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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 | Availability | Quantity |
---|---|---|---|
1 mg | $147 | In Stock | |
5 mg | $323 | In Stock | |
10 mg | $516 | In Stock | |
25 mg | $990 | In Stock | |
50 mg | $1,680 | In Stock | |
100 mg | $2,698 | In Stock | |
500 mg | $3,780 | 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 | M1 mAChR:28 nM (Ki), M2 mAChR:260 nM (Ki), M3 mAChR:15 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] |
Alias | YM-58790 free base |
Molecular Weight | 429.55 |
Formula | C27H31N3O2 |
Cas No. | 168830-70-4 |
Storage | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 60 mg/mL (139.68 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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