](CCCCN)C(N[C@@H](CC(N)=O)C(NCC(NCC(N1CCC[C@H]1C(N[C@@H](CO)C(N[C@@H](CO)C(NCC(N[C@@H](C)C(N1CCC[C@H]1C(N1CCC[C@H]1C(N1CCC[C@H]1C(N[C@H](C(N)=O)CO)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)CC(C)C)=O)=O)CCC(=O)O)=O)[C@@H](C)CC)=O)=O)CC(C)C)=O)CCCNC(=N)N)=O)C(C)C)=O)=O)=O)=O)=O)NC([C@@H](CCC(N)=O)NC([C@H](CCCCN)NC([C@H](CO)NC([C@H](CC(C)C)NC([C@H](CC(=O)O)N)=O)=O)=O)=O)=O.OC(C)=O.OC(C)=O.OC(C)=O
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| InChi Key |
WCPGFAUEYVSQIC-XIYMWFTDSA-N
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| InChi Code |
InChI=1S/C149H234N40O47S.3C2H4O2/c1-14-78(10)120(185-139(227)98(62-81-29-16-15-17-30-81)177-136(224)97(61-76(6)7)175-129(217)88(35-24-53-158-149(156)157)172-144(232)119(77(8)9)184-122(210)79(11)164-126(214)90(41-46-114(199)200)168-131(219)91(42-47-115(201)202)169-132(220)92(43-48-116(203)204)170-134(222)94(50-58-237-13)171-130(218)89(40-45-109(153)194)167-127(215)86(33-20-22-51-150)166-140(228)103(72-192)182-137(225)95(59-74(2)3)174-123(211)84(152)64-118(207)208)145(233)173-93(44-49-117(205)206)133(221)178-99(63-82-66-159-85-32-19-18-31-83(82)85)138(226)176-96(60-75(4)5)135(223)165-87(34-21-23-52-151)128(216)179-100(65-110(154)195)124(212)161-67-111(196)160-69-113(198)186-54-25-36-105(186)142(230)183-104(73-193)141(229)181-102(71-191)125(213)162-68-112(197)163-80(12)146(234)188-56-27-38-107(188)148(236)189-57-28-39-108(189)147(235)187-55-26-37-106(187)143(231)180-101(70-190)121(155)209;3*1-2(3)4/h15-19,29-32,66,74-80,84,86-108,119-120,159,190-193H,14,20-28,33-65,67-73,150-152H2,1-13H3,(H2,153,194)(H2,154,195)(H2,155,209)(H,160,196)(H,161,212)(H,162,213)(H,163,197)(H,164,214)(H,165,223)(H,166,228)(H,167,215)(H,168,219)(H,169,220)(H,170,222)(H,171,218)(H,172,232)(H,173,233)(H,174,211)(H,175,217)(H,176,226)(H,177,224)(H,178,221)(H,179,216)(H,180,231)(H,181,229)(H,182,225)(H,183,230)(H,184,210)(H,185,227)(H,199,200)(H,201,202)(H,203,204)(H,205,206)(H,207,208)(H4,156,157,158);3*1H3,(H,3,4)/t78-,79-,80-,84-,86-,87-,88-,89+,90-,91-,92-,93-,94-,95-,96-,97-,98-,99-,100-,101-,102-,103-,104-,105-,106-,107-,108-,119-,120-;;;/m0.../s1
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| Chemical Name |
acetic acid;(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2R)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-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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| Synonyms |
Avexitide 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 |
| 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 | 0.2817 mL | 1.4085 mL | 2.8170 mL | |
| 5 mM | 0.0563 mL | 0.2817 mL | 0.5634 mL | |
| 10 mM | 0.0282 mL | 0.1408 mL | 0.2817 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.
Link: https://clinicaltrials.gov/ct2/show/NCT01152333
Conditions:Appetite Regulation|ObesityProducts are for research use only; We do not sell to patients
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