Halopemide
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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:
[1] Scott, S. A.,Selvy, P.E.,Buck, J.R., et al. Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness. Nature Chemical Biology 5(2), 108-117 (2009).
[2] Loonen AJ, van Wijngaarden I, Janssen PA, Soudijn W. Regional localization of halopemide, a new psychotropic agent, in the rat brain. Eur J Pharmacol. 1978 Aug 15;50(4):403-8.
[3] De Cuyper H, van Praag HM, Verstraeten D. The clinical significance of halopemide, a dopamine-blocker related to the butyrophenones. Neuropsychobiology. 1984;12(4):211-6.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 416.9 |
Cas No. | 59831-65-1 |
Formula | C21H22ClFN4O2 |
Synonyms | NSC 354856,R34301 |
Solubility | ≤10mg/ml in DMSO;20mg/ml in dimethyl formamide |
Chemical Name | N-[2-[4-(5-chloro-2,3-dihydro-2-oxo-1H-benzimidazol-1-yl)-1-piperidinyl]-ethyl]-4-fluoro-benzamide |
SDF | Download SDF |
Canonical SMILES | ClC1=CC2=C(N(C3CCN(CCNC(C4=CC=C(F)C=C4)=O)CC3)C(N2)=O)C=C1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |