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| Other Sizes |
| Targets |
Formimidamide acetate does not have a defined biological target as a standalone compound. It is a chemical reagent and synthetic intermediate rather than a pharmacologically active drug. Its function is chemical—serving as a formylating agent and a source of formamidine in organic synthesis. However, it has been reported to have anti-tuberculosis activity and belongs to the class of aminoglycosides, and has been shown to have a potent cytotoxic effect on malignant brain cells in vitro. When used in pharmaceutical synthesis, the final products may target various biological pathways.
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| ln Vitro |
An intermediary in the production of active pharmaceutical ingredients is formamidine acetate. Additionally employed as a condensing agent in the synthesis of imidazole and pyrimidine heterocycles.
In vitro, formimidamide acetate has been reported to have a potent cytotoxic effect on malignant brain cells. It also exhibits anti-tuberculosis activity as a member of the aminoglycoside class. As a chemical reagent, its primary utility is in organic synthesis as an intermediate for the preparation of active pharmaceutical ingredients and as a condensing agent for the preparation of pyrimidine and imidazole heterocycles. In cell-based assays, the compound itself may be evaluated for cytotoxicity, but it is primarily used as a synthetic building block. |
| ln Vivo |
Formimidamide acetate is not a pharmacologically approved drug, but it has been reported to have anti-tuberculosis activity and potent cytotoxic effects on malignant brain cells in vitro. These activities suggest potential in vivo applications, but systematic in vivo pharmacological studies including efficacy in animal models have not been well documented. The compound is primarily used as a chemical intermediate in pharmaceutical synthesis. Any in vivo effects would be associated with the final drug products synthesized from this intermediate, not with the compound itself.
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| Enzyme Assay |
In vitro cytotoxicity assays for formimidamide acetate typically involve malignant brain cell lines (e.g., glioblastoma cells). Cells are cultured in appropriate media and treated with the compound at concentrations ranging from 1-100 µM for 24-72 hours. Cell viability is assessed using MTT or LDH release assays. For anti-tuberculosis activity, the compound is tested against Mycobacterium tuberculosis cultures using broth microdilution methods to determine minimum inhibitory concentrations (MICs). For synthetic applications, the compound is used as a condensing agent in the preparation of pyrimidine and imidazole heterocycles.
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| Cell Assay |
In vitro cell culture experiments with formimidamide acetate typically involve malignant brain cell lines to evaluate its cytotoxic effects. Cells are cultured in DMEM or RPMI medium supplemented with 10% FBS and antibiotics. The compound is dissolved in water or DMSO and added to cells at concentrations ranging from 1-100 µM for 24-72 hours. Cell viability is assessed using MTT, resazurin, or ATP-luminescence assays. Apoptosis is measured using Annexin V/PI staining or caspase activity assays. For anti-tuberculosis studies, the compound is tested against M. tuberculosis in appropriate biosafety level 3 facilities.
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| Animal Protocol |
In vivo animal studies with formimidamide acetate are not well documented, as the compound is primarily used as a chemical reagent and synthetic intermediate. When the compound is used to synthesize drug candidates (e.g., anti-tuberculosis agents), those final products undergo standard preclinical evaluation. Typical protocols for anti-tuberculosis candidates include efficacy studies in mouse models of tuberculosis infection, where animals are treated orally or intraperitoneally with the test compound. Bacterial burden in lungs and spleen is measured by colony counting. Pharmacokinetic and toxicology studies are also conducted as part of drug development.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of formimidamide acetate are not well characterized as it is primarily a chemical reagent rather than a drug substance. Based on its physicochemical properties (molecular weight 104.11, high water solubility, logP approximately -1.0), the compound would be expected to have low oral bioavailability due to poor membrane permeability. It would likely be distributed primarily in extracellular fluid and rapidly cleared via renal excretion. The compound may be metabolized via hydrolysis or conjugation reactions. However, the compound is not intended for human exposure and has not been evaluated in formal pharmacokinetic studies.
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| Toxicity/Toxicokinetics |
Toxicological data for formimidamide acetate indicate that it is a skin and eye irritant. The compound is hygroscopic and moisture-sensitive. Standard laboratory safety precautions should be followed when handling this compound, including the use of gloves, safety glasses, and working in a fume hood. The compound should be stored below +30°C in a dry environment. No acute toxicity, mutagenicity, or carcinogenicity data are available. The compound is not intended for drug, household, or other uses without further formulation and testing.
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| Additional Infomation |
Formimidamide acetate is a versatile reagent used as an intermediate in the synthesis of active pharmaceutical ingredients and as a condensing agent for the preparation of pyrimidine and imidazole heterocycles. It has been reported to have anti-tuberculosis activity and potent cytotoxic effects on malignant brain cells. The compound is hygroscopic and should be handled under dry conditions. It is also known as formamidine acetate. The compound has not undergone clinical trials and is not approved as a pharmaceutical. Its mechanism of action is chemical—serving as a formylating agent and synthetic building block.
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| Molecular Formula |
C3H8N2O2
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|---|---|
| Molecular Weight |
104.11
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| Exact Mass |
104.058
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| CAS # |
3473-63-0
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| Related CAS # |
463-52-5 (Parent)
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| PubChem CID |
160693
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| Appearance |
White to off-white solid powder
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| Density |
1.124
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| Boiling Point |
117.1ºC at 760 mmHg
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| Melting Point |
158-161 °C (dec.)(lit.)
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| Flash Point |
40ºC
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| LogP |
0.443
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
7
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| Complexity |
41.3
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O([H])C(C([H])([H])[H])=O.N([H])([H])/C(/[H])=N/[H]
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| InChi Key |
XPOLVIIHTDKJRY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C2H4O2.CH4N2/c1-2(3)4;2-1-3/h1H3,(H,3,4);1H,(H3,2,3)
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| Chemical Name |
acetic acid;methanimidamide
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
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
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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 | 9.6052 mL | 48.0261 mL | 96.0523 mL | |
| 5 mM | 1.9210 mL | 9.6052 mL | 19.2105 mL | |
| 10 mM | 0.9605 mL | 4.8026 mL | 9.6052 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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