| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Ticagrelor metabolite M5 targets the P2Y12 receptor, a platelet receptor for ADP. By antagonizing this receptor, it inhibits ADP-induced platelet aggregation, thereby reducing the risk of thrombotic events. Compared to clopidogrel, Ticagrelor has faster and more consistent inhibition of the ADP receptor. M5 contributes to the overall antiplatelet effect of Ticagrelor.
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| ln Vitro |
Ticagrelor metabolite M5 is a P2Y12 receptor antagonist. It is a metabolite of Ticagrelor, which is the first reversible oral antagonist of the P2Y12 receptor. Compared to clopidogrel, Ticagrelor and its metabolite M5 have faster and more consistent inhibition on ADP-receptors. The compound retains pharmacological activity as an antiplatelet agent.
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| ln Vivo |
Ticagrelor metabolite M5 is a major circulating metabolite of Ticagrelor and contributes to its antiplatelet effects in vivo. Ticagrelor is used for the treatment of acute coronary syndrome (ACS). The faster and more consistent inhibition of the ADP receptor by Ticagrelor and its metabolite M5 provides clinical benefits compared to other antiplatelet agents.
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| Enzyme Assay |
In vitro receptor binding assays for Ticagrelor metabolite M5 measure its affinity for the P2Y12 receptor. The receptor is incubated with a radiolabeled ligand and varying concentrations of the compound, and displacement is measured to determine binding affinity (Ki). Functional assays assess its ability to inhibit ADP-induced platelet aggregation using platelet-rich plasma.
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| Cell Assay |
In vitro cellular assays for Ticagrelor metabolite M5 involve treating platelets with the compound and measuring ADP-induced aggregation using aggregometry. Its effects on platelet activation markers, such as P-selectin expression, can be assessed by flow cytometry. Its binding to the P2Y12 receptor can be studied in cells expressing the receptor.
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| Animal Protocol |
In vivo animal models for Ticagrelor metabolite M5 are typically focused on its parent compound, Ticagrelor. These models include thrombosis models in mice or rats to evaluate the antiplatelet and antithrombotic effects of Ticagrelor and its metabolites. Pharmacokinetic studies measure the levels of M5 and other metabolites in plasma after Ticagrelor administration.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Ticagrelor metabolite M5 indicate that it is a major circulating metabolite of Ticagrelor. It is formed by O-dealkylation of Ticagrelor and has a similar half-life to the parent compound. It contributes to the overall antiplatelet effect of Ticagrelor. Its pharmacokinetics have been characterized in clinical studies.
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| Toxicity/Toxicokinetics |
Ticagrelor metabolite M5 is generally well-tolerated as part of Ticagrelor therapy. The most common side effects of Ticagrelor include bleeding, dyspnea, and gastrointestinal disturbances. The safety profile of M5 is similar to that of the parent compound. It is not used as a therapeutic agent on its own.
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| Additional Infomation |
Ticagrelor metabolite M5 is a major circulating metabolite of Ticagrelor, the first reversible oral P2Y12 receptor antagonist. It retains antiplatelet activity. Ticagrelor is used for acute coronary syndrome. Compared to clopidogrel, Ticagrelor and M5 provide faster and more consistent inhibition of the ADP receptor. M5 is also known as Ticagrelor impurity H.
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| Molecular Formula |
C14H22N6O4S
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|---|---|
| Molecular Weight |
370.43
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| Exact Mass |
370.142
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| CAS # |
1251765-07-7
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| PubChem CID |
78358176
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.8±0.1 g/cm3
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| Boiling Point |
711.4±70.0 °C at 760 mmHg
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| Flash Point |
384.1±35.7 °C
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| Vapour Pressure |
0.0±2.4 mmHg at 25°C
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| Index of Refraction |
1.787
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| LogP |
-0.73
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
25
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| Complexity |
438
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CCCSC1=NC(=C2C(=N1)N([C@@H]3C[C@@H]([C@H]([C@H]3O)O)OCCO)N=N2)N
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| InChi Key |
YTYBSYIHUFBLKV-YKDSUIRESA-N
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| InChi Code |
InChI=1S/C14H22N6O4S/c1-2-5-25-14-16-12(15)9-13(17-14)20(19-18-9)7-6-8(24-4-3-21)11(23)10(7)22/h7-8,10-11,21-23H,2-6H2,1H3,(H2,15,16,17)/t7-,8+,10+,11-/m1/s1
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| Chemical Name |
(1S,2S,3R,5S)-3-(7-amino-5-propylsulfanyltriazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol
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| Synonyms |
AR-C133913XX, T437700, Ticagrelor metabolite M5,AZD6140AR-C126532XX Brilinta Brilique Possia
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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) |
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 | 2.6996 mL | 13.4978 mL | 26.9957 mL | |
| 5 mM | 0.5399 mL | 2.6996 mL | 5.3991 mL | |
| 10 mM | 0.2700 mL | 1.3498 mL | 2.6996 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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