| Size | Price | Stock | Qty |
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| 5mg |
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| 5mg |
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| 10mg |
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| 10mg |
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| 25mg | |||
| 25mg | |||
| Other Sizes |
| Targets |
GLP-1R ( EC50 = 11.3 μM )
VU0453379 targets the glucagon-like peptide-1 receptor (GLP-1R), a class B G protein-coupled receptor that plays a key role in glucose homeostasis and has emerging importance in the central nervous system. As a PAM, it binds to an allosteric site distinct from the orthosteric site, enhancing the receptor's response to its endogenous agonist, GLP-1. |
|---|---|
| ln Vitro |
In vitro, VU0453379 acts as a positive allosteric modulator of GLP-1R with an EC50 of 1.3 μM. Its activity is confirmed in cell-based assays where it potentiates the effects of GLP-1. The compound is highly selective for GLP-1R.
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| ln Vivo |
In vivo, VU0453379 is a CNS-penetrant compound, meaning it can cross the blood-brain barrier. This property makes it a valuable tool for studying the role of GLP-1R signaling in the brain, which is implicated in neuroprotection, feeding behavior, and cognitive function.
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| Enzyme Assay |
In vitro receptor binding assays for VU0453379 are performed using membrane preparations expressing the GLP-1 receptor. These assays typically involve radioligand binding techniques to confirm its allosteric binding site and selectivity. Its PAM activity is confirmed through functional assays that measure its ability to potentiate GLP-1-induced responses.
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| Cell Assay |
In vitro cellular assays are performed using cell lines expressing the GLP-1 receptor. Cells are treated with the compound in the presence of a sub-maximal concentration of GLP-1, and receptor activation is measured by quantifying downstream signaling, such as cAMP accumulation. The EC50 of 1.3 μM is calculated from these concentration-response curves.
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| Animal Protocol |
In vivo animal experiments for VU0453379 are conducted to evaluate its effects in the central nervous system. Due to its CNS-penetrant nature, it can be administered systemically to study its impact on GLP-1R-mediated behaviors, such as food intake, anxiety, or cognition in rodent models.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties include its ability to penetrate the central nervous system. It has a LogP of 3.6 and is soluble in DMSO.
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| Toxicity/Toxicokinetics |
Toxicological data is not extensively detailed in the provided literature. However, as a research compound, its safety profile has not been formally evaluated for therapeutic use.
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| References | |
| Additional Infomation |
VU0453379 is a research compound and is not approved for clinical use. It is one of the first CNS-penetrant GLP-1R PAMs and serves as a critical tool for investigating the potential of GLP-1R signaling in the brain.
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| Molecular Formula |
C26H34N4O2
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|---|---|
| Molecular Weight |
434.573766231537
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| Exact Mass |
434.27
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| Elemental Analysis |
C, 71.86; H, 7.89; N, 12.89; O, 7.36
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| CAS # |
1638646-27-1
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| Related CAS # |
VU0453379 hydrochloride
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| PubChem CID |
101891769
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
3.6
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
32
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| Complexity |
759
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC(C)N1CCC[C@H]1CNC(=O)C2=CN(C(=O)C3=C2C4=CC=CC=C4N3C)C5CCCC5
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| InChi Key |
OEYYOVRNPJSWTO-IBGZPJMESA-N
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| InChi Code |
InChI=1S/C26H34N4O2/c1-17(2)29-14-8-11-19(29)15-27-25(31)21-16-30(18-9-4-5-10-18)26(32)24-23(21)20-12-6-7-13-22(20)28(24)3/h6-7,12-13,16-19H,4-5,8-11,14-15H2,1-3H3,(H,27,31)/t19-/m0/s1
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| Chemical Name |
2-cyclopentyl-9-methyl-1-oxo-N-[[(2S)-1-propan-2-ylpyrrolidin-2-yl]methyl]pyrido[3,4-b]indole-4-carboxamide
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| Synonyms |
VU 0453379; VU-0453379; VU0453379
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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: ~100 mg/mL (~230.11 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.75 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3011 mL | 11.5056 mL | 23.0113 mL | |
| 5 mM | 0.4602 mL | 2.3011 mL | 4.6023 mL | |
| 10 mM | 0.2301 mL | 1.1506 mL | 2.3011 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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