CFTR(inh)-172 is a potent and selective blocker of theCFTRchloride channel; reversibly inhibitsCFTRshort-circuit current in less than 2 minutes with aK_iof 300 nM.

Ki: 300 nM (CFTR)^[1]

Inhibition by CFTR(inh)-172 is complete in approximately 10 minutes (t_1/2=4 minutes) and is reversed after ishout with t_1/2approximately 5 minutes. CFTRinh-172 is nontoxic to FRT cells after 24 hours at concentrations up to 100 μM^[1]. 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_ivalues for inhibition of Cl^-current in wild-type, G551D, and G1349D CFTR are about 0.5 μM; however, K_iis significantly reduced to 0.2 μM for vF508 CFTR^[2].

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^[1].

409.40

Solid

C₁₈H₁₀F₃NO₃S₂

307510-92-5

Room temperature in continental US; may vary elsewhere.

DMSO : 50 mg/mL(122.13 mM;Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: 2.5 mg/mL (6.11 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.5 mg/mL (6.11 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.5 mg/mL (6.11 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (6.11 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。