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標簽:PF-03716556
聯系人:高小姐
電話:021-59541103 021-60443211
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詳細地址:上海嘉定區嘉羅公路1661
化學性質:
規格 | 5mg 25mg |
CAS | 928774-43-0 |
別名 | PF-03716556; PF03716556 |
化學名 | N-(2-hydroxyethyl)-N,2-dimethyl-8-[[(4R)-5-methyl-3,4-dihydro-2H-chromen-4-yl]amino]imidazo[1,2-a]pyridine-6-carboxamide |
分子式 | C22H26N4O3 |
分子量 | 394.48 |
溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:20): 0.04 mg/ml,Ethanol: 10 mg/ml |
儲存條件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述:
IC50: In porcine ion-tight membrane vesicles, PF-03716556 inhibited H+,K+-ATPase activity in a concentration-dependent manner, with a pIC50 value of 7.095 ± 0.077 at pH 7.4.
The gastric H+,K+-ATPase, which is responsible for gastric acid secretion, is a P2-type ATPase located in the apical membrane of parietal cells. Inhibition of the H+,K+-ATPase is currently the most effective way to control gastric acid secretion and remains an attractive target for the medical treatment of acidrelated diseases. PF-03716556 is a novel, potent, and selective acid pump antagonist for the treatment of gastroesophageal reflux disease.
In vitro: PF-03716556 demonstrated 3-fold greater inhibitory activity than revaprazan, the only acid pump antagonist that has been available on the market, in ion-tight assay. Kinetics experiments revealed that PF-03716556 has a competitive and reversible mode of action [1].
In vivo: PF-03716556 did not display any species differences, exhibiting highly selective profile including the canine kidney H+,K+-ATPase. In addition, more rapid onset of action than omeprazole and 3-fold greater potency than revaprazan were observed in Ghosh-Schild rats and Heidenhain pouch dogs [2].
特別提醒:
1. 本產品僅供科研使用。請勿用于醫藥、臨床診斷或治療,食品及化妝品等用途。請勿存放于普通住宅區。
2. 為了您的安全和健康,請穿好實驗服并佩戴一次性手套和口罩操作。
原創作者:上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名:上海生物
開 戶 行:中國銀行山東省分行營業部
賬 號:2169 2341 6278