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Clozapine - 10mM in DMSO, high purity , CAS No.5786-21-0(DMSO), Dopamine D2 receptor antagonist

7 Citations COA COA
In stock
Item Number
C408052
Grouped product items
SKU Size
Availability
 Price Qty
C408052-1ml
1ml
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$39.90
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Bulk Order  SDS  DATASHEET  Specification Sheet

5-HT2 Selective Inhibitors | Agonists | Antagonists | Modulators

View related series
Compound libraries (12325)

Basic Description

Synonyms HF 1854, LX 100-129 | 8-​chloro-​11-​(4-​methyl-​1-​piperazinyl)​-5H-​dibenzo[b,​e]​[1,​4]​diazepine
Specifications & Purity Moligand™, 10mM in DMSO
Biochemical and Physiological Mechanisms Clozapine (HF 1854, LX 100-129) is an atypical antipsychotic drug by acting as a 5-HT antagonist, used in the treatment of schizophrenia.
Storage Temp Store at -80°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade Moligand™
Action Type AGONIST, ALLOSTERIC MODULATOR, ANTAGONIST, GATING INHIBITOR
Mechanism of action Dopamine D2 receptor antagonist
Product Description

Information

Clozapine (HF 1854, LX 100-129) is an atypical antipsychotic drug by acting as a5-HTantagonist, used in the treatment of schizophrenia.
In vitro

Clozapine (10, 20 mg/kg) significantly increases the number of Fos-positive neurons in the nucleus accumbens, medial prefrontal cortex and lateral septal nucleus. Clozapine induces zif268 but not c-fos mRNA in rat striatum, while Haloperidol induces c-Fos-like immunoreactivity in the caudate-putamen. Clozapine is more selective for D4 receptors compared to D2 receptors. Clozapine is a mixed but weak D1/D2 antagonist. Clozapine produces a marked facilitation (300-400%) of NMDA-evoked responses in a concentration-dependent manner with EC50 of 14 nM. Clozapine, but not haloperidol, produces bursts of excitatory postsynaptic potentials (EPSPs), which are blocked by glutamate receptor antagonists, suggesting that these EPSPs are the result of increasing release of excitatory amino acids. Clozapine is a full agonist at the muscarinic M4 receptor (EC50 = 11 nM), producing inhibition of forskolin-stimulated cAMP accumulation. Clozapine potently antagonizes agonist-induced responses at the other four muscarinic receptor subtypes.

In vivo

Clozapine\xa0exhibits an "inverted-U" shaped dose-response\xa0curve, reversing the\xa0apomorphine-induced loss of prepulse\xa0inhibition\xa0(PPI) at low doses but not at high doses in the rats.\xa0Clozapine\xa0decreases PPI independent of\xa0apomorphine\xa0treatment in the rats.\xa0
Cell Data

cell lines：LNCaP cells, PC3 cells

Concentrations：

Incubation Time：

Powder Purity:≥99%

Product Properties

ALogP 3.422
hba_count 1
HBD Count 1
Rotatable Bond 1

Associated Targets(Human)

DRD1 Tclin D(1A) dopamine receptor (9 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
DRD2 Tclin D(2) dopamine receptor (40 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
DRD4 Tchem D(4) dopamine receptor (62 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
HRH4 Tchem Histamine H4 receptor (6 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
HRH1 Tclin Histamine H1 receptor (13 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
SLC6A4 Tclin Sodium-dependent serotonin transporter (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
DRD3 Tclin D(3) dopamine receptor (4 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
CHRM5 Tclin Muscarinic acetylcholine receptor M5 (3 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
CHRM3 Tclin Muscarinic acetylcholine receptor M3 (3 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
CHRM4 Tclin Muscarinic acetylcholine receptor M4 (4 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
ADRA2B Tclin Alpha-2B adrenergic receptor (3 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
CHRM2 Tclin Muscarinic acetylcholine receptor M2 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
ADRA2C Tclin Alpha-2C adrenergic receptor (4 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
HTR2A Tclin 5-hydroxytryptamine receptor 2A (40 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
HTR7 Tclin 5-hydroxytryptamine receptor 7 (28 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
ADRA1B Tclin Alpha-1B adrenergic receptor (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
CHRM1 Tclin Muscarinic acetylcholine receptor M1 (11 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
ADRA2A Tclin Alpha-2A adrenergic receptor (3 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
ADRA1D Tclin Alpha-1D adrenergic receptor (3 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
ADRA1A Tclin Alpha-1A adrenergic receptor (5 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
HTR2C Tclin 5-hydroxytryptamine receptor 2C (28 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
HTR1A Tclin 5-hydroxytryptamine receptor 1A (4 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
HTR3A Tclin 5-hydroxytryptamine receptor 3A (3 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
HTR6 Tchem 5-hydroxytryptamine receptor 6 (20 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
HTR2B Tclin 5-hydroxytryptamine receptor 2B (5 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
H1F0 Tchem Histone H1.0 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 (15 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)

