| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Target: Integrin alpha2beta1 (also known as VLA-2, GPIa/IIa, CD49b/CD29). TC-I 15 is an allosteric inhibitor that binds to the collagen-binding site on the alpha2I domain, preventing collagen from binding to the integrin alpha2beta1. This inhibits platelet adhesion to collagen under flow conditions, reducing thrombus formation without affecting platelet aggregation induced by other agonists (e.g., ADP, thrombin).
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| ln Vitro |
In vitro, TC-I 15 inhibits human platelet adhesion to type I collagen under static conditions with an IC50 of 12 nM, and under flow conditions with an IC50 of 715 nM. It inhibits binding to GFOGER peptide (collagen-mimetic peptide) with IC50 of 26.8 uM and to GLOGEN peptide with IC50 of 0.4 uM. It displays selectivity for alpha2beta1 over alphavbeta3, alpha5beta1, alpha6beta1, and alphaIIbbeta3 at concentrations exceeding 1000 nM.
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| ln Vivo |
In vivo, TC-I 15 inhibits platelet adhesion to collagen and thrombus deposition in animal models of thrombosis. It reduces occlusive thrombus formation in a ferric chloride-induced carotid artery injury model in mice or rats. It also has potential applications in oncology, as integrin alpha2beta1 is involved in cancer cell migration and metastasis (e.g., breast cancer, melanoma). Detailed animal efficacy data have been published.
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| Enzyme Assay |
For cell-free integrin alpha2beta1 binding assays: recombinant integrin alpha2I domain protein (100-200 ng) is immobilized on a microtiter plate. Varying concentrations of TC-I 15 (0-100 uM) are incubated with the immobilized integrin, then biotinylated collagen or collagen-mimetic peptides (GFOGER, GLOGEN) are added. After washing, bound peptide is detected with streptavidin-HRP and substrate. IC50 values (26.8 uM for GFOGER, 0.4 uM for GLOGEN) are calculated. For collagen binding assays: purified integrin alpha2beta1 is used in a competition ELISA format.
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| Cell Assay |
For cell-based assays: human platelets are isolated from whole blood by centrifugation and resuspended in Tyrode's buffer. Platelet adhesion assays: 96-well plates are coated with type I collagen (10 ug/mL). Platelets are pre-incubated with TC-I 15 (0-100 uM) for 10 min, then added to the coated wells and allowed to adhere for 30-60 min. After washing, adherent platelets are quantified by measuring endogenous acid phosphatase activity or by crystal violet staining. For flow adhesion: platelets are perfused over collagen-coated microslides at defined shear rates (e.g., 300-1500 s-¹) in the presence of TC-I 15, and adhesion is visualized by microscopy.
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| Animal Protocol |
For in vivo animal studies: in the ferric chloride-induced carotid artery thrombosis model, male mice (8-12 weeks old) are anesthetized, and the carotid artery is exposed. A filter paper soaked in 10-20% FeCl3 is applied to the artery for 2-3 min. TC-I 15 is administered intravenously (IV) or intraperitoneally (IP) at doses of 1-10 mg/kg, 30 min before FeCl3 application. Blood flow is monitored using a Doppler flow probe, and time to occlusive thrombus formation is recorded. At study end, carotid arteries are harvested for histology and thrombus size analysis. For tail bleeding time, a tail bleeding assay is performed to assess hemostatic function.
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| ADME/Pharmacokinetics |
PK properties of TC-I 15: For a small molecule integrin inhibitor (MW 520.62, ClogP ∼2.5), predicted PK in rodents after IV administration: plasma half-life 2-4 h, moderate volume of distribution, clearance primarily via hepatic metabolism. Oral bioavailability is likely low due to high molecular weight. The compound is soluble in DMSO and 1.1 eq. NaOH. No formal PK studies have been published.
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| Toxicity/Toxicokinetics |
No toxicity data have been reported for TC-I 15. Based on its mechanism (inhibition of alpha2beta1 integrin), potential toxicities include increased bleeding risk (prolonged bleeding time), impaired wound healing, and altered immune function. No acute toxicity or LD50 studies have been published. The compound is for research use only and not for human consumption.
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| References | |
| Additional Infomation |
TC-I 15 is a research compound not yet approved for clinical use. It is a valuable chemical tool for studying integrin alpha2beta1 biology, including its role in platelet adhesion, thrombosis, hemostasis, and cancer metastasis. It has potential applications in developing antithrombotic agents (for preventing arterial thrombosis) without increasing bleeding risk (unlike GP IIb/IIIa inhibitors), and in anticancer therapies targeting tumor cell adhesion and migration. It is also used as a reference standard for integrin inhibitor research.
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| Molecular Formula |
C23H28N4O6S2
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|---|---|
| Molecular Weight |
520.621623039246
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| Exact Mass |
520.145
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| CAS # |
916734-43-5
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| PubChem CID |
90488948
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| Appearance |
White to off-white solid powder
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| Density |
1.364±0.06 g/cm3 (20 °C, 760 mmHg)
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| LogP |
3.789
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
35
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| Complexity |
864
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC1([C@H](N(CS1)S(=O)(=O)C2=CC=CC=C2)C(=O)N[C@@H](CNC(=O)NCC3=CC=CC=C3)C(=O)O)C
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| InChi Key |
XKLHCUGVLCGKKX-RBUKOAKNSA-N
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| InChi Code |
InChI=1S/C23H28N4O6S2/c1-23(2)19(27(15-34-23)35(32,33)17-11-7-4-8-12-17)20(28)26-18(21(29)30)14-25-22(31)24-13-16-9-5-3-6-10-16/h3-12,18-19H,13-15H2,1-2H3,(H,26,28)(H,29,30)(H2,24,25,31)/t18-,19+/m0/s1
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| Chemical Name |
(2S)-2-[[(4R)-3-(benzenesulfonyl)-5,5-dimethyl-1,3-thiazolidine-4-carbonyl]amino]-3-(benzylcarbamoylamino)propanoic acid
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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 (~480.20 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 | 1.9208 mL | 9.6039 mL | 19.2079 mL | |
| 5 mM | 0.3842 mL | 1.9208 mL | 3.8416 mL | |
| 10 mM | 0.1921 mL | 0.9604 mL | 1.9208 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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