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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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Other Sizes |
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Siguazodan, also known as SKF 94836, is an orally active phosphodiesterase III (PDE-III) inhibitor. It's IC50 & Target is 117 nM.
ln Vitro |
Siguazodan specifically prevents PDE, the main cyclic AMP found in human platelet supernatants, from being hydrolyzed. PDE-III, also known as cyclic GMP-inhibited PDE, is the name of the inhibited enzyme. Siguazodan was found to be more efficient than adenosine 5'-diphosphate (ADP) and collagen in inhibiting U46619-induced aggregation in platelet-rich plasma (PRP). The effectiveness of watermelon zodan is not affected by treating PRP with aspirin. Siguazodan lowers cytoplasmic free calcium and raises cyclic AMP levels in platelets that have been cleaned. Siguazodan's reduced efficacy in suppressing the ADP response may be explained by the fact that ADP lessens its capacity to increase cyclic AMP. Ciguazodan is an inotrope and a vasodilator that has antiplatelet actions within the same dosage range [2].
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ln Vivo |
Siguazodan is an oral medication that acts for a long time in conscious dogs and is a strong and selective phosphodiesterase III inhibitor with inotropic and vasodilatory effects in a range of experimental animals [2].
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References |
[1]. Tang KM, et al. Photoaffinity labelling of cyclic GMP-inhibited phosphodiesterase (PDE III) in human and rat platelets and rat tissues: effects of phosphodiesterase inhibitors. Eur J Pharmacol. 1994 Jun 15;268(1):105-14.
[2]. Murray KJ, et al. The effects of siguazodan, a selective phosphodiesterase inhibitor, on human platelet function. Br J Pharmacol. 1990 Mar;99(3):612-6. [3]. Freitag A, et al. Phosphodiesterase inhibitors suppress alpha2-adrenoceptor-mediated 5-hydroxytryptamine release from tracheae of newborn rabbits. Eur J Pharmacol. 1998 Jul 31;354(1):67-71. |
Molecular Formula |
C14H16N6OM.W.
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Molecular Weight |
284.31644
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Exact Mass |
284.14
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Elemental Analysis |
C, 59.14; H, 5.67; N, 29.56; O, 5.63
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CAS # |
115344-47-3
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Appearance |
Solid powder
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SMILES |
C(N/C(/NC)=N\C1C=CC(C2C(C)CC(=O)NN=2)=CC=1)#N
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Synonyms |
Siguazodan; SK&F 94836; SKF 94836; SKF-94836; SKF94836;
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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 : ~12.5 mg/mL (~43.96 mM)
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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 | 3.5172 mL | 17.5858 mL | 35.1716 mL | |
5 mM | 0.7034 mL | 3.5172 mL | 7.0343 mL | |
10 mM | 0.3517 mL | 1.7586 mL | 3.5172 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.