Halopemide (Synonyms: NSC 354856,R34301) |
カタログ番号GC11243
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ハロペミドは強力なホスホリパーゼ D (PLD) 阻害剤であり、ヒト PLD1 と PLD2 の IC50 はそれぞれ 220 nM と 310 nM です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 59831-65-1
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 59831-65-1 | SDF | |
| 同義語 | NSC 354856,R34301 | ||
| Chemical Name | 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 | ||
| Formula | C21H22ClFN4O2 | M.Wt | 416.9 |
| 溶解度 | ≤10mg/ml in DMSO;20mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3987 mL | 11.9933 mL | 23.9866 mL |
| 5 mM | 479.7 μL | 2.3987 mL | 4.7973 mL |
| 10 mM | 239.9 μL | 1.1993 mL | 2.3987 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)