YM-58790
Based on 1 Customer Validation
YM-58790 is a potent antagonist of mAChR. YM-58790 binds M1, M2, M3 with Ki values of 28 nM, 260 nM, and 15 nM. YM-58790 exhibits potent inhibitory activity on bladder pressuer in reflexly-evoked rhythmic contraction in rats.
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- Pureté: 98.21%
- CAS No.: 214558-72-2
- Formule: C27H32ClN3O2
- Masse moléculaire:466.01
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Stockage:
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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mAChR3 15 nM (Ki) |
mAChR1 28 nM (Ki) |
mAChR2 260 nM (Ki) |
YM-58790 (compound 18b) (0-1 μM) shows potent inhibitory effect on urinary bladder contraction, but has little effect on bradycardia. YM-58790 exhibits selective antagonism between urinary bladder contraction and salivary secretion in vitro[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
YM-58790 (6.0 mg/kg; i.v.) shows poor M1 and M2 antagonism effect in vivo on McN-A343-induced pressor in pithed rats, but displays potent efficacy on M3 antagonism with an ED30 value of 0.36 mg/kg (i.v.) and an ID50 value of 2.4 mg/kg (i.v.)[1].
YM-58790 exhibits potent inhibitory activity on bladder pressuer in reflexly-evoked rhythmic contraction, similar to Oxybutynin (HY-B0267), and has about ten times less inhibitory effect on oxotremorine-induced salivary secretion than oxybutynin in rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 214558-72-2
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Appearance Solid
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Masse moléculaire 466.01
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Formule C27H32ClN3O2
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Color Light yellow to yellow
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SMILES
O=C(OC1CCN(CC2=CC=C(NC)C=C2)CC1)NC(C3=CC=CC=C3)C4=CC=CC=C4.[H]Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
DMSO : 100 mg/mL (214.59 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (271 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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Instruction de manipulation (2659 KB)
Références
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 | 2.1459 mL | 10.7294 mL | 21.4588 mL | 53.6469 mL |
| 5 mM | 0.4292 mL | 2.1459 mL | 4.2918 mL | 10.7294 mL | |
| 10 mM | 0.2146 mL | 1.0729 mL | 2.1459 mL | 5.3647 mL | |
| 15 mM | 0.1431 mL | 0.7153 mL | 1.4306 mL | 3.5765 mL | |
| 20 mM | 0.1073 mL | 0.5365 mL | 1.0729 mL | 2.6823 mL | |
| 25 mM | 0.0858 mL | 0.4292 mL | 0.8584 mL | 2.1459 mL | |
| 30 mM | 0.0715 mL | 0.3576 mL | 0.7153 mL | 1.7882 mL | |
| 40 mM | 0.0536 mL | 0.2682 mL | 0.5365 mL | 1.3412 mL | |
| 50 mM | 0.0429 mL | 0.2146 mL | 0.4292 mL | 1.0729 mL | |
| 60 mM | 0.0358 mL | 0.1788 mL | 0.3576 mL | 0.8941 mL | |
| 80 mM | 0.0268 mL | 0.1341 mL | 0.2682 mL | 0.6706 mL | |
| 100 mM | 0.0215 mL | 0.1073 mL | 0.2146 mL | 0.5365 mL |
YM-58790 Related Classifications
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