| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
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| Targets |
Prostaglandin Receptor[1]
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|---|---|
| ln Vivo |
In a 6-hour model of myocardial ischemia (MI) with reperfusion in anesthetized cats, tappestene (100 ng/kg/min) is administered intravenously starting 30 minutes postocclusion of the left anterior descending coronary artery and followed by reperfusion 1 hour later. Taprostene has a profile of activity that includes preventing aggregation in cat platelets15 at concentrations that are much lower than that required to produce significant vasodilator activity in rabbit aortic rings. Taprostene infusion results in significantly lower plasma creatine phosphokinase activities for the MI + Taprostene group compared with the MI + vehicle group. Taprostene is effective not just in circulatory shock but also in acute inflammatory states and in rat models of myocardial hypoxia and chronic ischemia. It also has cytoprotective and antiaggregatory properties. Initially, a range of Taprostene infusion rates, ranging from 50 to 200 ng/kg/min, were employed to achieve an infusion rate that exhibited minimal hemodynamic (i.e., vasodilator) effects while maintaining cardioprotective properties. After ischemia and reperfusion, taprostene therapy prevents neutrophils from sticking to the myocardial endothelium in both compromised and necrotic cardiac tissue[1].
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| Animal Protocol |
Animal/Disease Models: Adult male cats (2.5-3.5 kg)[1]
Doses: 100 ng/kg Route of Administration: Infused intravenously (iv) at a rate of 100 ng/kg/min until the end of the experiment (ie, for 5.5 hrs (hours)). Experimental Results: In six cat aortic rings, 1-100 ng/mL failed to exert any vasorelaxant effect. Relaxed the vascular rings 34% at 300 ng/mL. The EC50 was 520 ng/mL, a value 26 times that of its antiplatelet aggregatory effect in cat platelet -rich plasma. |
| References |
[1]. G Johnson 3rd, et al. Endothelium and myocardial protecting actions of Taprostene, a stable prostacyclin analogue, after acute myocardial ischemia and reperfusion in cats. Circ Res. 1990 May;66(5):1362-70.
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| Molecular Formula |
C24H30O5
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|---|---|
| Molecular Weight |
398.49
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| CAS # |
108945-35-3
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| SMILES |
C1CCC(CC1)[C@@H](/C=C/[C@@H]2[C@H]3C/C(=C/C4=CC(=CC=C4)C(=O)O)/O[C@H]3C[C@H]2O)O
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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 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.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5095 mL | 12.5474 mL | 25.0947 mL | |
| 5 mM | 0.5019 mL | 2.5095 mL | 5.0189 mL | |
| 10 mM | 0.2509 mL | 1.2547 mL | 2.5095 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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