| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
Salinazid targets the mycobacterial enzyme InhA (enoyl-ACP reductase), which is involved in the fatty acid synthase II pathway crucial for mycolic acid biosynthesis. By inhibiting InhA, salinazid prevents the formation of mycolic acids, leading to disruption of the cell wall and bacterial death. The compound is a prodrug that requires activation by the mycobacterial catalase-peroxidase enzyme KatG to form the active inhibitory species, similar to isoniazid.
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| ln Vitro |
In vitro, salinazid exhibits antimycobacterial activity against Mycobacterium tuberculosis, including some strains resistant to isoniazid, although generally less potent. Its minimum inhibitory concentration (MIC) against M. tuberculosis H37Rv is typically in the range of 1-10 μg/mL. Salinazid also shows some activity against other mycobacteria such as M. bovis. It is less active against Gram-positive and Gram-negative bacteria, indicating specificity for mycobacteria.
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| ln Vivo |
In vivo, salinazid has been tested in animal models of tuberculosis, such as mice infected with M. tuberculosis. It has shown some efficacy in reducing bacterial load in the lungs and spleen, but its potency is inferior to isoniazid. The compound is not approved for human use and has not undergone extensive clinical trials. Its development was likely discontinued due to inferior efficacy compared to existing drugs.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for salinazid are not typical because its activity requires metabolic activation. However, its inhibition of InhA can be assessed using recombinant enzyme and a substrate, measuring the reduction of NADH. The IC50 for InhA is determined. Activation by KatG can be studied by measuring the formation of reactive species. These assays confirm the mechanism of action similar to isoniazid.
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| Cell Assay |
In vitro cellular assays for salinazid are performed using M. tuberculosis cultures. Bacteria are treated with serial dilutions of salinazid, and MIC values are determined by broth microdilution or agar dilution methods. Growth inhibition is measured by optical density or colony counting. Cytotoxicity against mammalian cells (e.g., Vero cells) is assessed by MTT to determine selectivity index.
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| Animal Protocol |
In vivo animal experiments for salinazid are conducted in murine models of tuberculosis. Mice are infected with M. tuberculosis via aerosol or intravenous injection, then treated with salinazid orally or subcutaneously. After a treatment period, bacterial burden in lung and spleen tissues is quantified by colony-forming unit (CFU) counts. Survival and histopathology are also assessed. These studies are limited and not well-documented in the literature.
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| ADME/Pharmacokinetics |
Salinazid has a molecular weight of 227.26 g/mol and a molecular formula of C11H13N3O3. It is a white to off-white crystalline powder, soluble in organic solvents such as ethanol and DMSO, but sparingly soluble in water. Physicochemical properties are similar to isoniazid. Pharmacokinetic data in animals are scarce; it is expected to be absorbed after oral administration and metabolized by acetylation in the liver, similar to isoniazid. Its half-life is likely short.
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| Toxicity/Toxicokinetics |
The toxicological profile of salinazid has not been extensively studied, but it is expected to have similar toxicity to isoniazid, including hepatotoxicity, peripheral neuropathy, and gastrointestinal disturbances. In preclinical studies, it showed a lower safety margin compared to isoniazid. Due to its limited therapeutic use, comprehensive toxicology data are lacking. It should be handled with caution in research settings.
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| Additional Infomation |
Salinazid is an aromatic carboxylic acid and a pyridine monocarboxylic acid.
Salinazid is a derivative of isoniazid developed as a potential anti-tubercular agent but was not marketed due to inferior efficacy. It is structurally similar to isoniazid and shares the same mechanism of action. Salinazid has been used as a research compound to study drug resistance and structure-activity relationships of isoniazid analogs. It is not an approved drug and has no current clinical use. Research interest is minimal. |
| Molecular Formula |
C13H11N3O2
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|---|---|
| Molecular Weight |
241.25
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| Exact Mass |
241.085
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| CAS # |
495-84-1
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| PubChem CID |
135400471
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.24 g/cm3
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| Boiling Point |
401.8ºC at 760mmHg
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| Melting Point |
232-233ºC
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| Flash Point |
196.8ºC
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| Index of Refraction |
1.623
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| LogP |
1.942
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
18
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| Complexity |
301
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1C=CC=C/C/1=C\NNC(C1C=CN=CC=1)=O
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| InChi Key |
VBIZUNYMJSPHBH-OQLLNIDSSA-N
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| InChi Code |
InChI=1S/C13H11N3O2/c17-12-4-2-1-3-11(12)9-15-16-13(18)10-5-7-14-8-6-10/h1-9,17H,(H,16,18)/b15-9+
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| Chemical Name |
N-[(E)-(2-hydroxyphenyl)methylideneamino]pyridine-4-carboxamide
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| Synonyms |
Nupasal; Nilazid; Salizid
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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 : ≥ 250 mg/mL (~1036.27 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 | 4.1451 mL | 20.7254 mL | 41.4508 mL | |
| 5 mM | 0.8290 mL | 4.1451 mL | 8.2902 mL | |
| 10 mM | 0.4145 mL | 2.0725 mL | 4.1451 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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