NP118809
Based on 1 Customer Validation
NP118809 is a potent N-type calcium channel blocker, with an IC50 of 0.11 μM; also less potently inhibits L-type calcium channel with an IC50 of 12.2 μM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.73%
- No. CAS: 41332-24-5
- Fòrmula: C32H32N2O
- Peso molecular:460.61
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Almacenamiento: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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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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Ver todos los productos específicos de isoformas Calcium Channel
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Actividad biológica
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N-type calcium channel 0.11 μM (IC50) |
L-type calcium channel 12.2 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.11 μM
Compound: 2b, NP118809
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Blocking of rat N-type calcium channel alpha-1B/alpha-2-delta-1/beta-1b activity expressed in HEK293 cells assessed as whole cell current by whole cell patch clamp assay
Blocking of rat N-type calcium channel alpha-1B/alpha-2-delta-1/beta-1b activity expressed in HEK293 cells assessed as whole cell current by whole cell patch clamp assay
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[PMID: 19815411] |
| HEK293 | IC50 |
0.11 μM
Compound: NP-118809
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Inhibition of N type calcium channel alpha-1b/alpha-2-delta-1/beta-1b expressed in HEK293 cells at holding potential of -100 mV by whole-cell patch clamp method
Inhibition of N type calcium channel alpha-1b/alpha-2-delta-1/beta-1b expressed in HEK293 cells at holding potential of -100 mV by whole-cell patch clamp method
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[PMID: 20117000] |
| HEK293 | IC50 |
12.2 μM
Compound: 2b, NP118809
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Blocking of rat Voltage-dependent L-type calcium channel alpha1c/alpha2delta-1/beta1b activity expressed in HEK293 cells assessed as whole cell current by whole cell patch clamp assay
Blocking of rat Voltage-dependent L-type calcium channel alpha1c/alpha2delta-1/beta1b activity expressed in HEK293 cells assessed as whole cell current by whole cell patch clamp assay
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[PMID: 19815411] |
| HEK293 | IC50 |
12.2 μM
Compound: NP-118809
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Inhibition of L type calcium channel alpha-1c/alpha-2-delta-1/beta-1b expressed in HEK293 cells in presence of -100 mV holding potential by whole-cell patch clamp method
Inhibition of L type calcium channel alpha-1c/alpha-2-delta-1/beta-1b expressed in HEK293 cells in presence of -100 mV holding potential by whole-cell patch clamp method
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[PMID: 20117000] |
NP118809 is a potent N-type calcium channel blocker, with an IC50 of 0.11 μM; also inhibits L-type calcium channel with an IC50 of 12.2 μM. NP118809 inhibits the hERG potassium channel in HEK cells, with an IC50 of 7.4 μM[1].
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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No. CAS 41332-24-5
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Appearance Solid
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Peso molecular 460.61
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Fòrmula C32H32N2O
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Color Light yellow to yellow
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SMILES
O=C(CC(C1=CC=CC=C1)C2=CC=CC=C2)N3CCN(C(C4=CC=CC=C4)C5=CC=CC=C5)CC3
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Synonyms
39-1B4
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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 (108.55 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 (5.43 mM); Suspended solution; Need ultrasonic and warming
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 (274 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]. Zamponi GW, et al. Scaffold-based design and synthesis of potent N-type calcium channel blockers. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6467-72. [Content Brief]
[2]. Pajouhesh H, et al. Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors. Bioorg Med Chem Lett. 2010 Feb 15;20(4):1378-83. [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 | 2.1710 mL | 10.8552 mL | 21.7103 mL | 54.2759 mL |
| 5 mM | 0.4342 mL | 2.1710 mL | 4.3421 mL | 10.8552 mL | |
| 10 mM | 0.2171 mL | 1.0855 mL | 2.1710 mL | 5.4276 mL | |
| 15 mM | 0.1447 mL | 0.7237 mL | 1.4474 mL | 3.6184 mL | |
| 20 mM | 0.1086 mL | 0.5428 mL | 1.0855 mL | 2.7138 mL | |
| 25 mM | 0.0868 mL | 0.4342 mL | 0.8684 mL | 2.1710 mL | |
| 30 mM | 0.0724 mL | 0.3618 mL | 0.7237 mL | 1.8092 mL | |
| 40 mM | 0.0543 mL | 0.2714 mL | 0.5428 mL | 1.3569 mL | |
| 50 mM | 0.0434 mL | 0.2171 mL | 0.4342 mL | 1.0855 mL | |
| 60 mM | 0.0362 mL | 0.1809 mL | 0.3618 mL | 0.9046 mL | |
| 80 mM | 0.0271 mL | 0.1357 mL | 0.2714 mL | 0.6784 mL | |
| 100 mM | 0.0217 mL | 0.1086 mL | 0.2171 mL | 0.5428 mL |
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