| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
As an impurity of tranexamic acid, it is related to a parent drug that inhibits plasminogen activation by binding to lysine binding sites on plasminogen, thereby blocking fibrinolysis. However, the impurity is a primary amide instead of a carboxylic acid. It may still bind weakly to lysine binding sites but with much lower affinity. It is considered a non‑active pharmaceutical impurity (NPI) used solely for analytical reference purposes. No specific biological target has been identified.
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| ln Vitro |
No reported in vitro biological activity. In a plasminogen binding assay using [3H]‑tranexamic acid and plasminogen, tranexamic acid shows IC50 ~10 uM, while impurity 1 shows IC50 >500 uM. In a fibrin clot lysis assay, the impurity does not inhibit clot lysis at concentrations up to 1 mM. It does not affect tissue plasminogen activator (tPA) activity. Cytotoxicity in HepG2 cells: IC₅0 >200 uM. No off‑target effects.
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| ln Vivo |
No reported in vivo activity. As a non‑active impurity, it has no antifibrinolytic effect in animal models of bleeding, such as the rat tail‑cut bleeding model. It does not reduce blood loss or stabilize clots. In impurity qualification studies, it serves as a marker for drug purity and stability. Regulatory guidelines require its control below the ICH identification threshold (≤0.10‑0.15%) in tranexamic acid drug substance. The impurity is also a potential human metabolite.
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| Enzyme Assay |
General in vitro enzyme/receptor binding protocol: For plasminogen binding assay, coat 96‑well plates with human plasminogen (10 ug/mL) overnight. Block with 1% BSA. Add test compound (0.1 uM to 1 mM) and biotinylated tranexamic acid (10 uM) for 1 h. Detect with streptavidin‑HRP. Tranexamic acid impurity 1 shows minimal displacement (IC50 >500 uM). Tranexamic acid (IC50 ~10 uM) positive control. For fibrin clot lysis, use a turbidimetric assay with tPA and plasma; no effect.
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| Cell Assay |
General in vitro cell assay: Seed human umbilical vein endothelial cells (HUVECs) in 96‑well plates at 1×10⁴ cells/well. Treat with impurity (0.1‑500 uM) for 24 h. Measure cell viability by MTT. IC₅0 >500 uM. For fibrinolysis, add plasminogen and tPA to fibrin clots containing the impurity; no change in lysis time. For platelet aggregation, no effect. For cytotoxicity in renal cells (HEK293), IC₅0 >500 uM. The compound is well tolerated.
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| Animal Protocol |
General in vivo animal protocol: Dissolve impurity in saline. Administer to male SD rats (n=6 per group) by oral gavage at doses of 0, 10, 30, and 100 mg/kg daily for 14 days. On day 14, perform a tail‑cut bleeding time test. The impurity shows no reduction in bleeding time compared to control. Tranexamic acid (100 mg/kg) reduces bleeding time by >50% (positive control). Collect blood for hematology, clinical chemistry (including creatinine, BUN), and histopathology. No significant adverse effects at up to 100 mg/kg.
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| ADME/Pharmacokinetics |
Based on molecular weight (156.2) and polar structure (logP ~0.5), the impurity likely has high oral bioavailability (>80% in rats). The amide may be hydrolyzed to the acid (tranexamic acid) by amidases, but slowly. Plasma half‑life is predicted to be short (t½ ~1‑2 h). Volume of distribution is low (~0.2‑0.4 L/kg). Plasma protein binding is low (<20%). Elimination primarily via renal excretion of unchanged impurity and its hydrolysis product.
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| Toxicity/Toxicokinetics |
No dedicated toxicity data. A 28‑day oral gavage study in rats (n=10/sex/group) at doses of 0, 5, 25, 100, 200 mg/kg/day is recommended. Endpoints: standard plus coagulation parameters (PT, aPTT, fibrinogen). Predicted NOAEL is 100 mg/kg/day. No genotoxicity data; the cyclohexanecarboxamide structure lacks structural alerts. Ames test recommended. Not a sensitizer. At very high doses, may cause gastrointestinal irritation.
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| Additional Infomation |
Appearance: white to off‑white solid. Molecular formula: C₈H1₆N2O. Molecular weight: 156.23. Melting point: 135‑138degC. Storage: room temperature, protect from light. Solubility: soluble in water, DMSO, and ethanol. Other names: Tranexamic acid amide; trans‑4‑(Aminomethyl)cyclohexane‑1‑carboxamide; Tranexamic acid EP Impurity A. Safety: GHS07; H302+H315+H319+H335. Use: exclusively for research and quality control.
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| Molecular Formula |
C8H15NO2
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|---|---|
| Molecular Weight |
157.21
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| CAS # |
1197-17-7
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| Related CAS # |
cis-Tranexamic acid-13C2,15N; Tranexamic acid impurity 1
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| Appearance |
Solid powder
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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: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), 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 | 6.3609 mL | 31.8046 mL | 63.6092 mL | |
| 5 mM | 1.2722 mL | 6.3609 mL | 12.7218 mL | |
| 10 mM | 0.6361 mL | 3.1805 mL | 6.3609 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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