中文名 | GGTI-298 |
英文名 | GGTI-298 |
别名 | GGTASE I抑制剂(GGTI298) |
英文别名 | CS-2228 GGTI-298 GGTI298 (CF3CO2H)salt GGTI-298 trifluoroacetate salt N-4-[2(R)-AMINO-3-MERCAPTOPROPYL]AMINO-2-NAPHTHYLBENZOYL-(L)-LEUCINE METHYL ESTER, TFA N-[[4-(2-(R)-AMINO-3-MERCAPTOPROPYL)AMINO]-2-NAPHTHYLBENZOYL]LEUCINE METHYL ESTER TRIFLUOROACETATE SALT N-[[4-(2-(R)-Amino-3-mercaptopropyl)amino]-2-naphthylbenzoyl]leucine methyl ester trifluoroacetate salt N-[4-[2(R)-Amino-3-mercaptopropyl]amino-2-(1-naphthalenyl)benzoyl]-L-leucinemethylestertrifluoroacetatesalt |
CAS | 180977-44-0 |
EINECS | 604-604-1 |
化学式 | C27H33N3O3S |
分子量 | 479.63 |
熔点 | 99.5-100°C |
溶解度 | DMSO: 22 mg/mL |
存储条件 | −20°C |
外观 | 固体 |
颜色 | off-white |
体外研究 | Both RhoA inhibitor (GGTI298) and ROCK inhibitor (H1152) significantly reduce cAMP agonist-stimulated IK(ap), whereas the latter additionally reduces colocalization of KCNN4c with the apical membrane marker wheat germ agglutinin in T84WT cells. Knockdown of DR4 abolishes NF-κB activation, leading to sensitization of DR5-dependent apoptosis induced by the combination of GGTI298 and TRAIL. GGTI298/TRAIL activates NF-κB and inhibits Akt. knockdown of DR5, preventes GGTI298/TRAIL-induced IκBα and p-Akt reduction, suggesting that DR5 mediates reduction of IκBα and p-Akt induced by GGTI298/TRAIL. In contrast, DR4 knockdown further facilitates GGTI298/TRAIL-induced p-Akt reduction. |
体内研究 | The vivo mouse ileal loop experiments show fluid accumulation is reduced in a dose-dependent manner by TRAM-34, GGTI298, or H1152 when injected together with cholera toxin into the loop. |
危险品标志 | Xi - 刺激性物品![]() |
风险术语 | 36/37/38 - 刺激眼睛、呼吸系统和皮肤。 |
安全术语 | S26 - 不慎与眼睛接触后,请立即用大量清水冲洗并征求医生意见。 S36 - 穿戴适当的防护服。 |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.684 ml | 8.422 ml | 16.845 ml |
5 mM | 0.337 ml | 1.684 ml | 3.369 ml |
10 mM | 0.168 ml | 0.842 ml | 1.684 ml |
5 mM | 0.034 ml | 0.168 ml | 0.337 ml |
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