SBI-553
Based on 1 publication(s) in Google Scholar
SBI-553 is a potent and brain penetrant NTR1 allosteric modulator, with an EC50 of 0.34 μM.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.73%
- CAS No.: 1849603-72-0
- Formule: C26H31FN4O2
- Masse moléculaire:450.55
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Targeted Diversity Library
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Membrane Protein-targeted Compound Library
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Membrane Receptor-targeted Compound Library
HY-L150
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Allosteric Modulators (AMs) Compound Library
HY-L170
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
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Bioactive Compound Library
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Lactylation Compound Library
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Publications Citing Use of MedChemExpress (MCE) SBI-553
More
Activité biologique
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NTR1 |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | EC50 |
0.14 μM
Compound: 18; SBI-553
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Positive allosteric modulation of recombinant human NTR1 expressed in HEK293 cells assessed as increase in [125I]-neurotensin binding measured after 45 mins
Positive allosteric modulation of recombinant human NTR1 expressed in HEK293 cells assessed as increase in [125I]-neurotensin binding measured after 45 mins
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[PMID: 31390201] |
SBI-553 (0.03-30 μM) induces β-blocking protein recruitment and NTSR1 internalization, but does not stimulate Gq protein activation, 1,4, 5-triphosphate (IP3) production or calcium mobilization[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1849603-72-0
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Appearance Solid
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Masse moléculaire 450.55
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Formule C26H31FN4O2
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Color Light yellow to yellow
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SMILES
CN(C1=CC2=C(N=C(N=C2C=C1)C3(CC3)F)N4CCC(CC4)C5=C(C=CC=C5)OC)CCO
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Sci Signal
2023 Feb 14;16(772):eabq7842. PMID: 36787384
Solvant et solubilité
DMSO : 17 mg/mL (37.73 mM; ultrasonic and warming and heat to 80°C; 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: ≥ 2.08 mg/mL (4.62 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.62 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Pureté et documentation
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Fiche technique (277 KB)
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SDS (642 KB)
- English - EN (642 KB)
- Français - FR (642 KB)
- Deutsch - DE (642 KB)
- Norwegian - NO (642 KB)
- Español - ES (642 KB)
- Swedish - SV (642 KB)
- Italian - IT (642 KB)
- Korean - KR (642 KB)
- Portuguese - PT (642 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Pinkerton AB, et al. Discovery of β-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators. J Med Chem. 2019 Aug 20. [Content Brief]
[2]. Slosky LM, et al. β-Arrestin-Biased Allosteric Modulator of NTSR1 Selectively Attenuates Addictive Behaviors. Cell. 2020 Jun 11;181(6):1364-1379.e14. [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 |
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| DMSO | 1 mM | 2.2195 mL | 11.0975 mL | 22.1951 mL | 55.4877 mL |
| 5 mM | 0.4439 mL | 2.2195 mL | 4.4390 mL | 11.0975 mL | |
| 10 mM | 0.2220 mL | 1.1098 mL | 2.2195 mL | 5.5488 mL | |
| 15 mM | 0.1480 mL | 0.7398 mL | 1.4797 mL | 3.6992 mL | |
| 20 mM | 0.1110 mL | 0.5549 mL | 1.1098 mL | 2.7744 mL | |
| 25 mM | 0.0888 mL | 0.4439 mL | 0.8878 mL | 2.2195 mL | |
| 30 mM | 0.0740 mL | 0.3699 mL | 0.7398 mL | 1.8496 mL |
SBI-553 Related Classifications
HY-125880 Related Classifications
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