| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
GPR139 ( IC50 = 640 nM )
LP-471756 targets the GPR139 receptor, acting as a specific antagonist. It inhibits LP-360924-stimulated cAMP production with an IC50 of 640 nM. By blocking GPR139 activation, it prevents downstream signaling through the cAMP pathway. |
|---|---|
| ln Vitro |
LP-471756 (0-1000 µM) nacre suppresses cAMP production in GPR139 cells in response to LP-360924 stimulation with an IC50 value of 0.64 µM[2].
LP-471756 inhibits LP-360924-stimulated cAMP production in GPR139-expressing cells with an IC50 of 640 nM (0.64 μM). It is a specific antagonist of GPR139. In vitro activity is confirmed through cAMP assays in cells expressing GPR139. |
| ln Vivo |
C in vivo activity data for LP-471756 are limited in the available literature. As a research tool compound, its primary use is in vitro for studying GPR139 signaling pathways. In vivo studies would be required to assess therapeutic potential.
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| Enzyme Assay |
Non-cell-based assays for LP-471756 are not typical, as the compound acts as a receptor antagonist. Receptor binding studies may be performed using membrane preparations from cells expressing GPR139 and radiolabeled ligands. Binding affinity (Ki) would be determined by measuring displacement of the radiolabeled ligand.
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| Cell Assay |
Cellular assays for LP-471756 utilize cells expressing GPR139. Cells are treated with the compound at various concentrations (0-1000 μM), followed by stimulation with LP-360924 (a GPR139 agonist). cAMP levels are measured using immunoassays (ELISA or HTRF) or reporter gene assays. IC50 values for inhibition of cAMP production are determined.
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| Animal Protocol |
In vivo animal models for LP-471756 would be required to assess its therapeutic potential. As a GPR139 antagonist, it could be studied in models relevant to GPR139 biology. However, detailed in vivo protocols are not reported in the available literature. The compound is primarily a research tool for in vitro studies.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of LP-471756 include CAS number 413605-11-5. The compound is a small molecule GPR139 antagonist. Purity is 99.53%. Detailed PK parameters such as half-life and bioavailability are not extensively reported. The compound is a research tool for GPR139 studies.
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| Toxicity/Toxicokinetics |
LP-471756 is a potent GPR139 antagonist. It inhibits LP-360924-stimulated cAMP production. Detailed toxicity data are not extensively reported. The compound is a research tool for studying GPR139 signaling pathways and related biological processes.
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| References | |
| Additional Infomation |
LP-471756 is a potent GPR139 antagonist. It has CAS number 413605-11-5. The compound inhibits LP-360924-stimulated cAMP production with an IC50 of 640 nM. It is a specific antagonist of GPR139. It is used as a research tool for GPR139 signaling studies.
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| Molecular Formula |
C19H23NO2S
|
|---|---|
| Molecular Weight |
329.456423997879
|
| Exact Mass |
329.14
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| Elemental Analysis |
C, 69.27; H, 7.04; N, 4.25; O, 9.71; S, 9.73
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| CAS # |
413605-11-5
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| PubChem CID |
789353
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| Appearance |
White to off-white solid powder
|
| LogP |
5.2
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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 |
4
|
| Heavy Atom Count |
23
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| Complexity |
456
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC=CC=C1NS(=O)(=O)C2=CC=C(C=C2)C3CCCCC3
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| InChi Key |
STLMNZVBCJVQOZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H23NO2S/c1-15-7-5-6-10-19(15)20-23(21,22)18-13-11-17(12-14-18)16-8-3-2-4-9-16/h5-7,10-14,16,20H,2-4,8-9H2,1H3
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| Chemical Name |
4-cyclohexyl-N-(2-methylphenyl)benzenesulfonamide
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| Synonyms |
LP 471756; LP-471756; LP471756
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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: ~250 mg/mL (~758.8 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (6.31 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (6.31 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 (6.31 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 | 3.0353 mL | 15.1763 mL | 30.3527 mL | |
| 5 mM | 0.6071 mL | 3.0353 mL | 6.0705 mL | |
| 10 mM | 0.3035 mL | 1.5176 mL | 3.0353 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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