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Cat. No.: HY-U00104

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YM-46303

YM-46303 is an mAChR antagonist which exhibits the highest affinities for M1 and M3 receptors, and selectivity for M3 over M2 receptor.

For research use only. We do not sell to patients.

CAS No.: 171722-81-9
Formula: C₂₀H₂₃ClN₂O₂
Molecular Weight:358.86

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (270 KB)

YM-46303 Chemical Structure

CAS No.: 171722-81-9

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

YM-46303 is an mAChR antagonist which exhibits the highest affinities for M1 and M3 receptors, and selectivity for M3 over M2 receptor.

IC₅₀ & Target

mAChR^[1]

All mAChR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	IC₅₀	14.5 nM Compound: YM-46303	Displacement of [3H]NMS from human muscarinic M2 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting Displacement of [3H]NMS from human muscarinic M2 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting	[PMID: 21524581]
CHO-K1	IC₅₀	3 nM Compound: YM-46303	Displacement of [3H]NMS from human muscarinic M1 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting Displacement of [3H]NMS from human muscarinic M1 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting	[PMID: 21524581]
CHO-K1	IC₅₀	6 nM Compound: YM-46303	Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting Displacement of [3H]NMS from human muscarinic M3 receptor expressed in CHO-K1 cells after 1 hr by scintillation counting	[PMID: 21524581]

In Vivo

YM-46303 shows approximately ten times higher inhibitory activity on bladder pressure in reflexly-evoked rhythmic contraction, and about 5-fold greater selectivity for urinary bladder contraction against salivary secretion in rats compared to oxybutynin. Further evaluation of antimuscarinic effects on bradycardia and pressor in pithed rats, and on tremor in mice, show that YM-46303 can be useful for the treatment of urinary urge incontinence as a bladder-selective M3 antagonist with potent activities and fewer side effects^[1]. YM-46303 shows in vivo selective inhibitory activities on bladder pressure in reflexly-evoked rhythmic contraction against oxotremorine-induced salivary secretion. In addition, YM-46303 has potent activity in a guinea pig model of methacholine-induced bronchospasm on intravenous administration^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 171722-81-9
Molecular Weight 358.86
Formula C₂₀H₂₃ClN₂O₂
SMILES

O=C(OC12CCN(CC2)CC1)NC3=CC=CC=C3C4=CC=CC=C4.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Naito R, et al. Selective muscarinic antagonists. II. Synthesis and antimuscarinic properties of biphenylylcarbamate derivatives. Chem Pharm Bull (Tokyo). 1998 Aug;46(8):1286-94. [Content Brief]

[2]. Nagashima S, et al. Novel quinuclidinyl heteroarylcarbamate derivatives as muscarinic receptor antagonists. Bioorg Med Chem. 2014 Jul 1;22(13):3478-87. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vivo
Chemical Information
Purity & Documentation
References

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YM-46303

All mAChR Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

YM-46303 Related Classifications

HY-U00104 Related Classifications