CS-526

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CS-526 (AKU 517;R 105266) 是一种有效的、竞争性的、可逆的酸泵拮抗剂（钾竞争性酸阻滞剂），可抑制 H+,K+-ATPase 活性，IC50 为 61 nM。

CS-526 (AKU 517;R 105266) is a potent, competitive, and reversible acid pump antagonist (potassium-competitive acid blocker) that inhibits H+,K+-ATPase activity with IC50 of 61 nM; inhibits gastric acid secretion in pylorus-ligated rats with ID50 of 0.7 mg/kg (p.o.); inhibits histamine-stimulated gastric acid secretion in Heidenhain pouch dogs, inhibits acute gastric mucosal lesions and has potent antisecretory and antiulcer effects.Ulcer Phase 1 Discontinued.

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Animal Model:Pylorus-Ligated RatsDosage:1, 3, 10, 30 mg/kg Administration:Intraduodenal administration or p.o.Result:Dose-dependently inhibited gastric acid secretion with ID50 values of 2.8, 0.7 mg/kg for intraduodenal administration and oral administration, respectively.Animal Model:Reflux Esophagitis Model in Rats Dosage:1, 3, 10 mg/kg Administration:Intraduodenal administration or p.o.Result:Significantly reduced the lesion scores with ID50 values of 5.4, 1.9 mg/kg for intraduodenal and p.o. respectively.

AKU 517 | R 105266

Membrane Transporter/Ion Channel

Proton Pump

Proton Pump

Other Indications

Ulcer

313272-12-7

339.414

C20H22FN3O

>98% (HPLC)

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C[C@@H]1[C@@H](CN2C(C)=C(C)C3=C2C(OCC4=CC=C(F)C=C4)=NN=C3)C1

7-(4-fluorobenzyloxy)-2,3-dimethyl-1-{[(1S,2S)-2-methyl cyclopropyl]methyl}-1H-pyrrolo[2,3-d]pyridazine

(-20℃)

With Ice Pack

≥ 2 years