1. GPCR/G Protein
    Neuronal Signaling
  2. mAChR
  3. Revefenacin

Revefenacin (Synonyms: TD-4208; GSK1160724)

製品番号: HY-15851 純度: 99.78%
取扱説明書

Revefenacin (TD-4208; GSK1160724) is a potent mAChR antagonist; has a high affinity on M3 receptor with a Ki of 0.18 nM.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用としては使用しないように、十分ご注意ください。

Revefenacin 構造式

Revefenacin 構造式

CAS 番号 : 864750-70-9

容量 価格(税別) 在庫状況 数量
10 mM * 1  mL in DMSO USD 252 在庫あり
Estimated Time of Arrival: December 31
2 mg USD 120 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 192 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 312 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 1020 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 1920 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • 生物活性

  • プロトコル

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

Revefenacin (TD-4208; GSK1160724) is a potent mAChR antagonist; has a high affinity on M3 receptor with a Ki of 0.18 nM.

IC50 & Target

Ki: 0.42 nM (M1), 0.32 nM (M2), 0.18 nM (M3), 0.56 nM (M4), 6.7 nM (M5)[1]

体外実験

The Kis of revefenacin are 0.42, 0.32, 0.18, 0.56, and 6.7 nM at human M1, M2, M3, M4 and M5 receptors, respectively. In a functional assay, revefenacin is shown to be a functional antagonist with inhibition constants similar to binding Ki's. Revefenacin also inhibits agonist-induced contraction of guinea pig isolated tracheal ring preparation with an affinity of 0.1 nM, similar to the measured M3 biding Ki[1].

体内実験

In anesthetized dogs, revefenacin, along with tiotropium and glycopyrronium, produce sustained inhibition of acetylcholine-induced bronchoconstriction for up to 24 hours. In anesthetized rats, inhaled revefenacin exhibits dose-dependent 24-hour bronchoprotection against methacholine-induced bronchoconstriction. The estimated 24-hour potency is 45.0 µg/mL and the bronchoprotective potencies are maintained after 7 days of once-daily dosing[2].

臨床実験
分子量

597.75

分子式

C₃₅H₄₃N₅O₄

CAS 番号

864750-70-9

SMILES

O=C(OC1CCN(CCN(C(C2=CC=C(CN3CCC(C(N)=O)CC3)C=C2)=O)C)CC1)NC4=CC=CC=C4C5=CC=CC=C5

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : ≥ 125 mg/mL (209.12 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6729 mL 8.3647 mL 16.7294 mL
5 mM 0.3346 mL 1.6729 mL 3.3459 mL
10 mM 0.1673 mL 0.8365 mL 1.6729 mL
*Please refer to the solubility information to select the appropriate solvent.
参考文献
動物実験
[2]

Rats: To determine the bronchoprotective and antisialagogue potency after a single dose, rats are exposed by inhalation to a nebulized solution of revefenacin (3–3000 µg/mL), tiotropium (0.3–300 µg/mL), glycopyrronium (1–1000 µg/mL), or vehicle (sterile water). Bronchoprotective activity is assessed 24 hours postdose. For the antisialagogue effect, inhibition of Pilo is assessed 1, 6, or 12 hours after inhalation of an efficacious dose of test compound to determine the time point at which peak effect occurred. All subsequent doses are measured at this time point[2].

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • モル濃度カルキュレーター

  • 希釈カルキュレーター

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

RevefenacinTD-4208GSK1160724TD4208TD 4208GSK 1160724GSK-1160724mAChRMuscarinic acetylcholine receptorInhibitorinhibitorinhibit

最近チェックした製品:

オンラインお問い合わせ

Your information is safe with us. * Required Fields.

製品名

 

タイトル

お名前 *

 

PC 用メールアドレス *

電話番号 *

 

勤務先/学校名 *

Department *

 

カスタマ需要量 *

国会或いは地域 *

     

必ず会社名を記載ください。個人への返信は行いません。

メッセージ

バルクお問い合わせ

Inquiry Information

製品名:
Revefenacin
製品番号:
HY-15851
数量:
MCE 日本正規代理店: