| CAS NO: | 59831-65-1 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Cas No. | 59831-65-1 |
| 别名 | 卤培米特,NSC 354856,R34301 |
| 化学名 | N-[2-[4-(5-chloro-2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)-1-piperidinyl]-ethyl]-4-fluoro-benzamide |
| Canonical SMILES | ClC1=CC2=C(N(C3CCN(CCNC(C4=CC=C(F)C=C4)=O)CC3)C(N2)=O)C=C1 |
| 分子式 | C21H22ClFN4O2 |
| 分子量 | 416.9 |
| 溶解度 | ≤10mg/ml in DMSO;20mg/ml in dimethyl formamide |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | IC50: 220 and 310 nM for human PLD1 and PLD2, respectively Halopemide is a phospholipase D (PLD) inhibitor. Phospholipase D (PLD) is a key enzyme for the production of phosphatidic acid, a lipid second messenger. Phosphatidic acid involves in both G protein-coupled receptor and receptor tyrosine kinase signal transduction networks. In vitro: In a previous study, the IC50 of halopemide against PLD2 was found to be similar to that previously reported, but the compound had no preference for PLD2 over PLD1 [1]. In vivo: Animal study showed that the halopemide concentration in the rat brain was 10 times less than that of R29800, its chemical analog. However, the levels were the same in the pituitary gland. The highest level of halopemide was found to be in septal and thalamic areas while the neuroleptics were concentrated in the caudate nucleus. Moreover, in the caudate nucleus, halopemide was far less particle-bound [2]. Clinical trial: The activating and resocializing properties of halopemide were evaluating in an open and double-blind study in patients with various psychiatric disorders. The results showed a significant improvement in contact and activity, regardless of the nosological characteristics. Moreover, no significant difference in therapeutic effect between the single and the double dose was found [3]. References: |
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