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MedKoo Cat#: 317562 | Name: Clozapine
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Clozapine is an atypical antipsychotic drug because it binds to serotonin as well as dopamine receptors. Clozapine is a partial agonist at the 5-HT1A subunit of the serotonin receptor, putatively improving depression, anxiety, and the negative cognitive symptoms associated with schizophrenia. A direct interaction of clozapine with the GABAB receptor has also been shown. GABAB receptor-deficient mice exhibit increased extracellular dopamine levels and altered locomotor behaviour equivalent to that in schizophrenia animal models.

Chemical Structure

Clozapine
Clozapine
CAS#5786-21-0 (free base)

Theoretical Analysis

MedKoo Cat#: 317562

Name: Clozapine

CAS#: 5786-21-0 (free base)

Chemical Formula: C18H19ClN4

Exact Mass: 326.1298

Molecular Weight: 326.82

Elemental Analysis: C, 66.15; H, 5.86; Cl, 10.85; N, 17.14

Price and Availability

Size Price Availability Quantity
200mg USD 550.00 2 Weeks
500mg USD 950.00 2 Weeks
1g USD 1,450.00 2 Weeks
2g USD 2,650.00 2 Weeks
5g USD 5,450.00 2 Weeks
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Related CAS #
54241-01-9 (HCl) 34233-69-7 (N-oxide) 5786-21-0 (free base)
Synonym
Leponex; Fazaclo; CLOZARIL; Clozapin; Clozaril; Leponex; HF 1854; HF1854; HF-1854
IUPAC/Chemical Name
8-chloro-11-(4-methylpiperazin-1-yl)-10H-dibenzo[b,e][1,4]diazepine
InChi Key
ZUXABONWMNSFBN-UHFFFAOYSA-N
InChi Code
InChI=1S/C18H19ClN4/c1-22-8-10-23(11-9-22)18-14-4-2-3-5-15(14)20-16-7-6-13(19)12-17(16)21-18/h2-7,12,21H,8-11H2,1H3
SMILES Code
CN1CCN(CC1)C2=C3C=CC=CC3=NC4=C(N2)C=C(C=C4)Cl
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Clozapine is a potent antagonist of dopamine and a number of other receptors, with a Ki of 9.5 nM for muscarinic M1 receptor.
In vitro activity:
Clozapine binding affected fibrin formation by reducing coagulation speed and thickness of fibrin fibers suggesting that in the presence of clozapine, fibrinogen may acquire thrombogenic characteristics. ORAC and HORAC assays showed that clozapine reduced free radical-induced oxidation of fibrinogen. Reference: Int J Biol Macromol. 2020 Jul 1;154:142-149. https://pubmed.ncbi.nlm.nih.gov/32184141/
In vivo activity:
While control animals treated with vehicle showed marked signs of EAE with a mean score of 4.3 ± 0.7 at the peak of EAE and chronification over more than 50 d, clozapine led to a dose-dependent reduction of clinical signs (Figure 2B). Disease incidence declined dose-dependently following clozapine administration (Additional Table 3). Moreover, the onset of clinical signs was delayed by 3 d in 15 mg/kg treated mice. Reference: Front Immunol. 2021; 12: 656941. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8126707/
Solvent mg/mL mM comments
Solubility
DMSO 39.4 120.62
DMSO:PBS (pH 7.2) (1:1) 0.5 1.53
DMF 10.0 30.60
Ethanol 35.0 107.09
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 326.82 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Gligorijević N, Vasović T, Lević S, Miljević Č, Nedić O, Nikolić M. Atypical antipsychotic clozapine binds fibrinogen and affects fibrin formation. Int J Biol Macromol. 2020 Jul 1;154:142-149. doi: 10.1016/j.ijbiomac.2020.03.119. Epub 2020 Mar 14. PMID: 32184141. 2. Giridharan VV, Scaini G, Colpo GD, Doifode T, Pinjari OF, Teixeira AL, Petronilho F, Macêdo D, Quevedo J, Barichello T. Clozapine Prevents Poly (I:C) Induced Inflammation by Modulating NLRP3 Pathway in Microglial Cells. Cells. 2020 Feb 28;9(3):577. doi: 10.3390/cells9030577. PMID: 32121312; PMCID: PMC7140445. 3. Ceylan U, Haupeltshofer S, Kämper L, Dann J, Ambrosius B, Gold R, Faissner S. Clozapine Regulates Microglia and Is Effective in Chronic Experimental Autoimmune Encephalomyelitis. Front Immunol. 2021 May 3;12:656941. doi: 10.3389/fimmu.2021.656941. PMID: 34012440; PMCID: PMC8126707. 4. Robichon K, Patel V, Connor B, La Flamme AC. Clozapine reduces infiltration into the CNS by targeting migration in experimental autoimmune encephalomyelitis. J Neuroinflammation. 2020 Feb 12;17(1):53. doi: 10.1186/s12974-020-01733-4. PMID: 32050980; PMCID: PMC7014621.
In vitro protocol:
1. Gligorijević N, Vasović T, Lević S, Miljević Č, Nedić O, Nikolić M. Atypical antipsychotic clozapine binds fibrinogen and affects fibrin formation. Int J Biol Macromol. 2020 Jul 1;154:142-149. doi: 10.1016/j.ijbiomac.2020.03.119. Epub 2020 Mar 14. PMID: 32184141. 2. Giridharan VV, Scaini G, Colpo GD, Doifode T, Pinjari OF, Teixeira AL, Petronilho F, Macêdo D, Quevedo J, Barichello T. Clozapine Prevents Poly (I:C) Induced Inflammation by Modulating NLRP3 Pathway in Microglial Cells. Cells. 2020 Feb 28;9(3):577. doi: 10.3390/cells9030577. PMID: 32121312; PMCID: PMC7140445.
In vivo protocol:
1. Ceylan U, Haupeltshofer S, Kämper L, Dann J, Ambrosius B, Gold R, Faissner S. Clozapine Regulates Microglia and Is Effective in Chronic Experimental Autoimmune Encephalomyelitis. Front Immunol. 2021 May 3;12:656941. doi: 10.3389/fimmu.2021.656941. PMID: 34012440; PMCID: PMC8126707. 2. Robichon K, Patel V, Connor B, La Flamme AC. Clozapine reduces infiltration into the CNS by targeting migration in experimental autoimmune encephalomyelitis. J Neuroinflammation. 2020 Feb 12;17(1):53. doi: 10.1186/s12974-020-01733-4. PMID: 32050980; PMCID: PMC7014621.
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