| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg | |||
| Other Sizes |
| Targets |
PSN632408 specifically targets the G protein-coupled receptor GPR119. It acts as a potent and selective agonist at this receptor. GPR119 is primarily expressed in the pancreas and gastrointestinal tract and is involved in glucose metabolism and appetite regulation. The compound shows similar potency to the endogenous ligand OEA (oleoylethanolamide), with EC50 values of 5.6 µM for the mouse receptor and 7.9 µM for the human receptor.
|
|---|---|
| ln Vitro |
PSN632408 increases cAMP levels in a concentration-dependent manner, with an average EC50 value of 1.9 uM[1]. In cultured mouse islets, PSN632408 promotes beta cell multiplication [2].
In vitro, PSN632408 acts as a selective GPR119 agonist. Its activity is demonstrated in cell-based assays where it activates the receptor, leading to downstream signaling. It shows similar potency to OEA at both recombinant mouse and human GPR119 receptors, with EC50 values of 5.6 µM and 7.9 µM, respectively. This agonistic activity is the basis for its biological effects, which include stimulating beta cell replication and improving islet transplant function. |
| ln Vivo |
PSN632408 (100 mg/kg; PO; once daily for 14 days) inhibits food intake in rats and reduces body weight gain and white adipose tissue deposition following subchronic oral administration in high-fat-fed rats [1] .
In vivo, PSN632408 has demonstrated efficacy in rodent models. It suppresses food intake, reduces weight gain, and decreases white adipose tissue deposition in rats. These effects are consistent with the role of GPR119 in regulating appetite and metabolism. Its oral bioavailability makes it suitable for in vivo studies. These findings support its potential for treating obesity and related metabolic abnormalities. Furthermore, it shows potential for improving islet transplant function. |
| Enzyme Assay |
Cell-free assays for PSN632408 primarily involve radioligand binding studies to determine its affinity for the GPR119 receptor. Membranes are prepared from cells that overexpress the human or mouse GPR119 receptor. These membranes are then incubated with a radiolabeled GPR119 ligand and increasing concentrations of PSN632408. After incubation, the bound and free radioligand are separated, and the radioactivity is measured to calculate the inhibition constant (Ki). While specific Ki values are not provided in the summaries, the EC50 values for its agonistic activity are reported from cell-based functional assays.
|
| Cell Assay |
In vitro cell-based assays for PSN632408 are designed to measure its agonistic activity at the GPR119 receptor. A common method is to use cells that express GPR119 and a reporter gene (e.g., luciferase) under the control of a cAMP-responsive element (CRE). Upon activation of GPR119, which is a Gs-coupled receptor, intracellular cAMP levels increase, leading to reporter gene expression. Cells are treated with varying concentrations of PSN632408, and the luciferase activity is measured. The EC50, the concentration that produces 50% of the maximal response, is calculated from the dose-response curve.
|
| Animal Protocol |
Animal/Disease Models: Diet-induced obesity (DIO) rats [1]
Doses: 100 mg/kg Route of Administration: Oral; one time/day for 14 days Experimental Results: Average daily food intake diminished by 10% during the first week of administration , average daily food intake diminished by 15% during the second week. From day 6 onwards, weight gain was Dramatically attenuated and there was some evidence of weight loss. In vivo animal experiments for PSN632408 are conducted to study its effects on metabolism. In one study, the compound was administered orally to rats. Food intake and body weight were monitored over a period of time. The effects on adipose tissue were also assessed by measuring the weight of white adipose tissue deposits. For studies on beta cell replication and islet function, the compound would be administered to diabetic animal models, and its effect on glucose homeostasis, insulin secretion, and islet mass would be evaluated. |
| ADME/Pharmacokinetics |
Pharmacokinetic (PK) data for PSN632408 indicates that it is orally bioactive, suggesting it has sufficient oral bioavailability. Its solubility is 10 mM in DMSO. For in vivo use, it can be formulated, for example, in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline. Detailed PK parameters such as Cmax, Tmax, half-life, and AUC are not provided in the available literature. The compound is typically stored as a powder at -20°C.
|
| Toxicity/Toxicokinetics |
Toxicological data for PSN632408 is not extensively documented in the public literature. As a research compound targeting metabolic pathways, its safety profile would be a critical factor in its development. However, no specific LD50, organ toxicity, or genotoxicity data are available. Its use is strictly for research purposes and not for human consumption. All information is for research reference and not for diagnostic or clinical use.
|
| References |
|
| Additional Infomation |
PSN632408 is a research-grade compound used to study the role of the GPR119 receptor in glucose metabolism and appetite regulation. It is a valuable tool for validating GPR119 as a therapeutic target for type 2 diabetes and obesity. Its ability to stimulate beta cell replication and improve islet transplant function makes it particularly relevant for diabetes research. It has not been approved for clinical use. All information is for research reference and not for diagnostic or clinical use.
|
| Molecular Formula |
C18H24N4O4
|
|---|---|
| Molecular Weight |
360.414
|
| Exact Mass |
360.179
|
| CAS # |
857652-30-3
|
| PubChem CID |
11462546
|
| Appearance |
White to off-white solid powder
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
513.8±60.0 °C at 760 mmHg
|
| Flash Point |
264.5±32.9 °C
|
| Vapour Pressure |
0.0±1.3 mmHg at 25°C
|
| Index of Refraction |
1.564
|
| LogP |
2.19
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
26
|
| Complexity |
457
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
LHZWKWCEAXQUMX-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C18H24N4O4/c1-18(2,3)25-17(23)22-10-6-14(7-11-22)24-12-15-20-16(21-26-15)13-4-8-19-9-5-13/h4-5,8-9,14H,6-7,10-12H2,1-3H3
|
| Chemical Name |
tert-butyl 4-[(3-pyridin-4-yl-1,2,4-oxadiazol-5-yl)methoxy]piperidine-1-carboxylate
|
| Synonyms |
PSN-632408; PSN 632408; PSN632408
|
| 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 |
| 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) |
DMSO : ~50 mg/mL (~138.73 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.94 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.94 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.94 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7746 mL | 13.8731 mL | 27.7462 mL | |
| 5 mM | 0.5549 mL | 2.7746 mL | 5.5492 mL | |
| 10 mM | 0.2775 mL | 1.3873 mL | 2.7746 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
