| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
Pasiniazid targets enzymes essential for mycolic acid biosynthesis in mycobacteria. It disrupts cell wall synthesis, thereby inhibiting the growth of Mycobacterium tuberculosis. It also displays activity as an inhibitor of Human Jumonji Domain Containing 2E (JMJD2E) with a potency of 39,810.7 nM and Tyrosyl-DNA Phosphodiesterase (TDP1) with a potency of 5,623.4 nM.
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| ln Vitro |
In vitro, pasiniazid is a potent antimicrobial agent against Mycobacterium tuberculosis. It inhibits Human Jumonji Domain Containing 2E (JMJD2E) with a potency of 39,810.7 nM. It inhibits Tyrosyl-DNA Phosphodiesterase (TDP1) with a potency of 5,623.4 nM. It displays bioactivity as a COX inhibitor and NADPH inhibitor.
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| ln Vivo |
In vivo, pasiniazid is used as an anti-TB and anti-leprosy drug. It is active against several species of rapidly growing mycobacteria (RGM). The compound is used to treat various types of tuberculosis and leprosy.
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| Enzyme Assay |
In vitro enzyme assays for pasiniazid measure its inhibition of mycolic acid biosynthesis in mycobacteria. Inhibition of JMJD2E is assessed at 39,810.7 nM. Inhibition of TDP1 is assessed at 5,623.4 nM. COX and NADPH inhibition are measured using standard enzyme assays.
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| Cell Assay |
In vitro cell-based assays for pasiniazid use Mycobacterium tuberculosis cultures to assess antimicrobial activity. Minimum inhibitory concentrations (MIC) are determined using broth microdilution methods. The compound's effects on mycobacterial growth and cell wall synthesis are evaluated.
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| Animal Protocol |
In vivo animal models for pasiniazid include models of tuberculosis and leprosy. The compound is administered orally or by injection, and its effects on bacterial load, survival, and clinical signs of infection are evaluated. Pharmacokinetic studies measure drug exposure and tissue distribution.
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| ADME/Pharmacokinetics |
Pasiniazid has a molecular formula of C₁₃H₁₄N₄O₄ and a molecular weight of 290.28 g/mol. It is also known as 4-amino-2-hydroxybenzoic acid; pyridine-4-carbohydrazide. It is soluble in DMSO at 50 mg/mL. The compound is stored at room temperature. It is a derivative of isonicotinic acid.
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| Toxicity/Toxicokinetics |
The toxicity profile of pasiniazid is similar to that of other anti-tuberculosis drugs. Common adverse effects may include hepatotoxicity and gastrointestinal disturbances. The compound is for research use and clinical use as approved. Appropriate safety precautions should be taken during handling.
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| Additional Infomation |
Pasiniazid is an anti-tuberculosis and anti-leprosy drug used to treat various types of TB and leprosy. It targets mycolic acid biosynthesis in mycobacteria, disrupting cell wall synthesis. Pasiniazid is also known as 帕司烟肼. It displays a mechanism of action similar to that of isoniazid.
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| Molecular Formula |
C13H14N4O4
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|---|---|
| Molecular Weight |
290.2747
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| Exact Mass |
290.102
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| CAS # |
2066-89-9
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| PubChem CID |
16367
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| Appearance |
Typically exists as solid at room temperature
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| Boiling Point |
380.8ºC at 760 mmHg
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| Melting Point |
142-144°
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| Flash Point |
184.1ºC
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| Vapour Pressure |
1.78E-06mmHg at 25°C
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| LogP |
2.03
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
21
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| Complexity |
280
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O([H])C1C([H])=C(C([H])=C([H])C=1C(=O)O[H])N([H])[H].O=C(C1C([H])=C([H])N=C([H])C=1[H])N([H])N([H])[H]
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| InChi Key |
RKPHTRVPGYGVQD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C7H7NO3.C6H7N3O/c8-4-1-2-5(7(10)11)6(9)3-4;7-9-6(10)5-1-3-8-4-2-5/h1-3,9H,8H2,(H,10,11);1-4H,7H2,(H,9,10)
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| Chemical Name |
4-amino-2-hydroxybenzoic acid;pyridine-4-carbohydrazide
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ≥ 160 mg/mL (~551.21 mM)
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| Solubility (In Vivo) |
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.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] Oral Formulations
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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4451 mL | 17.2253 mL | 34.4507 mL | |
| 5 mM | 0.6890 mL | 3.4451 mL | 6.8901 mL | |
| 10 mM | 0.3445 mL | 1.7225 mL | 3.4451 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.
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.
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