| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
The molecular target is the platelet P2Y12 receptor, where the active thiol metabolite of prasugrel irreversibly binds and antagonizes ADP-mediated signaling; this blocks Gi-mediated inhibition of adenylyl cyclase and P2Y12-dependent activation of phosphoinositide 3-kinase, thereby inhibiting platelet aggregation and thrombus formation.
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|---|---|
| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as quantitative tracers while the drugs were being developed. Because deuteration may have an effect on a drug's pharmacokinetics and metabolic properties, it is a cause for concern [1].
In vitro, prasugrel-d5 is metabolized to its active thiol metabolite, which irreversibly inhibits P2Y12-mediated platelet aggregation in platelet-rich plasma and whole blood; the deuterated form retains antiplatelet activity while enabling LC-MS/MS quantification of prasugrel and its metabolites in plasma. |
| ln Vivo |
In vivo, oral prasugrel-d5 reduces ADP-induced platelet aggregation and thrombus formation in rodent and canine thrombosis models, with greater potency and faster onset than clopidogrel; the labeled form is used to quantify plasma concentrations of the active metabolite and to relate P2Y12 occupancy to antiplatelet efficacy.
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| Enzyme Assay |
Noncellular P2Y12 receptor binding assays incubate platelet membranes or recombinant P2Y12 receptor with a radiolabeled ADP analog or fluorescent antagonist and increasing concentrations of the prasugrel active metabolite; binding is quantified by filtration or fluorescence polarization, and irreversible occupancy is assessed by washout experiments.
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| Cell Assay |
Cellular assays use washed platelets or P2Y12-expressing cells treated with the prasugrel active metabolite; platelet aggregation is measured by light transmission aggregometry, P2Y12-mediated cAMP inhibition by enzyme immunoassay, and receptor internalization by flow cytometry.
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| Animal Protocol |
Animal protocols administer prasugrel-d5 orally to rats or dogs at doses of 1–10 mg/kg; ADP-induced platelet aggregation, bleeding time, and thrombus formation in arterial injury models are measured, and plasma concentrations of the active metabolite are quantified by LC-MS/MS to relate P2Y12 occupancy to antiplatelet efficacy.
|
| References |
| Molecular Formula |
C20H20FNO3S
|
|---|---|
| Molecular Weight |
373.441107749939
|
| Exact Mass |
378.146
|
| CAS # |
1127252-92-9
|
| Related CAS # |
Prasugrel;150322-43-3;Prasugrel hydrochloride;389574-19-0;Prasugrel (Maleic acid);389574-20-3
|
| PubChem CID |
25222363
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
493.5±45.0 °C at 760 mmHg
|
| Flash Point |
252.3±28.7 °C
|
| Vapour Pressure |
0.0±1.3 mmHg at 25°C
|
| Index of Refraction |
1.619
|
| LogP |
3.17
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
26
|
| Complexity |
555
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C(C1C=CC=CC=1F)(N1CCC2SC(OC(=O)C)=CC=2C1)C(C1([H])C([H])([H])C1([H])[H])=O
|
| InChi Key |
DTGLZDAWLRGWQN-GEXSZOTCSA-N
|
| InChi Code |
InChI=1S/C20H20FNO3S/c1-12(23)25-18-10-14-11-22(9-8-17(14)26-18)19(20(24)13-6-7-13)15-4-2-3-5-16(15)21/h2-5,10,13,19H,6-9,11H2,1H3/i6D2,7D2,13D
|
| Chemical Name |
[5-[1-(2-fluorophenyl)-2-oxo-2-(1,2,2,3,3-pentadeuteriocyclopropyl)ethyl]-6,7-dihydro-4H-thieno[3,2-c]pyridin-2-yl] acetate
|
| 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)
|
| 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 | 2.6778 mL | 13.3890 mL | 26.7781 mL | |
| 5 mM | 0.5356 mL | 2.6778 mL | 5.3556 mL | |
| 10 mM | 0.2678 mL | 1.3389 mL | 2.6778 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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