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CFTR(inh)-172

CAS No. : 307510-92-5

MCE 国际站：CFTR(inh)-172

产品活性：CFTR(inh)-172 是高效选择性的 CFTR 通道阻断剂; 在2分钟内可逆地抑制CFTR短路电流的 K_i 值为300 nM。

研究领域：Membrane Transporter/Ion Channel  |  Autophagy

作用靶点：CFTR  |  Autophagy

In Vitro: Inhibition by CFTR(inh)-172 is complete in approximately 10 minutes (t_1/2=4 minutes) and is reversed after ishout with t_1/2 approximately 5 minutes. CFTRinh-172 is nontoxic to FRT cells after 24 hours at concentrations up to 100 μM. CFTR(inh)-172 does not alter CFTR unitary conductance (8 pS), but reduces open probability by > 90% with K_i=0.6 μM. This effect is due to increased mean channel closed time without changing mean channel open time. The K_i values for inhibition of Cl^- current in wild-type, G551D, and G1349D CFTR are about 0.5 μM; however, K_i is significantly reduced to 0.2 μM for vF508 CFTR.

In Vivo: A single intraperitoneal injection of CFTR(inh)-172 (250 μg/kg) in mice reduces by more than 90% cholera toxin–induced fluid secretion in the small intestine over 6 hours. CFTR(inh)-172 is nontoxic at high concentrations in mouse models. CFTRinh-172 significantly reduces fluid secretion to that in saline control loops, whereas an inactive CFTRinh-172 analog does not inhibit fluid secretion.

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