ML314
Based on 1 Customer Validation
ML314 is a potent, BBB-penetrant and β-arrestin biased molecule agonist of NTR1 (EC50 = 1.9 μM). ML314 shows good selectivity against NTR2 and GPR35, but does not stimulate Ca2+ mobilization. ML314 can attenuate amphetamine-like hyperlocomotion in dopamine transporter knockout mice. ML314 attenuates methamphetamine-associated hyperlocomotion and potentiates the psychostimulant inhibitory effects of a ghrelin antagonist in wild type mouse model. ML314 also acts as an allosteric enhancer of endogenous neurotensin. ML314 antagonizes G protein signaling. ML314 can be studied in research for methamphetamine abuse conditions.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.52%
- No. CAS: 1448895-09-7
- Fòrmula: C24H28N4O3
- Peso molecular:420.50
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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GPCR/G Protein Compound Library
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Actividad biológica
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NTR1 |
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Cell Line
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Type | Value | Description | References |
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| CHO | EC50 |
>80 μM
Compound: 32, ML314
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Agonist activity at NTR1 (unknown origin) expressed in CHO cells assessed as stimulation of calcium flux
Agonist activity at NTR1 (unknown origin) expressed in CHO cells assessed as stimulation of calcium flux
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[PMID: 24611085] |
| CHO | EC50 |
2 μM
Compound: 3, ML314
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Agonist activity at NTSR1 (unknown origin) expressed in CHO cells assessed as potentiation of NT(8-13) peptide-induced change in intracellular Ca2+ level preincubated for 45 mins by FLIPR assay
Agonist activity at NTSR1 (unknown origin) expressed in CHO cells assessed as potentiation of NT(8-13) peptide-induced change in intracellular Ca2+ level preincubated for 45 mins by FLIPR assay
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[PMID: 24997685] |
| CHO-K1 | EC50 |
3.41 μM
Compound: 32, ML314
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Agonist activity at NTR1 (unknown origin) expressed in CHOK1 cells by beta-arrestin assay
Agonist activity at NTR1 (unknown origin) expressed in CHOK1 cells by beta-arrestin assay
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[PMID: 24611085] |
| U2OS | EC50 |
>40 μM
Compound: 32, ML314
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Agonist activity at GPR35 (unknown origin) expressed in human U2OS cells coexpressing beta-arrestin by GFP reporter gene assay
Agonist activity at GPR35 (unknown origin) expressed in human U2OS cells coexpressing beta-arrestin by GFP reporter gene assay
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[PMID: 24611085] |
| U2OS | EC50 |
>80 μM
Compound: 32, ML314
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Agonist activity at NTR2 (unknown origin) expressed in human U2OS cells coexpressing beta-arrestin by GFP reporter gene assay
Agonist activity at NTR2 (unknown origin) expressed in human U2OS cells coexpressing beta-arrestin by GFP reporter gene assay
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[PMID: 24611085] |
| U2OS | EC50 |
2 μM
Compound: 32, ML314
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Agonist activity at NTR1 (unknown origin) expressed in human U2OS cells coexpressing beta-arrestin by GFP reporter gene assay
Agonist activity at NTR1 (unknown origin) expressed in human U2OS cells coexpressing beta-arrestin by GFP reporter gene assay
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[PMID: 24611085] |
ML314 (10 μM) induces aggregation of β-arrestin in NTR1β-arrestin2/GFP containing U2OS cells[2].
ML314 (10 μM, 10 min) antagonizes G protein signaling in HEK293 cells expressing NTR1[2].
ML314 (2 μM) increases the number of NTR1 binding in U2OS cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
ML314 (10-30 mg/kg, i.p., single dose) reduces hyperlocomotion and conditioned place preference in C57BL/6J mice exposed to Methamphetamine[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice exposed to Methamphetamine[2]
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Dosage:10, 20, 30 mg/kg
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Administration:Intraperitoneal injection (i.p.)
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Result:Reduced 30% of the conditioned place preference.
Reduced the amplitude of the locomotion displacement curves compared to control group.
Chemical Information
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No. CAS 1448895-09-7
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Appearance Solid
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Peso molecular 420.50
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Fòrmula C24H28N4O3
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Color Light yellow to yellow
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SMILES
COC1=CC=CC=C1N2CCN(C3=C4C=C(OC)C(OC)=CC4=NC(C5CC5)=N3)CC2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvente y solubilidad
DMSO : 50 mg/mL (118.91 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (5.95 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Hershberger P, et al. Small Molecule Agonists for the Neurotensin 1 Receptor (NTR1 Agonists). Probe Reports from the NIH Molecular Libraries Program [Content Brief]
[2]. Barak, L. S., et al., (2016). ML314: A Biased Neurotensin Receptor Ligand for Methamphetamine Abuse. ACS chemical biology, 11(7), 1880–1890. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3781 mL | 11.8906 mL | 23.7812 mL | 59.4530 mL |
| 5 mM | 0.4756 mL | 2.3781 mL | 4.7562 mL | 11.8906 mL | |
| 10 mM | 0.2378 mL | 1.1891 mL | 2.3781 mL | 5.9453 mL | |
| 15 mM | 0.1585 mL | 0.7927 mL | 1.5854 mL | 3.9635 mL | |
| 20 mM | 0.1189 mL | 0.5945 mL | 1.1891 mL | 2.9727 mL | |
| 25 mM | 0.0951 mL | 0.4756 mL | 0.9512 mL | 2.3781 mL | |
| 30 mM | 0.0793 mL | 0.3964 mL | 0.7927 mL | 1.9818 mL | |
| 40 mM | 0.0595 mL | 0.2973 mL | 0.5945 mL | 1.4863 mL | |
| 50 mM | 0.0476 mL | 0.2378 mL | 0.4756 mL | 1.1891 mL | |
| 60 mM | 0.0396 mL | 0.1982 mL | 0.3964 mL | 0.9909 mL | |
| 80 mM | 0.0297 mL | 0.1486 mL | 0.2973 mL | 0.7432 mL | |
| 100 mM | 0.0238 mL | 0.1189 mL | 0.2378 mL | 0.5945 mL |
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