| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
MS21570 specifically targets GPR171, acting as a selective antagonist. It inhibits GPR171 with an IC₅₀ of 220 nM. By binding to the receptor, MS21570 prevents its activation by endogenous neuropeptides like BigLEN. This blockade allows researchers to investigate the consequences of inhibiting GPR171 signaling in various biological systems, providing insights into its function in the central nervous system.
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| ln Vitro |
In vitro, MS21570 demonstrates selective antagonist activity at GPR171. It inhibits BigLEN-mediated increases in [³⁵S]GTPγS binding in hypothalamic membranes, a measure of G protein activation. This confirms its ability to block receptor signaling at a functional level. The compound's selectivity for GPR171 makes it a specific tool for studying this receptor without off-target effects on other GPCRs. Its activity in biochemical assays is well-characterized, providing a solid foundation for its use as a research tool.
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| ln Vivo |
MS21570 dramatically reduced the increase in food intake mediated by CNO. Interestingly, compared to vehicle, MS21570 significantly increased center time, indicating an impact on anxiety-like behavior. The raised plus maze showed an increase in open-arm time following intra-BLA administration of MS21570, but no change in locomotor activity was observed during the test. Interestingly, MS21570 considerably reduced freezing evaluated 24 hours later when given prior to and right after fear conditioning. The pharmacokinetic and pharmacodynamic characteristics of MS21570 may be the cause of the behavioral variations seen between systemic and intra-BLA treatment. To fully describe GPR171 antagonists, more research is required [1].
In vivo, MS21570 has been shown to produce significant behavioral effects in animal models. It dramatically reduces the increase in food intake mediated by a GPR171 agonist, confirming its antagonistic activity in a physiological context. Furthermore, MS21570 has been shown to affect anxiety-like behavior, as indicated by a significant increase in center time in an open field test. It also increases open arm time in the elevated plus maze and attenuates freezing in a fear conditioning paradigm. These effects highlight the role of GPR171 in regulating anxiety and fear. |
| Enzyme Assay |
In vitro receptor binding and functional assays for MS21570 are performed using cell lines expressing 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 compound's ability to antagonize GPR171 activation by measuring downstream signaling, such as [³⁵S]GTPγS binding. The compound's potency (IC₅₀) is 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 pre-treated with MS21570 at various concentrations before stimulation with an agonist like BigLEN. The ability of MS21570 to block agonist-induced signaling is then measured using assays that detect downstream signaling events. 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 MS21570 are conducted in rodent models. The compound is typically administered via intraperitoneal (IP) injection or directly into the brain (e.g., intra-BLA). For feeding studies, food intake is measured. For anxiety and fear studies, behavioral tests like the elevated plus maze, open field test, and fear conditioning are performed. The effects on neuronal activity can be assessed by measuring immediate early gene expression. All animal procedures must be conducted in accordance with institutional guidelines.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for MS21570 are not extensively reported in public literature. The compound has a molecular weight of 237.34 and is soluble in DMSO and ethanol. It is typically stored as a powder at -20°C. For in vivo administration, it is formulated in suitable vehicles. A comprehensive pharmacokinetic profile is essential for interpreting its in vivo effects.
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| Toxicity/Toxicokinetics |
Toxicological data for MS21570 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 |
MS21570 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 anxiety, fear, and feeding behaviors. 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.
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| Molecular Formula |
C10H11N3S2
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|---|---|
| Molecular Weight |
237.33
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| Exact Mass |
237.039
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| CAS # |
65373-29-7
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| PubChem CID |
805117
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
389.6±35.0 °C at 760 mmHg
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| Flash Point |
189.4±25.9 °C
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| Vapour Pressure |
0.0±0.9 mmHg at 25°C
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| Index of Refraction |
1.654
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| LogP |
2.98
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
15
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| Complexity |
186
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CNC1=NN=C(S1)SCC2=CC=CC=C2
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| InChi Key |
KFLNRVSOQJTXDG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H11N3S2/c1-11-9-12-13-10(15-9)14-7-8-5-3-2-4-6-8/h2-6H,7H2,1H3,(H,11,12)
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| Chemical Name |
5-benzylsulfanyl-N-methyl-1,3,4-thiadiazol-2-amine
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| Synonyms |
MS 21570; MS-21570; MS21570
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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 : ~125 mg/mL (~526.67 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.53 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 (10.53 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 25.0 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: ≥ 2.5 mg/mL (10.53 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 | 4.2135 mL | 21.0677 mL | 42.1354 mL | |
| 5 mM | 0.8427 mL | 4.2135 mL | 8.4271 mL | |
| 10 mM | 0.4214 mL | 2.1068 mL | 4.2135 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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