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MK 56 Active Pharmaceutical Intermediates Pyrazinamide 98-96-4 Antibacterial

  • MK 56 Active Pharmaceutical Intermediates Pyrazinamide 98-96-4 Antibacterial
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Product Description

MK 56 Active Pharmaceutical Intermediates Pyrazinamide 98-96-4 Antibacterial


Antibacterial Pharmaceutical Raw Materials Pyrazinamide CAS 98-96-4

Product Name: Pyrazinamide
Synonyms: 2-Carbamylpyrazine;Aldinamid;Aldinamide;Eprazin;Farmizina;MK 56;mk56;NCI-C01785
CAS: 98-96-4
MW: 123.11
EINECS: 202-717-6
Product Categories: Drug bulk;Aromatic Carboxylic Acids, Amides, Anilides, Anhydrides & Salts;Pyrazines, Pyrimidines & Pyridazines;Antitubercular;Pyrazinamide;Pyrazines;Chloropyrazines, etc.;Amide;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Pyrazines, Pyrimidines & Pyridazines;API;Pyrazinoic acid amide;TEBRAZID
Melting point 189-191 °C(lit.)
Storage temp. -20°C Freezer
Water Solubility 15 mg/mL
Merck 7956
Chemical Properties : Crystalline Solid
Usage : Antibacterial (tuberculostatic)
Usage : An antibacterial agent used to study liver toxicity prevention .


Anti-tuberculosis drug

Pyrazinamide is a second-line anti-tuberculosis drug, also known as formamide pyrazine, carbamoyl pyrazine, and isonicotinic acid amine. At room temperature, it appears as a white crystalline powder and is slightly soluble in water and is odorless with slightly bitter taste. It has a good antibacterial effect against human type Mycobacterium tuberculosis with the strongest bactericidal effect at the range of pH value being between 5-5.5. It has especially optimal bactericidal effect against the Mycobacterium tuberculosis inside the slow-growing phagocytic cells in acidic environment. After pyrazinamide penetrates into the phagocytic cells and enter into the body of Mycobacterium tuberculosis, lactamase in vivo make it be de-amidated, being converted to pyrazine acid to play the antibacterial effect.

The in vivo inhibitory concentration is 12.5μg / ml with the concentration of 50 μg / ml being able to kill the Mycobacterium tuberculosis. The inhibitory concentration against Mycobacterium tuberculosis in vivo is 10 times lower than that in vitro with almost no inhibitory effect in a neutral, alkaline environment.

Its anti-bacterial effect is between streptomycin and paramisansodium. It has great toxicity and can easy to produce drug resistance and should be used in combination with other anti-TB drug.

Pyrazinamide has similar chemical structure with nicotinamide and can interfere with the dehydrogenase through substitution of nicotinamide, therefore preventing the dehydrogenation and inhibiting the utilization of oxygen by Mycobacterium tuberculosis, causing death of the bacteria due to failure of normal metabolism.

It is oral easily absorbed and is widely distributed in body tissues and fluids including liver, lung, cerebrospinal fluid, kidney and bile. After 2 hours, its plasma concentration can reach peak. The concentration of cerebrospinal fluid is similar as blood concentrations. It can subject to hepatic metabolism to be hydrolyzed to the pyrazine acid that is a kind of metabolite having antimicrobial activity, then further being hydroxylated into inactive metabolites and excreted in urine after glomerular filtration. The t1 / 2 is about 8 to 10 hours. It can be used in combination with other kind of anti-TB drug fro the treatment of some complex cases of tuberculosis and tubercular meningitis patients.


Pyrazinamide Dosage

When used in combination therapy with other anti-TB drug, the common dose of adult oral administration is: every 6 hours according to the weight 5-8.75mg / kg, or every eight hours according to the weight 6.7-11.7mg / kg; the highest value is 3 g daily.

Upon treatment of the infection of isoniazid resistant bacteria, you can increase the dose to 60 mg/kg daily.

Children should take with caution, the necessary reference amount should be: 20-25mg / kg daily, it should be separately orally administrated in 3 times with the maximum dose being 2 g daily, the treatment course is generally 2 to 3 months, it can not be more than six months.

L-Tryptophan DL-Lysine hydrochloride N-Acetyl-DL-Methionine
L-Threonine DL-Leucine D-Valine
D-Methionine L-Phenylalanine D-Leucine
DL-Isoleucine L-Serine DL-Isoleucine
DL-Threonine L-Leucine DL-Methionine
D-Galactose L-Lysine D-Tryptophan
L-Lysine hydrochloride L-Lysine monohydrochloride D-Threonine
L-lysine Acetate Ammonium chloride L-(+)-Glutamic acid
L-Valine Urea Medication Grad L-Glutamic acid
L-Methionine N-Acetyl-L-Methionine D-Galactose
DL-Methionine N-Acetyl-DL-Methionine L-Alanine
L-(+)-Glutamic acid D-Alanine L-Serine
L-lysine Acetate D-Valine L-Valine
L-Alanine D-Leucine L-Lysine hydrochloride
D-Methionine D-Threonine L-Methionine
D-Threonine D-Methionine L-Tryptophan
D-Valine DL-Isoleucine D-Alanine
D-Isoleucine DL-Phenylalanine D-Leucine
D-Alanine DL-Valine DL-Phenylalanine
DL-Methionine DL-Tryptophan DL-Valine
L-Glutamic acid DL-Methionine DL-Threonine
D-Galactose L-lysine Acetate L-Phenylalanine
DL-Phenylalanine L-(+)-Glutamic acid L-Serine
L-Tryptophan L-Glutamic acid DL-Methionine
L-Tryptophan L-Valine L-Threonine
L-Threonine L-Alanine L-Tryptophan
Sodium caprylate L-Tryptophan D-Arabinose
N-Acetyl-L-Cysteine L-Threonine DL-Threonine
D-Arabinose Zinc Bacitracin L-lysine Acetate
DL-Threonine L-Methionine L-Glutamic acid
L-Threonine DL-Threonine  

MK 56 Active Pharmaceutical Intermediates Pyrazinamide 98-96-4 Antibacterial Images


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