| 中文名称: | GGTI298 | ||||
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| 英文名称: | GGTI298 | ||||
| 别名: | GGTI298 (S)-methyl 2-(4-(((R)-2-amino-3-mercaptopropyl)amino)-2-(naphthalen-1-yl)benzamido)-4-methylpentanoate | ||||
| CAS No: | 180977-44-0 | 分子式: | C27H33N3O3S | 分子量: | 479.63 |
| CAS No: | 180977-44-0 | ||||
| 分子式: | C27H33N3O3S | ||||
| 分子量: | 479.63 | ||||
基本信息
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产品编号： |
G10351 |
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产品名称： |
GGTI298 |
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CAS: |
180977-44-0 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
6个月 |
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分子量： |
479.63 |
-20℃ |
1个月 |
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化学名： |
L-Leucine,N-[4-[[(2R)-2-amino-3-mercaptopropyl]amino]-2-(1-naphthalenyl)benzoyl]-,methylester |
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Solubility (25°C)： |
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体外:
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DMSO |
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Ethanol |
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Water |
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体内(现配现用): |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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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。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
2.0849mL |
10.4247mL |
20.8494mL |
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5mM |
0.4170mL |
2.0849mL |
4.1699mL |
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10mM |
0.2085mL |
1.0425mL |
2.0849mL |
生物活性
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产品描述 |
一种有效的 GGTase I 抑制剂，能够抑制 geranylgeranylated Rap1A 的过程，对 farnesylated Ha-Ras 的过程也有一定影响，在体内，IC50 值分别为 3和>20μM。 |
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靶点 |
IC50:3μM (Rap1A,in vivo),>20μM (Ha-Ras,in vivo) |
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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. |
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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. |
推荐实验方法(仅供参考)
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激酶实验： |
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The given cells are lysed with Reporter Lysis Buffer and subjected to luciferase activity assay using Luciferase Assay System in a luminometer.Relative luciferase activity is normalized to protein content. |
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细胞实验: |
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Cells are seeded in 96-well cell culture plates and treated the next day with the agents indicated.The viable cell number is determined using the sulforhodamine B assay. |
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动物实验: |
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The ileal loop experiment is performed in 6-8-week-old mice by a modified rabbit ileal loop assay.Following gut sterilization,the animals are kept fasted for 24h prior to surgery and fed only water ad libitum.Anesthesia is induced by a mixture of ketamine (35mg/kg of body weight) and xylazine (5mg/kg of body weight).A laparotomy is performed,and the experimental loops of 5-cm length are constricted at the terminal ileum by tying with non-absorbable silk.The following fluids are instilled in each loop by means of a tuberculin syringe fitted with a disposable needle through the ligated end of the loop as the ligatured is tightened: pure CT (1μg;positive control),saline (negative control),CT (1μg)+TRAM-34 (different concentrations inμM as indicated in Fig.7),CT (1μg) + H1152 (1μM),and CT (1μg)+GGTI298 (different concentrations inμM),a specific inhibitor of Rap1A.The intestine is returned to the peritoneum,and the mice are sutured and returned to their cages.After 6h,these animals are sacrificed by cervical dislocation,and the loops are excised.The fluid from each loop is collected,and the ratio of the amount of fluid contained in the loop with respect to the length of the loop (fluid accumulation ratio in g/cm) is calculated as a reflection of the efficacy of various inhibitors. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
