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Clotrimazole Antineoplastic and Immunosuppressive Antibiotics inhibitor

Name: Clotrimazole
Brand: Selleck Chemicals
SKU: S1606
Availability: InStock
Rating: 5 (5 reviews)

Cat.No.S1606

Clotrimazole (BAY b 5097, FB 5097) alters the permeability of the fungal cell wall by inhibiting the biosynthesis of ergosterol, used in the treatment of fungal infections.

Chemical Structure

Molecular Weight: 344.84

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Quality Control

Batch: Purity: 99.97%

99.97

Related Targets	Integrase Bacterial Antibiotics Anti-infection Fungal Antiviral COVID-19 Parasite Reverse Transcriptase HIV
Other Antineoplastic and Immunosuppressive Antibiotics Inhibitors	Staurosporine (STS) Cyclosporin A Oligomycin A (MCH 32) Puromycin Dihydrochloride Nigericin sodium salt Geldanamycin (NSC 122750) Honokiol Streptozotocin (STZ) Sodium Monensin (NSC 343257) Cephalomannine

Solubility

In vitro
Batch:

Ethanol : 69 mg/mL

DMSO : 11 mg/mL (31.89 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.550mg/ml (1.59mM)	Taking the 1 mL working solution as an example, add 50 μL of 11 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.550mg/ml (1.59mM)	Taking the 1 mL working solution as an example, add 50 μL of 11 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

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 ddH₂O, 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.

Chemical Information, Storage & Stability

Molecular Weight	344.84	Formula	C₂₂H₁₇ClN₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	23593-75-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	BAY b 5097, FB 5097			Smiles	C1=CC=C(C=C1)C(C2=CC=CC=C2)(C3=CC=CC=C3Cl)N4C=CN=C4

Mechanism of Action

In vitro	Clotrimazole causes a sustained depletion of intracellular Ca2+ stores, which results in activation of PKR, phosphorylation of eIF2alpha, and thereby in inhibition of protein synthesis at the level of translation initiation. This compound preferentially decreases the expression of the growth promoting proteins cyclin A, E and D1, resulting in inhibition of cyclin-dependent kinase activity and blockage of cell cycle in G1. It inhibits ADP-ribose-activated currents in HEK-293 cells expressing recombinant human TRPM2(hTRPM2). This chemical (3 mM to 30 mM) produces an essentially complete inhibition of theTRPM2-mediated current. It antagonizes ADP-ribose-activated whole-cell and single-channel currents in the rat insulinoma cell-line CRI-G1. This compound (2 mM) causes a sharp decline in parasitemia, complete inhibition of parasite replication, and destruction of parasites and host cells within a single intraerythrocytic asexual cycle (approximately 48 hours). It effectively and rapidly inhibits parasite growth in five different strains of P. falciparum, in vitro, irrespective of their Chloroquine sensitivity.
In vivo	Clotrimazole stimulates a subset of capsaicin-sensitive and mustard oil-sensitive trigeminal neurons, and evoked nocifensive behavior and thermal hypersensitivity with intraplantar injection in mice. This compound-induced pain behavior is suppressed by the TRPV1-antagonist BCTC [(N-(-4-tertiarybutylphenyl)-4-(3-cholorpyridin-2-yl)tetrahydropyrazine-1(2H)-carboxamide)] and absent in TRPV1-deficient mice. It inhibits the cold and menthol receptor TRPM8, and blocks menthol-induced responses in capsaicin- and mustard oil-insensitive trigeminal neurons.
References	[1] https://pubmed.ncbi.nlm.nih.gov/9653178/ [2] https://pubmed.ncbi.nlm.nih.gov/19881520/ [3] https://pubmed.ncbi.nlm.nih.gov/10618418/ [4] https://pubmed.ncbi.nlm.nih.gov/18199759/

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