Size | Price | |
---|---|---|
100mg | ||
250mg | ||
500mg |
ln Vitro |
The binding of haTRAP (high-affinity thrombin receptor-activating peptide) to PAR-1 on human platelet membranes is inhibited by Atopaxar Hydrobromide (0.0001-10 μM; 1h) in a concentration-dependent manner, with an IC50 of 0.019 μM [2]. Atopaxar Hydrobromide has no effect on platelet aggregation induced by collagen or ADP, but it has a strong inhibitory effect on human platelet aggregation induced by thrombin and TRAP (IC50 of 0.064 and 0.031 μM, respectively) [2]. In guinea pigs, Atopaxar Hydrobromide demonstrated a strong and targeted suppression of thrombin- and TRAP-induced platelet aggregation, with IC50 values of 0.13 and 0.097 μM, correspondingly [2].
|
---|---|
ln Vivo |
In a guinea pig model of photochemically induced thrombosis (PIT), atopaxar (30-100 mg/kg; po) hydrobromide causes a dose-dependent extension of femoral artery occlusion time [2]. Even at the highest tested dose of 1000 mg/kg, atopaxa hydrobromide did not cause the guinea pigs' bleeding time to be prolonged [2].
|
Animal Protocol |
Animal/Disease Models: guinea pig, PIT model [2]
Doses: Oral administration Route of Administration: 10 mg/kg, 30 mg/kg, 100 mg/kg Experimental Results: At 30 mg/kg, the occlusion time was prolonged by 1.8 times and 2.4 times compared with Compared with the standard, they are 100 mg/kg and 100 mg/kg respectively. |
References |
[1]. Chris Dockendorff, et al. Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor. ACS Med Chem Lett. 2012 Mar 8; 3(3): 232–237.
[2]. Motoji Kogushi, et al. The novel and orally active thrombin receptor antagonist E5555 (Atopaxar) inhibits arterial thrombosis without affecting bleeding time in guinea pigs. Eur J Pharmacol. 2011 Apr 25;657(1-3):131-7. |
Molecular Formula |
C29H39BRFN3O5
|
---|---|
Molecular Weight |
608.5395
|
CAS # |
474550-69-1
|
Related CAS # |
Atopaxar;751475-53-3
|
SMILES |
Br[H].FC1C(=C(C([H])=C2C=1/C(=N/[H])/N(C2([H])[H])C([H])([H])C(C1C([H])=C(C(=C(C=1[H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])OC([H])([H])[H])N1C([H])([H])C([H])([H])OC([H])([H])C1([H])[H])=O)OC([H])([H])C([H])([H])[H])OC([H])([H])C([H])([H])[H]
|
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 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 | 1.6433 mL | 8.2164 mL | 16.4328 mL | |
5 mM | 0.3287 mL | 1.6433 mL | 3.2866 mL | |
10 mM | 0.1643 mL | 0.8216 mL | 1.6433 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.