| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg |
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| Other Sizes |
| Targets |
Aleniglipron targets the glucagon-like peptide-1 (GLP-1) receptor. As a non-peptide agonist, it binds to a deep orthosteric cavity within the transmembrane domains (TM1, TM2, and TM7). This binding activates the GLP-1 receptor, stimulating insulin secretion, promoting satiety, and reducing body weight.
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|---|---|
| ln Vitro |
In vitro, Aleniglipron is a GLP-1 agonist with an EC50 value of less than 0.1 nM in the HDB cell line in a cAMP stimulation assay. This demonstrates potent activation of the GLP-1 receptor signaling pathway. Its non-peptide nature offers advantages over peptide GLP-1 agonists in terms of oral bioavailability and stability.
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| ln Vivo |
In vivo, Aleniglipron reduces body weight and improves insulin sensitivity. As an orally active compound, it can be administered via oral gavage. Its effects on weight loss and insulin sensitivity make it a promising candidate for obesity and type 2 diabetes research.
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| Enzyme Assay |
The non-cellular assay for Aleniglipron 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. Binding affinity and orthosteric binding mode can be confirmed.
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| Cell Assay |
In vitro cell-based assays for Aleniglipron involve culturing HDB cells or other cells expressing the GLP-1 receptor. Cells are treated with varying concentrations of the compound, and cAMP accumulation is measured as a readout of GLP-1 receptor activation. EC50 values are determined from dose-response curves.
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| Animal Protocol |
In vivo animal study protocols for Aleniglipron involve obesity or diabetes models. The compound is administered orally. Endpoints include body weight, food intake, glucose tolerance, insulin sensitivity, and metabolic parameters. Standard protocols for evaluating anti-obesity and antidiabetic efficacy are followed.
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| ADME/Pharmacokinetics |
Aleniglipron is orally active with favorable pharmacokinetic properties. It has a molecular formula of C49H55FN9O6P and a molecular weight of 916.0. As a non-peptide small molecule, it is expected to have good oral bioavailability. Further PK studies are needed for detailed characterization.
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| Toxicity/Toxicokinetics |
Toxicological data for Aleniglipron 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 |
Aleniglipron is a small molecule agonist of the GLP-1 receptor.
Aleniglipron (GSBR-1290, compound 121a) is an orally active, non-peptide GLP-1 agonist. It reduces body weight and improves insulin sensitivity. It binds to a deep orthosteric cavity within the GLP-1 receptor transmembrane domains. It is a research compound and is not an FDA-approved drug. |
| Molecular Formula |
C49H55FN9O6P
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|---|---|
| Molecular Weight |
915.99
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| Exact Mass |
915.4
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| CAS # |
2685823-26-9
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| PubChem CID |
164809721
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| Appearance |
White to off-white solid
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
66
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| Complexity |
1950
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CCP(=O)(CC)C1=C(C=C(C=C1)N2C=CN(C2=O)C3=C4[C@@H](N(CCC4=NN3C5=CC(=C(C(=C5)C)F)C)C(=O)C6=CC7=C(N6[C@]8(C[C@@H]8C)C9=NOC(=O)N9)C=CC(=C7)C1CCOCC1)C)NC
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| InChi Key |
CPOJUYUGONJVPZ-WIXASUBBSA-N
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| InChi Code |
InChI=1S/C49H55FN9O6P/c1-8-66(63,9-2)41-13-11-35(26-38(41)51-7)56-18-19-57(48(56)62)44-42-31(6)55(17-14-37(42)53-59(44)36-22-28(3)43(50)29(4)23-36)45(60)40-25-34-24-33(32-15-20-64-21-16-32)10-12-39(34)58(40)49(27-30(49)5)46-52-47(61)65-54-46/h10-13,18-19,22-26,30-32,51H,8-9,14-17,20-21,27H2,1-7H3,(H,52,54,61)/t30-,31-,49-/m0/s1
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| Chemical Name |
3-[(1S,2S)-1-[2-[(4S)-3-[3-[4-diethylphosphoryl-3-(methylamino)phenyl]-2-oxoimidazol-1-yl]-2-(4-fluoro-3,5-dimethylphenyl)-4-methyl-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carbonyl]-5-(oxan-4-yl)indol-1-yl]-2-methylcyclopropyl]-4H-1,2,4-oxadiazol-5-one
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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: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), 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: ~100 mg/mL (~109.2 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.73 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 | 1.0917 mL | 5.4586 mL | 10.9171 mL | |
| 5 mM | 0.2183 mL | 1.0917 mL | 2.1834 mL | |
| 10 mM | 0.1092 mL | 0.5459 mL | 1.0917 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/NCT06693843
Conditions:Obesity, Overweight, or Chronic Weight ManagementLink: https://clinicaltrials.gov/ct2/show/NCT06703021
Conditions:Obesity|Overweight|Chronic Weight ManagementLink: https://clinicaltrials.gov/ct2/show/NCT07400588
Conditions:Obese|Obesity|Obesity Type 2 Diabetes Mellitus|Weight Loss
Title:Aleniglipron Phase 2 Body Composition Study
Status:Active, not recruiting
updateDate:2026-03-03
Ctid:NCT07169942
Link: https://clinicaltrials.gov/ct2/show/NCT07169942
Conditions:Obesity, Overweight, or Chronic Weight ManagementLink: https://clinicaltrials.gov/ct2/show/NCT05762471
Conditions:Overweight or Obesity|Type2 Diabetes MellitusLink: https://clinicaltrials.gov/ct2/show/NCT06139055
Conditions:Healthy VolunteersLink: https://clinicaltrials.gov/ct2/show/NCT05893043
Conditions:Healthy VolunteersProducts are for research use only; We do not sell to patients
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