| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg |
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| Targets |
GPR132（EC50= 0.075 μM）
insulin secretion activity(EC50= 0.7 μM) GPR132 antagonist 1 targets the G protein-coupled receptor GPR132. The compound acts as an antagonist at this receptor, with an EC50 of 0.075 μM. GPR132 is a proton-sensing GPCR involved in various physiological processes, and its antagonism has been shown to enhance insulin secretion. |
|---|---|
| ln Vitro |
In vitro, GPR132 antagonist 1 has been shown to promote insulin secretion with an EC50 of 0.7 μM. Its activity as a GPR132 antagonist has been characterized, and it is a valuable tool for studying the role of GPR132 in metabolic regulation. The compound's in vitro activity is well documented.
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| ln Vivo |
In vivo data for GPR132 antagonist 1 are limited. As a research compound, its in vivo effects have not been extensively reported. However, its ability to promote insulin secretion in vitro suggests potential for in vivo applications in metabolic research. Further studies are needed to characterize its in vivo efficacy.
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| Enzyme Assay |
In vitro receptor binding assays for GPR132 antagonist 1 typically involve measuring its ability to displace a radiolabeled ligand from GPR132 or assessing its functional antagonism in a cell-based assay. The compound's EC50 of 0.075 μM for GPR132 has been determined using such methods.
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| Cell Assay |
In vitro cellular assays for GPR132 antagonist 1 involve treating cells expressing GPR132 with the compound and measuring its effect on receptor signaling. Functional assays may include measurement of intracellular calcium mobilization or cAMP levels. The compound's ability to promote insulin secretion can be assessed using insulin-secreting cell lines.
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| Animal Protocol |
In vivo animal studies for GPR132 antagonist 1 would typically involve administration to rodent models to evaluate its effects on glucose metabolism and insulin secretion. Doses and routes of administration would vary depending on the study design. However, such studies are not well documented in the available literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for GPR132 antagonist 1 are limited. As a small molecule with a molecular weight of 359.4 and a LogP of 3.5, the compound is expected to have reasonable oral bioavailability and tissue distribution. Specific PK parameters such as half-life and Cmax have not been reported.
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| Toxicity/Toxicokinetics |
Toxicological data for GPR132 antagonist 1 are limited. As a research compound, comprehensive toxicological assessments have not been reported. The compound is intended for research use only and is not intended for human therapeutic use. Standard safety precautions should be taken when handling the compound.
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| References | |
| Additional Infomation |
GPR132 antagonist 1 is a research tool for studying GPR132 biology and metabolic regulation. It is a selective GPR132 antagonist with an EC50 of 0.075 μM and has been shown to promote insulin secretion with an EC50 of 0.7 μM. The compound is not approved for clinical use and is intended for research purposes only.
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| Molecular Formula |
C18H17NO5S
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|---|---|
| Molecular Weight |
359.396283864975
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| Exact Mass |
359.082
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| CAS # |
898211-21-7
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| PubChem CID |
4319354
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| Appearance |
White to off-white solid powder
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| LogP |
3.5
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
25
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| Complexity |
567
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC1=C(OC2=C1C=C(C=C2)S(=O)(=O)NCCC3=CC=CC=C3)C(=O)O
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| InChi Key |
XFMCZHXUAWBOAL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H17NO5S/c1-12-15-11-14(7-8-16(15)24-17(12)18(20)21)25(22,23)19-10-9-13-5-3-2-4-6-13/h2-8,11,19H,9-10H2,1H3,(H,20,21)
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| Chemical Name |
3-methyl-5-(2-phenylethylsulfamoyl)-1-benzofuran-2-carboxylic acid
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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) |
DMSO : ≥ 100 mg/mL (~278.24 mM)
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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 | 2.7824 mL | 13.9121 mL | 27.8242 mL | |
| 5 mM | 0.5565 mL | 2.7824 mL | 5.5648 mL | |
| 10 mM | 0.2782 mL | 1.3912 mL | 2.7824 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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