| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
Neuropeptide Y-Y5 (NPY-Y5) receptor. As an antagonist, GW438014A blocks the binding of neuropeptide Y to the Y5 receptor, thereby inhibiting the orexigenic (appetite-stimulating) effects of NPY signaling.
|
|---|---|
| ln Vitro |
GW438014A is a potent and selective antagonist of the NPY-Y5 receptor. Specific IC50 or Ki values for receptor binding are not provided in the available literature. Its activity is demonstrated by its ability to inhibit food intake in vivo.
|
| ln Vivo |
In a genetically dynamic ob/ob paradigm of spontaneous and sleep-induced food gain, GW438014A (10 mg/kg; ip; daily, for 7 d) decreases food-induced and NPY-induced food intake [1].
GW438014A inhibits food intake and reduces weight gain in obese rodents. These findings demonstrate its in vivo efficacy as an anti-obesity agent. It has also demonstrated utility in neuroscience research, specifically in models of epilepsy. |
| Enzyme Assay |
The in vitro assay for NPY-Y5 receptor antagonism involves measuring the ability of GW438014A to compete with radiolabeled NPY for binding to the Y5 receptor. The receptor is incubated with the radioligand and varying concentrations of GW438014A, and the amount of bound radioligand is measured. The IC50 or Ki value is determined.
|
| Cell Assay |
Specific in vitro cell-based assay protocols for GW438014A are not detailed. Its antagonist activity can be assessed in cells expressing the NPY-Y5 receptor by measuring the inhibition of NPY-induced signaling, such as calcium flux or cAMP modulation.
|
| Animal Protocol |
Animal/Disease Models: obese ob/ob mice [1]
Doses: 10 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day for 7 days. Experimental Results: The weight gain rate of lean rats and obese rats was diminished. GW438014A has been evaluated in obese rodent models. The compound is typically administered orally or intraperitoneally, and food intake and body weight are monitored. These studies have demonstrated its efficacy in reducing food intake and weight gain. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for GW438014A are not reported in the available literature. As an orally active compound, it is expected to have good bioavailability. Detailed PK parameters are not provided.
|
| Toxicity/Toxicokinetics |
Specific toxicological data for GW438014A are not available. As a research compound, its safety profile has not been comprehensively characterized. Toxicity studies would be required to determine its safety margin.
|
| References | |
| Additional Infomation |
GW438014A is a research tool for studying the role of NPY-Y5 receptor in appetite regulation, obesity, and energy homeostasis. It is also used in neuroscience research. It is not an approved therapeutic agent.
|
| Molecular Formula |
C23H23N3O4S
|
|---|---|
| Molecular Weight |
437.511424303055
|
| Exact Mass |
341.152
|
| CAS # |
469861-49-2
|
| PubChem CID |
6918627
|
| Appearance |
White to off-white solid powder
|
| LogP |
4.5
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
26
|
| Complexity |
456
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
S(C)(=O)(=O)O.O=C(C1C=CC=CC=1)NC1=NC2C=CC=CC=2N1CCC1C=CC=CC=1
|
| InChi Key |
CDUDZZGLFOFINU-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C22H19N3O/c26-21(18-11-5-2-6-12-18)24-22-23-19-13-7-8-14-20(19)25(22)16-15-17-9-3-1-4-10-17/h1-14H,15-16H2,(H,23,24,26)
|
| Chemical Name |
N-[1-(2-phenylethyl)benzimidazol-2-yl]benzamide
|
| Synonyms |
GW 438014 A; GW-438014-A; GW438014A
|
| 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 : ~250 mg/mL (~571.42 mM)
|
|---|---|
| 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 | 2.2857 mL | 11.4283 mL | 22.8566 mL | |
| 5 mM | 0.4571 mL | 2.2857 mL | 4.5713 mL | |
| 10 mM | 0.2286 mL | 1.1428 mL | 2.2857 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
