化學名 | 1-(6-bromo-2-methoxyquinolin-3-yl)-4-(dimethylamino)-2-naphthalen-1-yl-1-phenylbutan-2-ol | |
簡稱 | Bedaquiline | |
別名 | Sirturo, TMC207, R207910, TMC 207, R 207910, TMC-207, R-207910 | |
中文名 | 貝達喹啉 | |
化學式 | C32H31BrN2O2 | |
分子量 | 555.5 | |
CAS號 | 843663-66-1 | |
純度 | 98% | |
溶劑/溶解度 | Water<1mg/ml; DMSO6mg/ml; Ethanol<1mg/ml | |
溶液配制 | 5mg加入0.9ml DMSO,或者每5.56mg加入1ml DMSO,配制成10mM溶液。SC3251-10mM用DMSO配制。 |
生物信息:
產品描述 | Bedaquiline(TMC207; R207910) is an anti-tuberculosis drug which selectively inhibit the mycobacterial energy metabolism i.e. ATP synthesis and found to be effective against all states of Mycobacterium tuberculosis. | ||||
信號通路 | Anti-infection | ||||
靶點 | anti-TB | - | - | - | - |
IC50 | - | - | - | - | - |
體外研究 | Preclinical studies have shown the efficacy of bedaquiline in terms of reduction in bacterial load and treatment duration. Phase II clinical studies have established the safety, tolerability and earlier sputum conversion time in patients with MDR-TB. In 2012 FDA approved bedaquiline for treatment of MDR-TB and XDR-TB. Bedaquiline possesses a unique mechanism of action that disrupts the activity of the mycobacterial adenosine triphosphate synthase. Clinical trials have been conducted evaluating the use of bedaquiline in combination with a background regimen for the treatment of adults with pulmonary MDR-TB. Bedaquiline has an excellent in vitro activity against Mycobacterium tuberculosis, including multidrug resistant M tuberculosis; however, its side effect profile limits its use against MDR-TB when no other effective regimen can be provided. | ||||
體內研究 | N/A | ||||
臨床實驗 | N/A | ||||
特征 | N/A |
相關實驗數據(此數據來自于公開文獻,并不保證其有效性):
酶活性檢測實驗 | |
方法 | N/A |
細胞實驗 | |
細胞系 | N/A |
濃度 | N/A |
處理時間 | N/A |
方法 | N/A |
動物實驗 | |
動物模型 | N/A |
配制 | N/A |
劑量 | N/A |
給藥方式 | N/A |
參考文獻:
1. Lakshmanan M, et al. J Young Pharm. 2013 Dec, 5(4), 112-115.2. Chahine EB, et al. Ann Pharmacother. 2014 Jan, 48(1), 107-15.包裝清單:
產品編號 | 產品名稱 | 包裝 |
SC3251-10mM | Bedaquiline (抗結核分枝桿菌) | 10mM×0.2ml |
SC3251-5mg | Bedaquiline (抗結核分枝桿菌) | 5mg |
SC3251-25mg | Bedaquiline (抗結核分枝桿菌) | 25mg |
— | 說明書 | 1份 |
保存條件:
-20℃保存,至少一年有效。5mg和25mg包裝也可室溫保存,至少6個月有效。如果溶于非DMSO溶劑,建議分裝后-80℃保存,預計6個月內有效。
注意事項:
本產品僅限于專業人員的科學研究用,不得用于臨床診斷或治療,不得用于食品或藥品,不得存放于普通住宅內。為了您的安全和健康,請穿實驗服并戴一次性手套操作。
使用說明:
1.收到產品后請立即按照說明書推薦的條件保存。使用前可以在2,000-10,000g離心數秒,以使液體或粉末充分沉降至管底后再開蓋使用。
2.對于10mM溶液,可直接稀釋使用。對于固體,請根據本產品的溶解性及實驗目的選擇相應溶劑配制成高濃度的儲備液(母液)后使用。
3.具體的最佳工作濃度請參考本說明書中的體外、體內研究結果或其它相關文獻,或者根據實驗目的,以及所培養的特定細胞和組織,通過實驗進行摸索和優化。