| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
Succinate/succinate receptor antagonist 1 targets the succinate receptor 1 (SUCNR1), also known as GPR91. SUCNR1 is a G protein-coupled receptor that is activated by succinate, a metabolite of the citric acid cycle. By blocking this receptor, the antagonist aims to reduce inflammatory responses and potentially modulate disease pathways associated with metabolic disorders, cardiovascular diseases, and certain cancers. The compound inhibits SUCNR1 activation with an IC₅₀ of 20 μM.
|
|---|---|
| ln Vitro |
In vitro, succinate/succinate receptor antagonist 1 inhibits the activation of succinate receptor 1 (SUCNR1) with an IC₅₀ of 20 μM. It blocks succinate signaling in gingival tissue. The compound may be utilized in the study of periodontal disease. As a selective antagonist of SUCNR1, it effectively inhibits its activation. The compound is a synthetic antagonist designed to interrupt succinate-mediated signaling pathways.
|
| ln Vivo |
Succinate/succinate receptor antagonist 1 is not a pharmacologically approved drug and does not have established in vivo therapeutic activity. It is a research compound used to study the role of succinate signaling in various disease models. By blocking SUCNR1, the antagonist aims to reduce inflammatory responses and potentially modulate disease pathways associated with metabolic disorders, cardiovascular diseases, and certain cancers. The compound may be utilized in the study of periodontal disease.
|
| Enzyme Assay |
In vitro receptor binding assays for succinate/succinate receptor antagonist 1 typically involve competition binding studies with radiolabeled succinate or other ligands. A standard protocol involves preparing membranes from cells expressing SUCNR1 and incubating them with varying concentrations of the test compound (typically 0.1-100 µM) and a radiolabeled ligand. Non-specific binding is determined in the presence of excess unlabeled succinate. Bound radioactivity is separated by filtration and quantified by scintillation counting. IC₅₀ values are calculated from dose-response curves.
|
| Cell Assay |
In vitro cell culture experiments with succinate/succinate receptor antagonist 1 typically involve cells expressing SUCNR1. Cells are cultured in appropriate media and treated with the compound at concentrations ranging from 0.1-100 µM for 24-72 hours. Succinate-induced signaling (e.g., calcium mobilization, cAMP levels) is measured to assess receptor inhibition. Cell viability is assessed using MTT assays to ensure that observed effects are not due to cytotoxicity. The compound is soluble in DMSO (25 mg/mL).
|
| Animal Protocol |
In vivo animal studies with succinate/succinate receptor antagonist 1 are conducted to study its effects on inflammatory and metabolic disease models. A typical protocol involves administering the compound orally or intraperitoneally to rodents at doses ranging from 1-50 mg/kg. Blood and tissue samples are collected for analysis of inflammatory markers and metabolic parameters. The compound may be used in models of periodontal disease, metabolic disorders, and inflammatory conditions.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of succinate/succinate receptor antagonist 1 are not fully characterized. Based on its physicochemical properties (molecular weight 277.32, soluble in DMSO at 25 mg/mL), the compound would be expected to have moderate oral bioavailability. The compound should be stored as a powder at -20°C for 3 years or 4°C for 2 years, and in solvent at -80°C for 6 months or -20°C for 1 month. The compound requires protection from light.
|
| Toxicity/Toxicokinetics |
Succinate/succinate receptor antagonist 1 may cause skin and eye irritation. Standard laboratory safety precautions should be followed when handling this compound, including the use of gloves, safety glasses, and working in a fume hood. The compound should be stored in a cool, dry place away from light and moisture. No acute toxicity data are available. The compound is not intended for drug, household, or other uses.
|
| References | |
| Additional Infomation |
Succinate/succinate receptor antagonist 1 is a research compound used to study the succinate receptor (SUCNR1) signaling pathway. It is also known as compound 7a and 2-(4-(1,8-naphthyridin-2-yl)phenyl)-N-methylacetamide. The compound has potential applications in studying periodontal disease, metabolic disorders, and inflammatory conditions. It has not undergone clinical trials and is not approved as a pharmaceutical.
|
| Molecular Formula |
C17H15N3O
|
|---|---|
| Molecular Weight |
277.320503473282
|
| Exact Mass |
277.121
|
| CAS # |
2361972-29-2
|
| PubChem CID |
139308923
|
| Appearance |
White to off-white solid powder
|
| LogP |
2.3
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
21
|
| Complexity |
352
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1(CC(NC)=O)=CC=C(C2C=CC3C(N=2)=NC=CC=3)C=C1
|
| InChi Key |
CNTLNLSLKYIFRS-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C17H15N3O/c1-18-16(21)11-12-4-6-13(7-5-12)15-9-8-14-3-2-10-19-17(14)20-15/h2-10H,11H2,1H3,(H,18,21)
|
| Chemical Name |
N-methyl-2-[4-(1,8-naphthyridin-2-yl)phenyl]acetamide
|
| 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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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: 25 mg/mL (90.15 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.50 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 20.8 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: ≥ 2.08 mg/mL (7.50 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 20.8 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: ≥ 2.08 mg/mL (7.50 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 | 3.6059 mL | 18.0297 mL | 36.0594 mL | |
| 5 mM | 0.7212 mL | 3.6059 mL | 7.2119 mL | |
| 10 mM | 0.3606 mL | 1.8030 mL | 3.6059 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
