2. GPCR/G Protein Neuronal Signaling
  3. mAChR
  4. YM-58790

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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YM-58790 Chemical Structure

YM-58790 Chemical Structure

CAS No. : 214558-72-2

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Other Forms of YM-58790:

YM-58790 Related Antibodies

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mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

  • Biological Activity

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Description

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[1].

IC50 & Target

mAChR3

15 nM (Ki)

mAChR1

28 nM (Ki)

mAChR2

260 nM (Ki)

In Vitro

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 Related Antibodies
In Vivo

YM-58790 (3 mg/kg, i.v.) has no effect on oxotremorine-induced tremor in mice[1].
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.
Molecular Weight

466.01

Formula

C27H32ClN3O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(OC1CCN(CC2=CC=C(NC)C=C2)CC1)NC(C3=CC=CC=C3)C4=CC=CC=C4.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1459 mL 10.7294 mL 21.4588 mL
5 mM 0.4292 mL 2.1459 mL 4.2918 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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
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YM-58790 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

YM-58790214558-72-2YM58790YM 58790mAChRMuscarinic acetylcholine receptorbladder pressuerrhythmic contractionreflexly-evoked rhythmic contractionInhibitorinhibitorinhibit

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