Structure
Sarpogrelate hydrochloride, Inhibitor
Sarpogrelate hydrochloride
Purity
98.00%
Synonyms
Sarpogrelate hydrochloride; MCI-9042; inhibitor
Purity/Purification
98.00%
Form/Format
Powder
Formula
C24H32ClNO6
CAS
135159-51-2
Smiles
Cl.COc1cccc(CCc2ccccc2OCC(CN(C)C)OC(=O)CCC(O)=O)c1
Receptor (IC50)
5-HT2
Solubility
DMSO: 46.6mg/mL (100mM)
(<1mg/ml refers to the product slightly soluble or insoluble)
(<1mg/ml refers to the product slightly soluble or insoluble)
Preparation and Storage
Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent
For obtaining a higher solubility, please warm the tube at 37 degree C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 degree C for several month.
For obtaining a higher solubility, please warm the tube at 37 degree C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 degree C for several month.
Structure
Structure
Related Product Information for Sarpogrelate hydrochloride, inhibitor
Sarpogrelate (MCI-9042) hydrochloride, a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD. Target: 5-HT2 Recepter Sarpogrelate is a drug which acts as an antagonist at the 5HT2A and 5-HT2B receptors. Sarpogrelate was shown to have the same affinity as ritanserin for 5-HT2A receptors, with a Ki value of 8.39nM. Sarpogrelate lacked prominent 5-HT1-like, 5-HT3, beta, H1, H2 and M3 antagonist activity and weakly blocked alpha 1-adrenoceptors (pKB = 6.30). (S)-M-1 showed weak affinity for 5-HT1-like receptors (pKB = 6.30), alpha 1-(pKB = 6.80) and beta-(pKB = 6.54) adrenoceptors, while (R)-M-1 was a weak antagonist at histamine H1 receptors (pKB = 6.49). After 12 weeks of sarpogrelate administration, FBF and LBF responses during RH showed significant increases from 13.2 +/- 1.7 to 18.1 +/- 2.2 mL/min per 100 mL tissue (P <0.01) and from 8.2 +/- 0.9 to 14.2 +/- 2.1 mL/min per 100 mL tissue (P <0.05), respectively. Sarpogrelate-induced augmentation of FBF and LBF responses to RH was maintained at 24 weeks. Long-term oral administration of sarpogrelate improves vascular function in patients with PAD.
Product Categories/Family for Sarpogrelate hydrochloride, inhibitor
References
1. Pertz, H. and S. Elz, In-vitro pharmacology of sarpogrelate and the enantiomers of its major metabolite: 5-HT2A receptor specificity, stereoselectivity and modulation of ritanserin-induced depression of 5-HT contractions in rat tail artery. J Pharm Pharma
2. Miyazaki, M., et al., Sarpogrelate hydrochloride, a selective 5-HT2A antagonist, improves vascular function in patients with peripheral arterial disease. J Cardiovasc Pharmacol, 2007. 49 (4): p. 221-7.
3. Nishio, H., A. Inoue, and Y. Nakata, Binding affinity of sarpogrelate, a new antiplatelet agent, and its metabolite for serotonin receptor subtypes. Arch Int Pharmacodyn Ther, 1996. 331 (2): p. 189-202.
2. Miyazaki, M., et al., Sarpogrelate hydrochloride, a selective 5-HT2A antagonist, improves vascular function in patients with peripheral arterial disease. J Cardiovasc Pharmacol, 2007. 49 (4): p. 221-7.
3. Nishio, H., A. Inoue, and Y. Nakata, Binding affinity of sarpogrelate, a new antiplatelet agent, and its metabolite for serotonin receptor subtypes. Arch Int Pharmacodyn Ther, 1996. 331 (2): p. 189-202.
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Product Notes
The Sarpogrelate hydrochloride (Catalog #AAA5751444) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "Sarpogrelate hydrochloride, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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