| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
Suloctidil targets multiple pathways involved in platelet aggregation and vascular tone. It inhibits platelet aggregation by blocking the activation of platelets in response to various stimuli, including ADP, collagen, and thrombin. Suloctidil also causes vasodilation by relaxing vascular smooth muscle, possibly through calcium channel blockade or by enhancing the production of vasodilatory mediators such as prostacyclin. The compound's antiplatelet and vasodilatory effects contribute to its ability to improve blood flow.
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|---|---|
| ln Vitro |
In vitro, Suloctidil has been shown to inhibit platelet aggregation induced by ADP, collagen, and thrombin in a concentration-dependent manner. It also causes relaxation of isolated blood vessels in vitro. The compound has been shown to increase the production of prostacyclin (PGI2) by vascular endothelial cells, which contributes to its vasodilatory and antiplatelet effects. Suloctidil also inhibits the release of thromboxane A2 from platelets.
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| ln Vivo |
In vivo, Suloctidil has been shown to improve blood flow in animal models of peripheral vascular disease. It has been studied in clinical trials for the treatment of intermittent claudication, Raynaud's phenomenon, and cerebrovascular disorders. Suloctidil has been shown to increase walking distance in patients with intermittent claudication and to reduce the frequency and severity of Raynaud's attacks. However, its clinical development has been limited.
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| Enzyme Assay |
In vitro platelet aggregation assays for Suloctidil typically involve collecting platelet-rich plasma from human or animal blood. The platelets are stimulated with aggregating agents such as ADP, collagen, or thrombin, and aggregation is measured using a platelet aggregometer. Suloctidil is added at various concentrations, and its ability to inhibit aggregation is determined. The IC50 value for inhibition of aggregation is calculated from dose-response curves.
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| Cell Assay |
In vitro cell-based studies with Suloctidil typically involve cultured vascular endothelial cells or smooth muscle cells. The effect of Suloctidil on prostacyclin production is measured by ELISA. The compound's effect on intracellular calcium levels can be assessed using fluorescent calcium indicators. The relaxation of isolated blood vessels is studied in organ bath experiments.
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| Animal Protocol |
In vivo animal studies with Suloctidil have been conducted in rodent and canine models. The compound is typically administered orally or intravenously. The effect on blood flow is assessed using various techniques, including laser Doppler flowmetry and plethysmography. The antiplatelet effect is evaluated by measuring platelet aggregation in blood samples collected from treated animals. The efficacy of Suloctidil in improving walking distance is assessed in models of peripheral vascular disease.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Suloctidil have been characterized in preclinical and clinical studies. Following oral administration, it is rapidly absorbed. Suloctidil is extensively metabolized in the liver, primarily by cytochrome P450 enzymes. The elimination half-life is approximately 2-4 hours. Suloctidil is excreted in the urine primarily as metabolites. The compound is highly protein-bound.
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| Toxicity/Toxicokinetics |
Suloctidil has been evaluated in clinical trials and has shown a generally acceptable safety profile. The most common adverse effects reported are gastrointestinal, including nausea, vomiting, and diarrhea. Headache, dizziness, and flushing have also been reported. Suloctidil has been associated with rare cases of hepatotoxicity. The compound should be used with caution in patients with liver disease.
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| References | |
| Additional Infomation |
(1S,2R)-2-(octylamino)-1-[4-(propyl-2-ylthio)phenyl]-1-propanol is an alkylbenzene. It is a peripheral vasodilator that has been used to treat peripheral and cerebrovascular diseases. It is hepatotoxic and has been the cause of death. (From Martindale Pharmacopoeia, 30th edition, p. 1312) See also: sulotil (note moved here).
Suloctidil is a vasodilator and antiplatelet agent that was investigated for the treatment of peripheral vascular diseases. It is not widely approved as a drug and is not commercially available in many countries. Suloctidil continues to be an area of research for its potential therapeutic applications in vascular disorders. |
| Molecular Formula |
C20H35NOS
|
|---|---|
| Molecular Weight |
337.563
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| Exact Mass |
337.244
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| CAS # |
54767-75-8
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| PubChem CID |
657255
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| Appearance |
White to off-white solid powder
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| Density |
0.99g/cm3
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| Boiling Point |
467.3ºC at 760 mmHg
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| Melting Point |
62.5°C
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| Flash Point |
236.4ºC
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| Vapour Pressure |
1.56E-09mmHg at 25°C
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| Index of Refraction |
1.528
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| LogP |
5.95
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
12
|
| Heavy Atom Count |
23
|
| Complexity |
277
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
CCCCCCCCN[C@H](C)[C@H](C1=CC=C(C=C1)SC(C)C)O
|
| InChi Key |
BFCDFTHTSVTWOG-YLJYHZDGSA-N
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| InChi Code |
InChI=1S/C20H35NOS/c1-5-6-7-8-9-10-15-21-17(4)20(22)18-11-13-19(14-12-18)23-16(2)3/h11-14,16-17,20-22H,5-10,15H2,1-4H3/t17-,20-/m1/s1
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| Chemical Name |
(1S,2R)-2-(octylamino)-1-(4-propan-2-ylsulfanylphenyl)propan-1-ol
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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 : ≥ 30 mg/mL (~88.87 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 | 2.9624 mL | 14.8122 mL | 29.6244 mL | |
| 5 mM | 0.5925 mL | 2.9624 mL | 5.9249 mL | |
| 10 mM | 0.2962 mL | 1.4812 mL | 2.9624 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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