Names and Identifiers

Smiles CN1CCN(CC1)C2=NC3=C(NC4=C2C=CC=C4)C=CC(=C3)Cl
Molecular Weight 326.82
Reaxy-Rn 764984
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=764984&ln=

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Chemical and Physical Properties

Solubility Solubility (25°C) In vitro DMSO: 37 mg/mL (201.53 mM); Water: 37 mg/mL (201.53 mM); Ethanol: 37 mg/mL (201.53 mM);
DMSO(mg / mL) Max Solubility 65
DMSO(mM) Max Solubility 198.89
Water(mg / mL) Max Solubility <1

Citations of This Product

How to Cite Aladdin Scientific Products?
1. Huanhuan Yang, Cong Liu, Chuanhong Zhu, Yan Zheng, Juan Li, Qianyun Zhu, Hao Wang, Xiangming Fang, Quan Liu, Man Liang, Zilong Liu.  (2023)  Determination of ten antipsychotics in blood, hair and nails: Validation of a LC–MS/MS method and forensic application of keratinized matrix analysis.  JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS,  234  (115557). 
2. Xinding Yao, Zhenwei Wang, Yue Geng, Hongkun Zhao, Elaheh Rahimpour, William E. Acree, Abolghasem Jouyban.  (2022)  Hirshfeld surface and electrostatic potential surface analysis of clozapine and its solubility and molecular interactions in aqueous blends.  JOURNAL OF MOLECULAR LIQUIDS,  360  (119328). 
3. Jiajing Xin, Saihong Yan, Xiangsheng Hong, Huan Zhang, Jinmiao Zha.  (2021)  Environmentally relevant concentrations of clozapine induced lipotoxicity and gut microbiota dysbiosis in Chinese rare minnow (Gobiocypris rarus).  ENVIRONMENTAL POLLUTION,  286  (117298). 
4. Yi Gong, Yueru Wang, Zibo Huang, Jiao sha, Yu Li, Tao Li, Baozeng Ren.  (2021)  Solubility, solvent effect, molecular simulation and thermodynamic properties of clozapine in twelve pure solvents.  JOURNAL OF CHEMICAL THERMODYNAMICS,  158  (106398). 
5. Kai Hu, Tiantian Pang, Yanmei Shi, Jiamin Cheng, Yanjie Huang.  (2020)  Facile preparation of a magnetic porous organic frameworks for highly sensitive determination of eight alkaloids in urine samples based UHPLC-MS/MS.  MICROCHEMICAL JOURNAL,  157  (105048). 
6. Juan Cui, Huaping Wang, Zhiqiang Zheng, Qing Shi, Tao Sun, Qiang Huang, Toshio Fukuda.  (2018)  Fabrication of perfusable 3D hepatic lobule-like constructs through assembly of multiple cell type laden hydrogel microstructures.  Biofabrication,  11  (1): (15016). 
7. Danyi Lu, Qian Xie, Baojian Wu.  (2017)  N-glucuronidation catalyzed by UGT1A4 and UGT2B10 in human liver microsomes: Assay optimization and substrate identification.  JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS,  145  (692). 

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