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YM-58790 free base is a potent mAChR antagonist that inhibits M1 mAChR, M2 mAChR, and M3 mAChR with Ki values of 28 nM, 260 nM, and 15 nM, respectively. It inhibits reflex rhythmic bladder contractions in rats by inhibiting bladder pressurization.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $62 | In Stock | In Stock | |
| 5 mg | $135 | In Stock | In Stock | |
| 10 mg | $217 | In Stock | In Stock | |
| 25 mg | $415 | In Stock | In Stock | |
| 50 mg | $593 | In Stock | In Stock |
| Description | YM-58790 free base is a potent mAChR antagonist that inhibits M1 mAChR, M2 mAChR, and M3 mAChR with Ki values of 28 nM, 260 nM, and 15 nM, respectively. It inhibits reflex rhythmic bladder contractions in rats by inhibiting bladder pressurization. |
| Targets&IC50 | M3 mAChR:15 nM (Ki), M1 mAChR:28 nM (Ki), M2 mAChR:260 nM (Ki) |
| In vitro | YM-58790 free base (compound 18b) (0-1 μM) potently inhibits urinary bladder contraction with minimal impact on bradycardia. In vitro, YM-58790 selectively antagonizes urinary bladder contraction without significantly affecting salivary secretion. [1] |
| In vivo | YM-58790 free base (3 mg/kg, i.v.) exhibits no impact on oxotremorine-induced tremor in mice.[1] At 6.0 mg/kg, i.v., YM-58790 free base shows limited M1 and M2 antagonistic effects on McN-A343-induced pressor response in pithed rats but demonstrates robust M3 antagonism, with an ED30 value of 0.36 mg/kg and an ID50 value of 2.4 mg/kg.[1] Additionally, YM-58790 free base exhibits strong inhibitory activity on bladder pressure during reflexly-evoked rhythmic contractions in rats.[1] |
| Synonyms | YM-58790 free base |
| Molecular Weight | 429.55 |
| Formula | C27H31N3O2 |
| Cas No. | 168830-70-4 |
| Smiles | C(NC(OC1CCN(CC2=CC=C(NC)C=C2)CC1)=O)(C3=CC=CC=C3)C4=CC=CC=C4 |
| Relative Density. | 1.18 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 60 mg/mL (139.68 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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