Mediazine (about 0-20 μg/mL, 18 h) inhibits several mycobacteria, with MIC values ranging from 5 μg/mL to 15 μg/mL [1].

Mediazine (ip, 10 μg/gm body weight/day, 6 weeks) exhibits antagonistic effects against mycobacteria in H37Rv-infected mice [1]. Mediizine (oral, 10 mg/kg daily for 28 days) enhances survival in mice infected with Mycobacterium tuberculosis (Mtb) H37Rv [2].

Cell proliferation assay [1]
Cell Types: Mycobacteria: M. smegmatis 798/1546, M., fortuitum 1529, M. scrofulaceum 1323, M. gordonae 1324, M. rnarinum 50, M., flavescens 1541, M. terrae 1450, Mycobacterium tuberculosis, H37Ra 16, H37Rv 16, K1, K2, ICRC bacilli, "Skinnis" bacilli.
Tested Concentrations: Approximately 0-20 μg/mL
Incubation Duration: 18 hrs (hours)
Experimental Results: Inhibition of mycobacteria with MIC values ranging from 5 μg/mL to 15 μg/mL.

Animal/Disease Models: H37Rv infected mice [1]
Doses: 10 μg/gm body weight/day, 6 weeks
Route of Administration: intraperitoneal (ip) injection
Experimental Results: Demonstrated antimycobacterial activity against mycobacteria.

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Animal/Disease Models: Swiss albino male mice infected with Mycobacterium tuberculosis (Mtb) H37Rv [2]
Doses: 10 mg/kg per day for 28 days
Route of Administration: Oral
Experimental Results: Survival time extended to 28 days, no signs of disease, The survival rate is 71.42%.

Absorption, distribution, and excretion It is well absorbed in the digestive tract.

Toxicity Summary
Medechloraz binds to histamine H1 receptors. This blocks the action of endogenous histamine, thereby temporarily relieving histamine-induced adverse symptoms.

[1]. Antimycobacterial activity of methdilazine (Md), an antimicrobic phenothiazine. APMIS. 1993 Jun;101(6):449-54.

[2]. Activity of the phenothiazine methdilazine alone or in combination with isoniazid or streptomycin against Mycobacterium tuberculosis in mice. J Med Microbiol. 2009 Dec;58(Pt 12):1667-1668.

Crystals. (NTP, 1992)
Mederapazine is a phenothiazine compound with a nitrogen atom substituted by a (1-methylpyrrolidone-3-yl)methyl group; it is a first-generation antihistamine with anticholinergic properties. It can be used as a histamine antagonist, cholinergic antagonist, and antipruritic. It is a phenothiazine and N-alkylpyrrolidine compound.
Mederapazine is a phenothiazine compound with antihistamine activity. It is used to treat various skin conditions to relieve itching.
Mederapazine is only present in individuals who have used or taken this drug. It is a phenothiazine compound with antihistamine activity. It is used to treat various skin conditions to relieve itching. Mederapazine binds to histamine H1 receptors, blocking the action of endogenous histamine, thereby temporarily relieving histamine-induced adverse symptoms.
See also: Mederapazine hydrochloride (salt form). Drug Indications Used to relieve symptoms of allergic reactions, especially for controlling pruritic skin conditions. Mechanism of Action Metoprazine binds to histamine H1 receptors, blocking the action of endogenous histamine, thereby temporarily relieving histamine-induced adverse symptoms. Pharmacodynamics In allergic reactions, allergens interact and cross-link with IgE antibodies on the surface of mast cells and basophils. Once a mast cell-antibody-antigen complex is formed, a series of complex reactions occur, ultimately leading to cell degranulation and the release of histamine (and other chemical mediators) from mast cells or basophils. After histamine release, it can react with local or systemic tissues via histamine receptors. Histamine acts on H1 receptors, causing itching, vasodilation, hypotension, flushing, headache, tachycardia, and bronchoconstriction. Histamine also increases vascular permeability, exacerbating pain. Metoprazine is a histamine H1 receptor antagonist. It competes with histamine for normal H1 receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract. It can effectively and temporarily relieve symptoms such as sneezing, watery and itchy eyes, and runny nose caused by hay fever and other upper respiratory allergies.

C18H20N2S

296.4298

296.135

1982-37-2

Methdilazine hydrochloride;1229-35-2

14677

Typically exists as solid at room temperature

1.185 g/cm3

430.4ºC at 760 mmHg

189 to 190 °F (NTP, 1992)
87-88 °C
87 - 88 °C

214.1ºC

4.243

0

3

2

21

339

0

CN1CCC(C1)CN2C3=CC=CC=C3SC4=CC=CC=C42

HTMIBDQKFHUPSX-UHFFFAOYSA-N

InChI=1S/C18H20N2S/c1-19-11-10-14(12-19)13-20-15-6-2-4-8-17(15)21-18-9-5-3-7-16(18)20/h2-9,14H,10-13H2,1H3

10-[(1-methylpyrrolidin-3-yl)methyl]phenothiazine

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)