Clomipramine HCl (G34586)

Alias: Clomimipramine; G 34586; 3-Chloroimipramine; G-34586; G34586; Trade names: Anafranil, Clomicalm
Cat No.:V0990 Purity: ≥98%
Clomipramine HCl (G-34586; G34586; Trade names: Anafranil, Clomicalm), the hydrochloride salt of clomipramine which is a tricyclic antidepressant (TCA), is a potent blocker of serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) with Ki of 0.14, 54 and 3 nM, respectively.
Clomipramine HCl (G34586) Chemical Structure CAS No.: 17321-77-6
Product category: 5-HT Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
100mg
500mg
1g
5g
10g
Other Sizes

Other Forms of Clomipramine HCl (G34586):

  • Clomipramine D3 HCl
  • Clomipramine
  • Clomipramine D3
  • Clomipramine-d6 hydrochloride (Chlorimipramine-d6 (hydrochloride); G-34586-d6 (hydrochloride); NSC-169865-d6 (hydrochloride))
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Clomipramine HCl (G-34586; G34586; Trade names: Anafranil, Clomicalm), the hydrochloride salt of clomipramine which is a tricyclic antidepressant (TCA), is a potent blocker of serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) with Ki of 0.14, 54 and 3 nM, respectively. Clomipraminehas been used to treat chronic pain, major depressive disorder, panic disorder, and obsessive compulsive disorder.

Biological Activity I Assay Protocols (From Reference)
Targets
5-HT
ln Vitro
Clomipramine hydrochloride inhibits both norreplenishing and 5-HT replenishment, although clomipramine hydrochloride inhibits 5-HT replenishment more than it inhibits norreplenishing replenishment [1]. It is concentration-dependent, but not for AChE in the brain striatum [2]. Clomipramine hydrochloride interferes with autophagy attenuation and severely impairs the viability of tumor cells leading to cytotoxicity [3]. Clomipramine hydrochloride reduces autophagy in primary neuronal cultures. Clomipramine hydrochloride (1-5 μM) negatively regulates neuronal autophagy staining in cultured primary cells [3]. Western Blot Analysis[3] Cell Line: Primary Cortical Neurons Concentration: 1 and 5 µM Incubation Time: 12, 24 and 48 hours Results: Enhanced LC3-I to LC3-II in a concentration-dependent manner at all analyzed time points transformation.
ln Vivo
Clomipramine Hydrochloride (5 -20 mg/kg; ip) The hydrochloride salt causes significant hypertension in the nozzle. Clomipramine Hydrochloride Promotes Electrode Release by Burning 5-HT2B and/or 5-HT2C Bus Adapters Hypertension In rats, clomipramine hydrochloride reduces immobility in the forced swim test, which is inhibitory to drug resistance. behavioral model. Clomipramine hydrochloride also inhibits the marble burying behavior of rats, an animal model of obsessive-compulsive disorder [1]. Clomipramine (20 mg/animal model: C57BL/6 J mice (6 weeks old, 22 to 25 g) [3] Dose: 20 mg/kg Administration: intraperitoneal injection for 21 days Results: vs. vehicle Both LC3-II and p62 were significantly increased in the livers of clomipramine-treated mice compared with clomipramine-treated mice.
Cell Assay
Cell Line: Primary cortical neurons
Concentration: 1 and 5 µM
Incubation Time: 12, 24 and 48 hours
Result: Enhanced the LC3-I conversion to LC3-II in a concentration-dependent manner at all analyzed time points.
Animal Protocol
C57BL/6 J mice (6 weeks of age and 22 to 25 g)
20 mg/kg
Treated intraperitoneally for 21 days
References

[1]. The tricyclic antidepressant Clomipramine increases plasma glucose levels of mice. J Pharmacol Sci. 2003 Sep;93(1):74-9.

[2]. Comparative study of the inhibitory effect of antidepressants on cholinesterase activity in Bungarus sindanus (krait) venom, human serum and rat striatum. J Enzyme Inhib Med Chem. 2008 Dec;23(6):912-7.

[3]. The tricyclic antidepressant Clomipramine inhibits neuronal autophagic flux. Sci Rep. 2019 Mar 19;9(1):4881.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H24CL2N2
Molecular Weight
351.31
Exact Mass
350.13
Elemental Analysis
C, 64.96; H, 6.89; Cl, 20.18; N, 7.97
CAS #
17321-77-6
Related CAS #
Clomipramine-d3 hydrochloride; 1398065-86-5; Clomipramine; 303-49-1; Clomipramine-d3; 136765-29-2; Clomipramine-d6 hydrochloride; 1189882-28-7; Clomipramine-13C,d3 hydrochloride
Appearance
White to off-white crystalline powder
SMILES
CN(C)CCCN1C2=CC=CC=C2CCC3=C1C=C(C=C3)Cl.Cl
InChi Key
WIMWMKZEIBHDTH-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H23ClN2.ClH/c1-21(2)12-5-13-22-18-7-4-3-6-15(18)8-9-16-10-11-17(20)14-19(16)22;/h3-4,6-7,10-11,14H,5,8-9,12-13H2,1-2H3;1H
Chemical Name
3-(2-chloro-5,6-dihydrobenzo[b][1]benzazepin-11-yl)-N,N-dimethylpropan-1-amine;hydrochloride
Synonyms
Clomimipramine; G 34586; 3-Chloroimipramine; G-34586; G34586; Trade names: Anafranil, Clomicalm
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 50~70 mg/mL (142.3~199.3 mM)
Water: ~70 mg/mL (~199.3 mM)
Ethanol: ~70 mg/mL (~199.3 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 3 mg/mL (8.54 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 3 mg/mL (8.54 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 3 mg/mL (8.54 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


Solubility in Formulation 4: 100 mg/mL (284.65 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.8465 mL 14.2324 mL 28.4649 mL
5 mM 0.5693 mL 2.8465 mL 5.6930 mL
10 mM 0.2846 mL 1.4232 mL 2.8465 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01575158 Completed Drug: Citalopram
Drug: Clomipramine
Drug: placebo
Depression University of Aarhus October 1997 Not Applicable
NCT02028598 Completed Drug: Treatment 1
Drug: Treatment 2
Drug: Treatment 3
Healthy CTC Bio, Inc. January 2014 Phase 1
NCT00254735 Completed Drug: quetiapine fumarate
Drug: SSRI/Clomipramine
Obsessive Compulsive Disorder AstraZeneca April 2002 Phase 3
NCT01439984 Completed Drug: Clomipramine Premature Ejaculation Symyoo September 2011 Phase 3
NCT00564564 Completed Drug: Quetiapine
Drug: Clomipramine
Obsessive Compulsive Disorder University of Sao Paulo January 2006 Phase 4
Biological Data
  • Clomipramine and fluoxetine treatments reduce autophagy flux in cortical neurons. Sci Rep . 2019 Mar 19;9(1):4881.
  • Autophagic flux is decreased by clomipramine treatment in mouse tissues. Sci Rep . 2019 Mar 19;9(1):4881.
  • Clomipramine and fluoxetine modulate C. elegans autophagy in a different manner. Sci Rep . 2019 Mar 19;9(1):4881.
  • The graphs show rat brain striatum acetylcholinesterase experiments in the presence of 0.5 mM different antidepressants (Clom; clomipramine, Sert; sertraline, Paro; paroxetine and Imip; imipramine). J Enzyme Inhib Med Chem . 2008 Dec;23(6):912-7.
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