SRI-37240是一种有效的提前终止密码子 (PTCs) 抑制剂。SRI-37240 抑制CFTR的无义突变。在 HEK293T 细胞中，SRI-37240 改变 PTCs 的细胞翻译终止。当与 G418 使用联合时，SRI-37240 还能恢复原发性支气管上皮细胞的 CFTR 功能。
| 生物活性 | SRI-37240 is a potentpremature termination codons(PTCs) inhibitor. SRI-37240 suppressesCFTRnonsense mutations. SRI-37240 alters cellular translation termination at PTCs in HEK293T cells. SRI-37240 can also restoreCFTRfunction in primary bronchial epithelial cells when combination with G418[1]. |
| IC50& Target | Premature termination codons, CFTR[1] |
体外研究
(In Vitro) | SRI-37240 (1, 3, 10 and 30 μM; 48 h) induces concentration-dependent increases in CFTR-dependent (Forskolin-stimulated and sensitive to the inhibitor CFTRInh-172) chloride conductance[1].
SRI-37240 (10 μM; 72 h) significantly increases the amount of full-length, fully glycosylated form of CFTR protein, and the unprocessed, immature form of full-length CFTR protein in 16HBEge cells when co-treated with G418 (100 μM)[1].
SRI-37240 (10 μM; 24 h) alters cellular translation termination at PTCs in HEK293T cells, also increases global densities of ribosomes at normal stop codons without affecting densities of ribosomes in 3-UTRs[1].
SRI-37240 (10 μM; 72 h) restores CFTR function in primary bronchial epithelial cells when combination with G418[1].
Western Blot Analysis[1] | Cell Line: | CFTR-G542X 16HBEge | | Concentration: | 10 μM | | Incubation Time: | 24 h | | Result: | Significantly increased the amount of Band C CFTR protein, which represents the full-length, fully glycosylated form of CFTR and Band B, which represents the unprocessed, immature form of full-length CFTR protein when combined with G418 (100 μM). |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 11.36 mg/mL(29.47 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.5943 mL | 12.9715 mL | 25.9430 mL | | 5 mM | 0.5189 mL | 2.5943 mL | 5.1886 mL | | 10 mM | 0.2594 mL | 1.2972 mL | 2.5943 mL |
*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。 |
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