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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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250mg |
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500mg |
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Purity: ≥98%
Asapiprant (S555739) is a novel, potent and selective Prostaglandin D2receptor 1 (DP1) receptor antagonist (Ki = 0.44 nM) with the potential for treating allergic airway diseases. Asapiprant showed high affinity and selectivity for the DP1 receptor over other targets. After asapiprant treatment, a significant suppression of antigen-induced nasal resistance, nasal secretion, and cell infiltration in nasal mucosa was observed. Further, treatment with asapiprant suppressed antigen-induced asthmatic responses, airway hyper-responsiveness, and cell infiltration and mucin production in lung. These results show that asapiprant is a potent and selective DP1 receptor antagonist, and exerts suppressive effects in the animal models of allergic diseases. Thus, asapiprant has potential as a novel therapy for allergic airway diseases.
ln Vivo |
Oral treatment of 1 mg/kg and 3 mg/kg of asapilan to sheep significantly (P<0.01) decreased the increase in nasal resistance by 82% and 92%, respectively. Oral injection of 5 mg/kg Asapiprant to sheep decreased prostaglandin (PG) D2 (PGD)2-induced nasal resistance by 86%. Asapiprant (3, 10 and 30 mg/kg) suppressed immediate airway responses (IAR) by 52%, 57% and 96% and late airway responses (LAR) when taken orally 1 hour before antigen challenge to pigs ) are 67%, 50% and 79% respectively. Asapiprant (5 mg/kg) was taken orally for 4 days. Asapiprant significantly (P<0.01) decreased sheep antigen-induced nasal resistance by 73%. Treatment of pigs with 3 and 30 mg/kg Asapiprant significantly (P<0.01) decreased nasal secretions by 53% and 72%, respectively. Treatment of rats with 10 mg/kg Asapiprant significantly reduced airway hyperresponsiveness (AHR), inflammatory cell infiltration, and mucus formation in bronchoalveolar lavage fluid (BALF) despite treatment with 0.1 mg/kg Asapiprant. (P<0.05) had no significant effect on any response [1].
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References |
[1]. Takahashi G, et al. Effect of the potent and selective DP1 receptor antagonist, asapiprant (S-555739), in animal models of allergic rhinitis and allergic asthma. Eur J Pharmacol. 2015 Oct 15;765:15-23
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Molecular Formula |
C24H27N3O7S
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Molecular Weight |
501.5521
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CAS # |
932372-01-5
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Related CAS # |
932372-01-5
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
S(C1C([H])=C([H])C(=C([H])C=1[H])OC([H])(C([H])([H])[H])C([H])([H])[H])(N1C([H])([H])C([H])([H])N(C2C([H])=C([H])C(C3=NC([H])=C([H])O3)=C(C=2[H])OC([H])([H])C(=O)O[H])C([H])([H])C1([H])[H])(=O)=O
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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 : ~11.11 mg/mL (~22.15 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.11 mg/mL (2.21 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 11.1 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.11 mg/mL (2.21 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 11.1 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.11 mg/mL (2.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.9938 mL | 9.9691 mL | 19.9382 mL | |
5 mM | 0.3988 mL | 1.9938 mL | 3.9876 mL | |
10 mM | 0.1994 mL | 0.9969 mL | 1.9938 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.