| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 500mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Sarpogrelate HCl targets serotonin (5-HT) receptors, specifically the 5-HT2A, 5-HT2B, and 5-HT2C subtypes. It acts as a selective antagonist with Kis of 3.02 nM for 5-HT2A, 269 nM for 5-HT2B, and 37.2 nM for 5-HT2C. By blocking these receptors, it inhibits 5-HT2 induced platelet aggregation, vasoconstriction, and vascular smooth muscle proliferation.
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| ln Vitro |
Compared to 5-HT1 (pKi=4.58), α1-, α2-, and β-adrenergic (pKi=3.17-6.19), and muscarinic receptors (pKi=4.39), sargredoxate is more selective for 5-HT2 (pKi=7.54). Human umbilical vein endothelial cells (HUVEC)-induced THP-1 cell adhesion is greatly reduced by sarpogrelate (10 μM) [3]. In HUVEC, sarpogrelate (10 μM) dramatically lowers PRP-induced E-selectin expression [3].
In vitro, sarpogrelate hydrochloride is a potent and selective 5-HT2 receptor antagonist. It inhibits ex vivo platelet aggregation stimulated by serotonin in combination with collagen. It also suppresses blood vessel constriction mediated by 5-HT2 in vitro. These activities confirm its antithrombotic and vasodilatory effects. |
| ln Vivo |
Sarpogrelate (5 mg/kg; daily intraperitoneal injection for 4 weeks) suppresses HFFD-induced obesity and decreases leukocyte-endothelial cell interactions in mice [3].
In vivo, sarpogrelate hydrochloride is launched in Japan as an antithrombotic agent. It is used for the treatment of peripheral vascular disease and other conditions associated with platelet aggregation and vasoconstriction. Its clinical efficacy is related to its ability to block 5-HT2 receptors and inhibit serotonin-mediated platelet aggregation and vasoconstriction. |
| Enzyme Assay |
The in vitro receptor binding assay for sarpogrelate hydrochloride typically involves radioligand displacement studies using membrane preparations from cells expressing 5-HT2A, 5-HT2B, and 5-HT2C receptors. The compound's affinity (Ki) is determined by measuring its ability to displace a specific radiolabeled ligand from these receptors. These cell-free assays provide a direct measure of the compound's binding profile.
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| Cell Assay |
In vitro cellular assays for sarpogrelate hydrochloride assess its functional antagonism at 5-HT2 receptors. Platelets or vascular smooth muscle cells are treated with sarpogrelate, and its ability to inhibit serotonin-induced aggregation or contraction is measured. These assays demonstrate the compound's functional activity in a relevant cellular context.
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| Animal Protocol |
Animal/Disease Models: Male C57BL/6 mice (7 weeks old) were fed normal chow (NC) or high-fat diet (HFFD) containing 30% fructose in drinking water [3].
Doses: 5 mg/kg. Route of Administration: every Daily intraperitoneal (ip) injection for 4 weeks Experimental Results: Prevented HFFD-induced increases in body weight, visceral fat weight, and serum monocyte chemoattractant protein-1 levels. Leukocyte-endothelial interactions and blood levels of mononuclear cell chemoattractant protein-1 (MCP-1) are diminished. In vivo animal studies for sarpogrelate hydrochloride have been conducted in animal models of thrombosis and vascular disease to evaluate its efficacy. These studies typically involve administering the compound to animals and measuring platelet aggregation, thrombus formation, or vascular responses. Its efficacy in these models supports its clinical use. |
| ADME/Pharmacokinetics |
Sarpogrelate hydrochloride is orally active and is administered as a tablet. Its pharmacokinetic properties are characterized by good absorption and a relatively short half-life. It is metabolized in the liver and excreted in urine. Its pharmacokinetic profile supports its use as an oral antithrombotic agent.
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| Toxicity/Toxicokinetics |
Sarpogrelate hydrochloride is generally well-tolerated. Common adverse effects include gastrointestinal disturbances, headache, and dizziness. It may increase the risk of bleeding. Its safety profile has been established in clinical use in Japan.
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| References |
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| Additional Infomation |
Sagrelate hydrochloride is a stilbene compound.
Sarpogrelate HCl (Anplag; MCI 9042) is a potent and selective antagonist of 5-HT2A, 5-HT2B, and 5-HT2C receptors. It is launched in Japan as an antithrombotic agent. It inhibits platelet aggregation, vasoconstriction, and vascular smooth muscle proliferation. It is available as a prescription medication in some countries. |
| Molecular Formula |
C24H32CLNO6
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|---|---|
| Molecular Weight |
465.9670
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| Exact Mass |
465.191
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| CAS # |
135159-51-2
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| Related CAS # |
Sarpogrelate;125926-17-2;Sarpogrelate-d3 hydrochloride
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| PubChem CID |
444005
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| Appearance |
White to off-white solid powder
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| Boiling Point |
585.9ºC at 760 mmHg
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| Melting Point |
145-148°C
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| Flash Point |
308.1ºC
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| Vapour Pressure |
1.43E-14mmHg at 25°C
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| LogP |
3.999
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
32
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| Complexity |
540
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
POQBIDFFYCYHOB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H31NO6.ClH/c1-25(2)16-21(31-24(28)14-13-23(26)27)17-30-22-10-5-4-8-19(22)12-11-18-7-6-9-20(15-18)29-3;/h4-10,15,21H,11-14,16-17H2,1-3H3,(H,26,27);1H
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| Chemical Name |
4-((1-(dimethylamino)-3-(2-(3-methoxyphenethyl)phenoxy)propan-2-yl)oxy)-4-oxobutanoic acid hydrochloride
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| Synonyms |
MCI-9042; MCI9042; MCI 9042; LS-187,118; LS187,118; LS 187,118; Trade name: Anplag.
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ≥ 62 mg/mL (~133.06 mM)
H2O : ~33.33 mg/mL (~71.53 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.37 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 25.0 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: ≥ 2.5 mg/mL (5.37 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 25.0 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: ≥ 2.5 mg/mL (5.37 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10 mg/mL (21.46 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1461 mL | 10.7303 mL | 21.4606 mL | |
| 5 mM | 0.4292 mL | 2.1461 mL | 4.2921 mL | |
| 10 mM | 0.2146 mL | 1.0730 mL | 2.1461 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03947489 | Completed | Drug: Sarpogrelate HCL 300mg | Healthy | Daewoong Pharmaceutical Co. LTD. | 2019-03-04 | Phase 1 |
| NCT03947528 | Unknown status | Drug: Sarpogrelate HCL 300mg | Healthy | Daewoong Pharmaceutical Co. LTD. | 2019-03-04 | Phase 1 |
| NCT01841086 | Completed | Drug: Anplag Drug: UI03SPG300CT |
Healthy | Korea United Pharm. Inc. | 2011-09 | Phase 1 |
| NCT03574285 | Completed | Drug: Anpl-one SR Tab. 300mg Drug: Sarpodipil SR Tab. 300mg |
Healthy | Daewoong Pharmaceutical Co. LTD. | 2018-05-31 | Phase 1 |
| NCT03573622 | Completed | Drug: Anpl-one SR Tab. 300mg Drug: Sarpodipil SR Tab. 300mg |
Healthy | Daewoong Pharmaceutical Co. LTD. | 2018-05-31 | Phase 1 |
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