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製品番号: 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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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CAS 番号: 171722-81-9
分子式: C₂₀H₂₃ClN₂O₂
分子量:358.86

保管条件:

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

Data Sheet (270 KB)

YM-46303 構造式

CAS 番号: 171722-81-9

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Use of MCE Products

Fluorescent Dye

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

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]

mAChR アイソフォーム固有の製品をすべて表示 :

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]

体内実験

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.

化学情報

CAS 番号 171722-81-9
分子量 358.86
分子式 C₂₀H₂₃ClN₂O₂
SMILES

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

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (270 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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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MOQ

Minimum order quantity

100 mg

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生物活性
- 製品説明
- IC₅₀ & Target
- 体内実験
化学情報
純度とドキュメンテーション
参考文献

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YM-46303

mAChR アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

YM-46303 関連分類

HY-U00104 関連分類