VU0238441
Based on 1 Customer Validation
VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC50s of 3.2 μM, 2.8 μM, 2.2 μM, 2.1 μM, >10 μM for M1, M2, M3, M5 and M4, respectively.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.87%
- CAS. Nr.: 85511-68-8
- Formel: C16H9ClF3NO2
- Molecular Weight:339.70
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Speicherung:Powder -20°C, 3 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
- Verweise
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Biologische Aktivität
EC50: 3.2 μM (M1), 2.8 μM (M2), 2.2 μM (M3), 2.1 μM (M5) and >10 μM (M4)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
>10 μM
Compound: 2
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Agonist activity at rat muscarinic M4 expressed in CHO cells assessed as stimulation of calcium mobilization
Agonist activity at rat muscarinic M4 expressed in CHO cells assessed as stimulation of calcium mobilization
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[PMID: 20004578] |
| CHO | EC50 |
>10 μM
Compound: 56
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Activation of rat muscarinic M4 receptor expressed in CHO cells coexpressing chimeric Gqi5 protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
Activation of rat muscarinic M4 receptor expressed in CHO cells coexpressing chimeric Gqi5 protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
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[PMID: 19438238] |
| CHO | EC50 |
2.1 μM
Compound: 2
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Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization
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[PMID: 20004578] |
| CHO | EC50 |
2.11 μM
Compound: 56
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Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
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[PMID: 19438238] |
| CHO | EC50 |
2.2 μM
Compound: 2
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Agonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilization
Agonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilization
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[PMID: 20004578] |
| CHO | EC50 |
2.22 μM
Compound: 56
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Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
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[PMID: 19438238] |
| CHO | EC50 |
2.8 μM
Compound: 2
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Agonist activity at rat muscarinic M2 expressed in CHO cells assessed as stimulation of calcium mobilization
Agonist activity at rat muscarinic M2 expressed in CHO cells assessed as stimulation of calcium mobilization
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[PMID: 20004578] |
| CHO | EC50 |
2.84 μM
Compound: 56
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Activation of rat muscarinic M2 receptor expressed in CHO cells co-expressing chimeric Gqi5 protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
Activation of rat muscarinic M2 receptor expressed in CHO cells co-expressing chimeric Gqi5 protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
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[PMID: 19438238] |
| CHO | EC50 |
3.2 μM
Compound: 2
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Agonist activity at rat muscarinic M1 expressed in CHO cells assessed as stimulation of calcium mobilization
Agonist activity at rat muscarinic M1 expressed in CHO cells assessed as stimulation of calcium mobilization
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[PMID: 20004578] |
| CHO | EC50 |
3.2 μM
Compound: 56
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Activation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
Activation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization
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[PMID: 19438238] |
VU0238441 is an analogue of VU0119498[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 85511-68-8
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Appearance Solid
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Molecular Weight 339.70
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Formel C16H9ClF3NO2
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Color Brown to red
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SMILES
O=C1N(CC2=CC=C(C(F)(F)F)C=C2)C3=C(C=CC=C3Cl)C1=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 125 mg/mL (367.97 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 (275 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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Handling Instructions (2659 KB)
Verweise
[1]. Thomas M Bridges, et al. Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM. Bioorg Med Chem Lett. 2010 Jan 15;20(2):558-62. [Content Brief]
[2]. Thomas M Bridges, et al. Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. J Med Chem. 2009 Jun 11;52(11):3445-8. [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 | 2.9438 mL | 14.7189 mL | 29.4377 mL | 73.5943 mL |
| 5 mM | 0.5888 mL | 2.9438 mL | 5.8875 mL | 14.7189 mL | |
| 10 mM | 0.2944 mL | 1.4719 mL | 2.9438 mL | 7.3594 mL | |
| 15 mM | 0.1963 mL | 0.9813 mL | 1.9625 mL | 4.9063 mL | |
| 20 mM | 0.1472 mL | 0.7359 mL | 1.4719 mL | 3.6797 mL | |
| 25 mM | 0.1178 mL | 0.5888 mL | 1.1775 mL | 2.9438 mL | |
| 30 mM | 0.0981 mL | 0.4906 mL | 0.9813 mL | 2.4531 mL | |
| 40 mM | 0.0736 mL | 0.3680 mL | 0.7359 mL | 1.8399 mL | |
| 50 mM | 0.0589 mL | 0.2944 mL | 0.5888 mL | 1.4719 mL | |
| 60 mM | 0.0491 mL | 0.2453 mL | 0.4906 mL | 1.2266 mL | |
| 80 mM | 0.0368 mL | 0.1840 mL | 0.3680 mL | 0.9199 mL | |
| 100 mM | 0.0294 mL | 0.1472 mL | 0.2944 mL | 0.7359 mL |
VU0238441 Related Classifications
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