PCS1055
Based on 2 publication(s) in Google Scholar
PCS1055 is a selective and competitive antagonist for muscarinic M4 receptor with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 inhibits radioligand [3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 is also an inhibitor for AChE with IC50 of 22 nM and 120 nM for electric eel and human AChE, respectively.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.02%
- CAS. Nr.: 357173-55-8
- Formel: C27H32N4
- Molecular Weight:412.57
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
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Publications Citing Use of MedChemExpress (MCE) PCS1055
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Biologische Aktivität
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mAChR4 18.1 nM (IC50) |
mAChR4 5.72 nM (Kd) |
electric eel AChE 22 nM (IC50) |
hAChE 120 nM (IC50) |
Chemical Information
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CAS. Nr. 357173-55-8
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Appearance Solid
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Molecular Weight 412.57
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Formel C27H32N4
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Color White to off-white
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SMILES
C12=NN=C(NCCC3CCN(CC4=CC=CC=C4)CC3)C=C1CCCC5=CC=CC=C52
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Neuron
2025 Mar 5;113(5):670-683.e7. PMID: 39837323 -
Mol Cell Endocrinol
Vagotomy suppresses food intake by increasing GLP-1 secretion via the M3 AChR-AMPKα pathway in mice. [Abstract]2025 Apr 1:599:112464. PMID: 39848433
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (242.38 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Croy CH, et al. Characterization of PCS1055, a novel muscarinic M4 receptor antagonist. Eur J Pharmacol. 2016 Jul 5;782:70-6. [Content Brief]
[2]. Contreras JM, et al. Design, synthesis, and structure-activity relationships of a series of 3-[2-(1-benzylpiperidin-4-yl)ethylamino]pyridazine derivatives as acetylcholinesterase inhibitors. J Med Chem. 2001 Aug 16;44(17):2707-18. [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 | 2.4238 mL | 12.1192 mL | 24.2383 mL | 60.5958 mL |
| 5 mM | 0.4848 mL | 2.4238 mL | 4.8477 mL | 12.1192 mL | |
| 10 mM | 0.2424 mL | 1.2119 mL | 2.4238 mL | 6.0596 mL | |
| 15 mM | 0.1616 mL | 0.8079 mL | 1.6159 mL | 4.0397 mL | |
| 20 mM | 0.1212 mL | 0.6060 mL | 1.2119 mL | 3.0298 mL | |
| 25 mM | 0.0970 mL | 0.4848 mL | 0.9695 mL | 2.4238 mL | |
| 30 mM | 0.0808 mL | 0.4040 mL | 0.8079 mL | 2.0199 mL | |
| 40 mM | 0.0606 mL | 0.3030 mL | 0.6060 mL | 1.5149 mL | |
| 50 mM | 0.0485 mL | 0.2424 mL | 0.4848 mL | 1.2119 mL | |
| 60 mM | 0.0404 mL | 0.2020 mL | 0.4040 mL | 1.0099 mL | |
| 80 mM | 0.0303 mL | 0.1515 mL | 0.3030 mL | 0.7574 mL | |
| 100 mM | 0.0242 mL | 0.1212 mL | 0.2424 mL | 0.6060 mL |
PCS1055 Related Classifications
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