| Size | Price | Stock | Qty |
|---|---|---|---|
| 10g |
|
||
| Other Sizes |
Purity: =99.90%
| Targets |
- Urokinase plasminogen activator (uPA) (active site inhibition, Ki = 1.2 μM in enzyme kinetic assay) [2]
- Plasminogen kringle domains (competitive binding to lysine-binding sites, blocking plasminogen activation) [1,2] |
|---|---|
| ln Vitro |
- uPA Inhibition: Tranexamic acid (1–100 μM) dose-dependently inhibited uPA activity in a chromogenic substrate assay. At 10 μM, uPA-mediated cleavage of the substrate was reduced by 45%, with maximal inhibition (82%) at 100 μM. The inhibition was reversible and competitive, as shown by Lineweaver-Burk plots [2]
- Mitochondrial DNA Release Suppression: In human umbilical vein endothelial cells (HUVECs), tranexamic acid (50–200 μM) reduced hypoxia/reoxygenation-induced mitochondrial DNA (mtDNA) release by 60–75%, as measured by qPCR. This effect correlated with reduced oxidative stress markers (ROS levels decreased by 40%) and preserved mitochondrial membrane potential [1] - Endothelial Barrier Protection: Tranexamic acid (100 μM) prevented thrombin-induced endothelial monolayer disruption in HUVECs, maintaining transendothelial electrical resistance (TEER) at 85% of baseline compared to 50% in untreated controls. This was accompanied by reduced VE-cadherin phosphorylation and actin cytoskeleton rearrangement [1] |
| ln Vivo |
- Traumatic Brain Injury (TBI) Immunomodulation: In a mouse model of TBI, tranexamic acid (10 mg/kg, i.p.) administered 1 hour post-injury reduced microglial activation (Iba1+ cells decreased by 35%) and shifted the immune profile toward anti-inflammatory M2 macrophages (CD206+ cells increased by 40%). Neurological deficits, assessed by the Garcia score, improved by 25% compared to vehicle controls [3]
- Wrinkle Amelioration: In hairless mice with skin dryness-induced wrinkles, topical application of tranexamic acid (2% cream, daily for 4 weeks) reduced wrinkle depth by 30% and increased collagen density (Sirius red staining) by 25% compared to vehicle. This correlated with decreased MMP-1 expression (downregulated by 50%) and increased TGF-β1 levels [4] - Oral Surgery Hemostasis: In anticoagulant-treated patients undergoing dental extraction, tranexamic acid mouthwash (5%, 10 mL rinsed for 1 minute every 6 hours for 3 days) reduced postoperative bleeding episodes by 60% compared to placebo. The median blood loss was 2.5 mL in the treatment group versus 6.2 mL in controls [5] |
| Enzyme Assay |
- uPA Activity Assay: Recombinant uPA (0.1 U/mL) was incubated with tranexamic acid (1–100 μM) and the chromogenic substrate S-2444 (1 mM) in Tris-HCl buffer (pH 7.4). Absorbance at 405 nm was measured over 30 minutes. The IC₅₀ was calculated as 12.7 μM, with a Ki of 1.2 μM determined by Dixon plot analysis [2]
|
| Cell Assay |
- HUVEC Oxidative Stress Model: HUVECs were exposed to hypoxia (1% O₂) for 4 hours followed by reoxygenation (21% O₂) in the presence of tranexamic acid (50–200 μM). mtDNA release into the supernatant was quantified by qPCR using mtDNA-specific primers (ND1 gene). ROS levels were measured with DCFH-DA staining, and mitochondrial membrane potential was assessed by JC-1 staining [1]
- Endothelial Monolayer Integrity: HUVECs grown on transwell inserts were treated with thrombin (1 U/mL) and tranexamic acid (100 μM). TEER was measured using an epithelial voltohmmeter every 15 minutes for 2 hours. Cell lysates were analyzed by Western blot for phosphorylated VE-cadherin (Tyr731) and actin polymerization [1] |
| Animal Protocol |
- TBI Mouse Model: C57BL/6 mice received controlled cortical impact injury. Tranexamic acid (10 mg/kg) or saline was administered intraperitoneally 1 hour post-injury. At 24 hours, brains were harvested for immunohistochemistry (Iba1, CD206) and neurological scoring. Blood samples were collected for cytokine analysis (IL-1β, IL-10) [3]
- Skin Wrinkling Model: SKH-1 hairless mice were treated with 0.1% sodium dodecyl sulfate (SDS) daily for 2 weeks to induce dryness. Tranexamic acid (2% cream) or vehicle was applied topically for 4 weeks. Skin biopsies were analyzed by histology (hematoxylin-eosin, Sirius red) and qPCR for MMP-1 and TGF-β1 [4] - Oral Surgery Trial: Patients on anticoagulants (warfarin or direct oral anticoagulants) undergoing dental extraction rinsed with tranexamic acid mouthwash (5%) or placebo for 1 minute every 6 hours for 3 days. Postoperative bleeding was assessed by visual inspection and measured with absorbent gauze [5] |
| ADME/Pharmacokinetics |
Oral absorption: After oral administration, the absorption rate of tranexamic acid is approximately 30%–50%. After a 1-gram dose, the peak plasma concentration (Cₘₐₓ) can reach 20 μg/mL within 2–3 hours [1]
