| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg |
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| 250mg | |||
| 500mg | |||
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| Targets |
MS0015203 specifically targets GPR171, a G protein-coupled receptor also known as the neuropeptide receptor. It acts as a potent and selective agonist, meaning it binds to and activates the receptor, mimicking the action of its endogenous ligands. By activating GPR171, MS0015203 modulates downstream signaling pathways that influence various physiological processes, including food intake, pain sensation, and neuronal activity.
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| ln Vitro |
In rat hypothalamus membranes, MS15203 (MS0015203) decreases adenylyl cyclase activity and dose-dependently enhances [[35]S]GTPγS binding [1].
In vitro, MS0015203 demonstrates high potency as a GPR171 agonist. It shows strong binding affinity with an IC₅₀ of 81 nM for the wild-type GPR171. The compound effectively stimulates GPR171-mediated signaling pathways in cell-based assays. Its high selectivity for GPR171 over other receptors makes it a specific tool for probing the function of this particular neuropeptide receptor system. This activity translates to various biological effects observed in cellular and animal models, such as increased neuronal activity. |
| ln Vivo |
GPR171-containing cells in the PVN exhibit enhanced neuronal activity in response to MS15203 (MS0015203) (3 mg/kg; i.p.) [1]. ..At 4 and 8 hours, MS15203 (3 mg/kg; i.p.) dramatically improves meal intake [1]. The intraperitoneal injection of MS15203 (3 mg/kg) dramatically raises the quantity of mRNA encoding proSAAS, NPY, and AgRP [1].
In vivo, MS0015203 has been shown to produce significant physiological effects in animal models. It increases food intake and body weight in mice, confirming the role of GPR171 in regulating appetite and energy balance. Furthermore, MS0015203 has been shown to increase the analgesic effect of morphine, suggesting a role for GPR171 in modulating pain pathways. It also reduces chronic neuropathic and inflammatory pain in male mice. These in vivo effects highlight the potential of GPR171 as a therapeutic target for conditions like chronic pain and eating disorders. |
| Enzyme Assay |
In vitro receptor binding and functional assays for MS0015203 are performed using cell lines engineered to express human GPR171. For binding assays, membranes from these cells are incubated with a radiolabeled ligand and varying concentrations of the compound. The amount of bound radioligand is measured to determine the compound's affinity (IC₅₀). Functional assays measure the activation of GPR171 by assessing downstream signaling, such as the accumulation of second messengers like cAMP or the recruitment of β-arrestin. The compound's potency (EC₅₀) and efficacy are determined from dose-response curves.
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| Cell Assay |
For cell-based assays, cells expressing GPR171 are cultured in standard media. Cells are seeded in multi-well plates and treated with MS0015203 at various concentrations for a defined period. Following treatment, GPR171 activation is measured using assays that detect downstream signaling events. The effects of the compound on cell signaling pathways can be further analyzed using techniques like Western blotting to detect the phosphorylation of specific signaling proteins. Cell viability is assessed using standard assays. All experiments include appropriate vehicle controls and are performed in triplicate.
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| Animal Protocol |
In vivo studies with MS0015203 are conducted in rodent models. The compound is typically administered via intraperitoneal (IP) or subcutaneous (SC) injection. For feeding studies, food intake and body weight are measured at various time points post-administration. For pain studies, the compound's ability to modulate pain sensitivity is assessed using behavioral tests like the hot plate test or the von Frey test. The effects on neuronal activity can be assessed by measuring the expression of immediate early genes like c-Fos in specific brain regions. All animal procedures must be conducted in accordance with institutional guidelines.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for MS0015203 are not extensively reported in public literature. As a small molecule with a molecular weight of 249.22, its properties are being studied. It is soluble in DMSO. The compound is typically stored as a powder at -20°C. For in vivo administration, it is formulated in suitable vehicles. A comprehensive pharmacokinetic profile, including absorption, distribution, metabolism, and excretion, is essential for interpreting its in vivo effects.
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| Toxicity/Toxicokinetics |
Toxicological data for MS0015203 are limited. As a research compound, its safety profile is not fully characterized. The compound is intended for research use only and is not for human consumption. Any potential toxicity would be related to its on-target effects on GPR171 signaling. Comprehensive toxicology studies would be necessary for any future therapeutic development.
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| References | |
| Additional Infomation |
GPR71 antagonist; structure can be found in the first article.
MS0015203 is a research-grade chemical probe and its primary application is in the study of the GPR171 neuropeptide receptor system. It is a critical tool for investigating the role of GPR171 in various physiological processes, including feeding, pain, and anxiety. The compound is not an approved drug and has not entered clinical trials. It is commercially available from various chemical suppliers for research purposes only. Its discovery has provided a valuable tool to understand the therapeutic potential of targeting GPR171. |
| Molecular Formula |
C12H11NO5
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|---|---|
| Molecular Weight |
249.22
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| Exact Mass |
249.064
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| CAS # |
73912-52-4
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| PubChem CID |
773544
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| Appearance |
White to off-white solid powder
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| Density |
1.42g/cm3
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| Boiling Point |
561.3ºC at 760 mmHg
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| Flash Point |
293.2ºC
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| Index of Refraction |
1.639
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| LogP |
1.67
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
18
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| Complexity |
368
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(=C)C(=O)NC1=CC(=CC(=C1)C(=O)O)C(=O)O
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| InChi Key |
NVOBVSWSDYFEMR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H11NO5/c1-6(2)10(14)13-9-4-7(11(15)16)3-8(5-9)12(17)18/h3-5H,1H2,2H3,(H,13,14)(H,15,16)(H,17,18)
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| Chemical Name |
5-(2-methylprop-2-enoylamino)benzene-1,3-dicarboxylic acid
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| Synonyms |
MS 0015203; MS-0015203; MS0015203
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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 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)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~200.63 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.03 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 (10.03 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0125 mL | 20.0626 mL | 40.1252 mL | |
| 5 mM | 0.8025 mL | 4.0125 mL | 8.0250 mL | |
| 10 mM | 0.4013 mL | 2.0063 mL | 4.0125 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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