PF-06456384 trihydrochloride
Based on 1 Customer Validation
PF-06456384 trihydrochloride is an extremely potent and selective Nav1.7 sodium channel blocker (IC50: 0.01 nM for hNaV1.7; 75 nM for rNaV1.7; <0.1 nM for mNaV1.7). PF-06456384 trihydrochloride shows no significant analgesic efficacy in the mouse Formalin pain model.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.41%
- CAS. Nr.: 1834610-75-1
- Formel: C35H35Cl3F3N7O3S2
- Molecular Weight:829.18
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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DSP-2230Nav1.7/Nav1.8 Channel Blocker
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
h Nav1.7 0.01 nM (IC50) |
rNaV1.7 75 nM (IC50) |
hNav1.1 314 nM (IC50) |
hNav1.2 3 nM (IC50) |
hNav1.3 6438 nM (IC50) |
hNav1.4 1451 nM (IC50) |
hNav1.5 2592 nM (IC50) |
hNav1.6 5.8 nM (IC50) |
hNav1.8 26000 nM (IC50) |
mNaV1.7 <0.1 nM (IC50) |
In Vitro
PF-06456384 trihydrochloride potently inhibits NaV1.7 channels in the PatchXpress automated electrophysiology assay with an IC50 of 0.58 nM[1].
PF-06456384 trihydrochloride potently inhibits human NaV1.7 channels in the conventional patch clamp electrophysiology assay with an IC50 of 0.01 nM[1].
PF-06456384 (trihydrochloride) inhibits rat NaV1.7 channels in the conventional patch clamp electrophysiology assay with an IC50 of 75 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
In Vivo
PF-06456384 (20 or 40 mg/kg; i.v.) trihydrochloride produces a plasma concentration 40-fold higher than the predicted value in male Wistar-Han rats, and does not reach steady state at the 2-hour time point[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wild-type mice[1]
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Dosage:0.28 mg/kg; 5.4 mg/kg
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Administration:i.v.; continuous infusion
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Result:Achieved an unbound plasma concentration ≥60× the mouse NaV1.7 IC50.
Produced no significant reduction in motion counts (pain-related behavior) relative to vehicle control at either dose.
Chemical Information
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CAS. Nr. 1834610-75-1
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Appearance Solid
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Molecular Weight 829.18
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Formel C35H35Cl3F3N7O3S2
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Color White to off-white
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SMILES
N#CC1=CC(S(=O)(NC2=NC=NS2)=O)=CC=C1OC3=CC=C(C4=CC(C(F)(F)F)=CC=C4)C=C3C5=CC(CNCCC6CCNCC6)=NC=C5.[H]Cl.[H]Cl.[H]Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 125 mg/mL (150.75 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Reinheit & Dokumentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Storer RI, et al. Highly potent and selective NaV1.7 inhibitors for use as intravenous agents and chemical probes. Bioorg Med Chem Lett. 2017;27(21):4805-4811. [Content Brief]
[2]. Pike A, et al. The role of organic anion-transporting polypeptides and formulation in the clearance and distribution of a novel Nav 1.7 channel blocker. Biopharm Drug Dispos. 2018;39(8):388-393. [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 (sealed storage, away from moisture). 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 | 1.2060 mL | 6.0301 mL | 12.0601 mL | 30.1503 mL |
| 5 mM | 0.2412 mL | 1.2060 mL | 2.4120 mL | 6.0301 mL | |
| 10 mM | 0.1206 mL | 0.6030 mL | 1.2060 mL | 3.0150 mL | |
| 15 mM | 0.0804 mL | 0.4020 mL | 0.8040 mL | 2.0100 mL | |
| 20 mM | 0.0603 mL | 0.3015 mL | 0.6030 mL | 1.5075 mL | |
| 25 mM | 0.0482 mL | 0.2412 mL | 0.4824 mL | 1.2060 mL | |
| 30 mM | 0.0402 mL | 0.2010 mL | 0.4020 mL | 1.0050 mL | |
| 40 mM | 0.0302 mL | 0.1508 mL | 0.3015 mL | 0.7538 mL | |
| 50 mM | 0.0241 mL | 0.1206 mL | 0.2412 mL | 0.6030 mL | |
| 60 mM | 0.0201 mL | 0.1005 mL | 0.2010 mL | 0.5025 mL | |
| 80 mM | 0.0151 mL | 0.0754 mL | 0.1508 mL | 0.3769 mL | |
| 100 mM | 0.0121 mL | 0.0603 mL | 0.1206 mL | 0.3015 mL |
PF-06456384 trihydrochloride Related Classifications
HY-118952A Related Classifications
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