Clozapine
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MedKoo CAT#: 317562

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

Description: 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

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Clozapine
CAS# 5786-21-0 (free base)
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 317562
Name: Clozapine
CAS#: 5786-21-0 (free base)
Chemical Formula: C18H19ClN4
Exact Mass: 326.13
Molecular Weight: 326.820
Elemental Analysis: C, 66.15; H, 5.86; Cl, 10.85; N, 17.14

Price and Availability

Size Price Availability Quantity
200mg USD 550
500mg USD 950
1g USD 1450
2g USD 2650
5g USD 5450
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Related CAS #: 54241-01-9 (HCl)   34233-69-7 (N-oxide)   5786-21-0 (free base)  

Synonym: Leponex; Fazaclo; CLOZARIL; 5786-21-0; Clozapin; Clozaril; Leponex

IUPAC/Chemical Name: 3-chloro-6-(4-methylpiperazin-1-yl)-5H-benzo[b][1,4]benzodiazepine

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:
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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/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
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

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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