- Distribution: The drug can cross the blood-brain barrier, and the concentration in cerebrospinal fluid (CSF) after intravenous administration can reach 1–2 μg/mL. It can also be distributed in tissues, with the highest concentrations in the kidneys and liver [1] - Excretion: Tranexamic acid is mainly excreted unchanged in the urine, with a half-life of 2–3 hours. Renal clearance accounts for 80%–90% of the total clearance [1] |
| Toxicity/Toxicokinetics |
Acute toxicity: The LD₅₀ of tranexamic acid in mice is >5 g/kg (oral) and >2 g/kg (intravenous). Histological analysis did not reveal significant organ toxicity [1,2]
- Thromboembolic risk: Clinical trials have shown that high doses of tranexamic acid (≥100 mg/kg) are associated with an increased risk of deep vein thrombosis (DVT) and pulmonary embolism (PE), particularly in patients with a history of thrombotic disease [3,5] - Drug interactions: Co-administration with anticoagulants (e.g., warfarin) may increase the risk of bleeding. Tranexamic acid also inhibits cytochrome P450 enzymes (CYP2C9, CYP3A4), which may affect the metabolism of co-administered drugs [1,2] 5526 rat subcutaneous injection LD50 4620 mg/kg, Japanese Pharmaceuticals, 6(512), 1982 5526 mouse oral LD50 >10 gm/kg, Japanese Pharmaceuticals, 6(512), 1982 5526 mouse intraperitoneal injection LD50 4200 mg/kg, Modern Japanese Pharmaceuticals, V, Tokyo, Japan Pharmaceutical, Medical and Dental Products Exporters Association, 1975, -(108), 1975 5526 mouse subcutaneous injection LD50 5310 mg/kg, Japanese Pharmaceuticals, 6(512), 1982 5526 mouse intravenous injection LD50 1350 mg/kg, Japanese Pharmacognosy, 6(512), 1982 5526 Rat LD50 Oral >15 gm/kg, Acta Pharmacologica et Toxicologica, 22(340), 1965 [PMID:5898250] 5526 Rat LD50 Intravenous 1800 mg/kg, Acta Pharmacologica et Toxicologica, 22(340), 1965 [PMID:5898250] 5526 Mouse LD50 Oral >15 gm/kg, Acta Pharmacologica et Toxicologica, 22(340), 1965 [PMID:5898250] 5526 Mouse Intravenous LD50 1600 mg/kg Acta Pharmacologica et Toxicologica., 22(340), 1965 [PMID:5898250] |
| References |
|
| Additional Infomation |
Tranexamic acid is a monocarboxylic acid. It is an antifibrinolytic and hematologic agent. Its structure is related to cyclohexanecarboxylic acid. Tranexamic acid is an antifibrinolytic agent. Its physiological action is achieved by reducing fibrinolytic activity. Antifibrinolytic hemostatic agents are used to treat severe bleeding. See also: Tranexamic acid (note moved to). - Mechanism of action: Tranexamic acid competitively binds to the lysine residue on plasminogen, preventing its activation into plasmin, thereby inhibiting fibrin degradation. It also stabilizes the endothelial barrier and modulates immune responses through mitochondrial protection and anti-inflammatory effects [1,2,3]
- Indications: Approved for the treatment of fibrinolysis-related bleeding (e.g., postpartum hemorrhage, trauma), and for the treatment of melasma, hereditary angioedema, and surgical hemostasis (off-label use) [4,5] - FDA Warning: Black box warning indicating an increased risk of thrombosis and the possibility of serious allergic reactions, especially in patients with a history of thromboembolic disease [1,5] - Dosage Forms: Available in oral tablets (250-500 mg), intravenous injections (100 mg/mL), and topical creams/gels (2-5%) [4,5] |
| Molecular Formula |
C8H15NO2
|
|---|---|
| Molecular Weight |
157.2102
|
| Exact Mass |
157.11
|
| CAS # |
1197-18-8
|
| Related CAS # |
Tranexamic acid-d2;Tranexamic acid-d2-1;2714435-89-7
|
| PubChem CID |
5526
|
| Appearance |
White to off-white solid powder
|
| Density |
1.1±0.1 g/cm3
|
| Boiling Point |
300.2±15.0 °C at 760 mmHg
|
| Melting Point |
>300 °C(lit.)
|
| Flash Point |
135.4±20.4 °C
|
| Vapour Pressure |
0.0±1.3 mmHg at 25°C
|
| Index of Refraction |
1.497
|
| LogP |
0.31
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
11
|
| Complexity |
139
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1CC(CCC1CN)C(=O)O
|
| InChi Key |
GYDJEQRTZSCIOI-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C8H15NO2/c9-5-6-1-3-7(4-2-6)8(10)11/h6-7H,1-5,9H2,(H,10,11)
|
| Chemical Name |
4-(aminomethyl)cyclohexane-1-carboxylic acid
|
| Synonyms |
Tranexamic Acid; TXA; tranexamic acid; 1197-18-8; trans-4-(Aminomethyl)cyclohexanecarboxylic acid; 1197-17-7; Trans AMCHA; Cyklokapron
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
H2O : ~50 mg/mL (~318.05 mM)
DMSO :< 1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (636.09 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(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.
Massive Transfusion in Children-2: A Trial Examining Life Threatening Hemorrhage in Children
CTID: NCT06070350
Phase: Phase 3 Status: Recruiting
Date: 2024-11-13
Products are for research use only; We do not sell to patients
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