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製品番号: HY-14825

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Tarafenacin

(別名: SVT-40776)

Tarafenacin (SVT-40776) is an orally active, selective M3 muscarinic receptor (M3 muscarinic receptor) antagonist with 203-fold selectivity over the M2 muscarinic receptor. Tarafenacin does not affect atrial contraction, arterial blood pressure or arterial pressure at high doses. Tarafenacin can be used in the research of overactive bladder.

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。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 385367-47-5
分子式: C₂₁H₂₀F₄N₂O₂
分子量:408.39

保管条件:

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

Data Sheet (273 KB)

Tarafenacin 構造式

CAS 番号: 385367-47-5

容量

価格（税別）

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数量

Amount: USD 0.00

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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
- 体外実験
- 体内実験
- 臨床実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
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関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

mAChR3

0.19 nM (Ki)

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	0.9 nM Compound: 4q	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	1.5 nM Compound: 4q	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]
CHO-K1	IC₅₀	97.3 nM Compound: 4q	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]

体外実験

Tarafenacin (3-1000 nmol/L; 60 min) potently inhibits carbachol-induced contractions in mouse isolated urinary bladder detrusor smooth muscle^[1].
Tarafenacin (0.1-10 μmol/L; 60 min) inhibits Carbachol (HY-B1208)-induced negative chronotropism in mouse isolated atrial tissue, exhibiting a 199-fold functional selectivity for mouse urinary bladder over atrial tissue^[1].
Tarafenacin (20 min) potently inhibits Carbachol-induced inositol phosphate accumulation in mouse bladder smooth muscle with a K_i of 0.19 nM, and shows 23-fold greater selectivity over mouse salivary glands^[2].

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

体内実験

Tarafenacin (1-3000 nmol/kg (log dose); i.v.; cumulative bolus; 15 min between doses) potently inhibits spontaneous guinea pig bladder contractions with an ED₂₅ of 6.97 mg/kg, and exhibits greater than 175-fold bladder versus vascular selectivity, with no observed effects on arterial blood pressure^[1].

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

Animal Model:

DH female guinea pigs (250-300 g)^[1]
Dosage:

1-3000 nmol/kg (Log dose)
Administration:

i.v.; cumulative bolus; 15 min between doses
Result:

Inhibited spontaneous bladder contractions in a dose-dependent manner, with an ED₂₅ of 17.1 nmol/kg.
Did not affect arterial blood pressure at tested doses, resulting in a bladder versus vascular selectivity of more than 175-fold.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 385367-47-5
分子量 408.39
分子式 C₂₁H₂₀F₄N₂O₂
SMILES

O=C(O[C@H]1CN2CCC1CC2)N(C3=CC=CC(F)=C3)CC4=CC(F)=C(F)C(F)=C4
別名

SVT-40776
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 (273 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]. Salcedo C, et al. In vivo and in vitro pharmacological characterization of SVT-40776, a novel M3 muscarinic receptor antagonist, for the treatment of overactive bladder. Br J Pharmacol. 2009 Mar;156(5):807-17. [Content Brief]

[2]. Balsa D, et al. FUNCTIONAL BLADDER SELECTIVITY OF SVT-40776: A COMPARATIVE

[3]. Huang X, et al. Microscopic binding of M5 muscarinic acetylcholine receptor with antagonists by homology modeling, molecular docking, and molecular dynamics simulation. J Phys Chem B. 2012 Jan 12;116(1):532-41. [Content Brief]

Calculators

モル濃度計算機

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

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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)

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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.

Keywords

MOQ

Minimum order quantity

100 mg

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生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
- 臨床実験
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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Tarafenacin

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

Tarafenacin 関連分類

HY-14825 関連分類