Peturadol
Based on 1 Customer Validation
NB001 (HTS 09836) is an adenylcyclase 1 (AC1) inhibitor which has effect on neural and non-neural pain by modulating AC1 activity.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.91%
- No. CAS: 686301-48-4
- Fòrmula: C12H20N6O
- Peso molecular:264.33
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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Actividad biológica
AC1[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
10 μM
Compound: NB001
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Inhibition of AC1 (unknown origin) expressed in HEK293 cells assessed as decrease in Ca2+/calmodulin-mediated cAMP accumulation by enzyme immunoassay
Inhibition of AC1 (unknown origin) expressed in HEK293 cells assessed as decrease in Ca2+/calmodulin-mediated cAMP accumulation by enzyme immunoassay
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[PMID: 30472604] |
Peturadol (0.1-200μM, 15-30 min) inhibits AC1 mediated cAMP production in mouse anterior cingulate cortex (ACC) slices with an IC50 of 5.1 μM, inhibits AC1 mediated cAMP production in SH-SY5Y cell with an IC50 of 8.3 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SH-SY5Y
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Concentration:0.1-200μM
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Incubation Time:15-30 min
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Result:Inhibited cAMP production.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MPTP (HY-15608)-induced mouse Parkinson’s disease models[2]
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Dosage:20-40 mg/kg
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Administration:po, single dose
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Result:Reduced pain-related and anxiety-related behaviors.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 686301-48-4
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Appearance Solid
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Peso molecular 264.33
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Fòrmula C12H20N6O
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Color White to pink
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SMILES
OCCCCCNCCN1C=NC2=C(N)N=CN=C12
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Synonyms
HTS 09836; NB001
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 50 mg/mL (189.16 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 1.25 mg/mL (4.73 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (4.73 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
Pureza y Documentación
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Ficha de datos (270 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Min Zhuo. Method for treating neuronal and non-neuronal pain. US8124599B2.
[2]. Wang H, et al., Identification of an adenylyl cyclase inhibitor for treating neuropathic and inflammatory pain. Sci Transl Med. 2011 Jan 12;3(65):65ra3. [Content Brief]
[3]. Zhou Z, et al., Inhibition of calcium-stimulated adenylyl cyclase subtype 1 (AC1) for the treatment of pain and anxiety symptoms in Parkinson's disease mice model. Mol Pain. 2024 Jan-Dec;20:17448069241266683. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.7832 mL | 18.9158 mL | 37.8315 mL | 94.5788 mL |
| 5 mM | 0.7566 mL | 3.7832 mL | 7.5663 mL | 18.9158 mL | |
| 10 mM | 0.3783 mL | 1.8916 mL | 3.7832 mL | 9.4579 mL | |
| 15 mM | 0.2522 mL | 1.2611 mL | 2.5221 mL | 6.3053 mL | |
| 20 mM | 0.1892 mL | 0.9458 mL | 1.8916 mL | 4.7289 mL | |
| 25 mM | 0.1513 mL | 0.7566 mL | 1.5133 mL | 3.7832 mL | |
| 30 mM | 0.1261 mL | 0.6305 mL | 1.2611 mL | 3.1526 mL | |
| 40 mM | 0.0946 mL | 0.4729 mL | 0.9458 mL | 2.3645 mL | |
| 50 mM | 0.0757 mL | 0.3783 mL | 0.7566 mL | 1.8916 mL | |
| 60 mM | 0.0631 mL | 0.3153 mL | 0.6305 mL | 1.5763 mL | |
| 80 mM | 0.0473 mL | 0.2364 mL | 0.4729 mL | 1.1822 mL | |
| 100 mM | 0.0378 mL | 0.1892 mL | 0.3783 mL | 0.9458 mL |
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