Sarpogrelate (hydrochloride)
CAS No. : 135159-51-2
(Synonyms: MCI-9042)
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| Cat. No. : | HY-10564 |
| M.Wt: | 465.97 |
| Formula: | C24H32ClNO6 |
| Purity: | >98 % |
| Solubility: | DMSO : ≥ 62 mg/mL;H2O : 33.33 mg/mL (ultrasonic) |
Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis[1][2][3].
In Vitro: Sarpogrelate is selective for 5-HT2 (pKi=7.54) over 5-HT1 (pKi=4.58), α1-, α2-, and β-adrenergic (pKi=3.17-6.19), and muscarinic receptors (pKi=4.39)[2].
Sarpogrelate (10 μM) significantly reduces the number of platelet-rich plasma (PRP)-induced THP-1 cell that adheres to human umbilical vein endothelial cells (HUVECs)[3].
Sarpogrelate (10 μM) significantly reduces the expression of PRP-induced E-selectin in HUVECs[3].
In Vivo: Sarpogrelate (5 mg/kg; i.p. daily for 4 weeks) inhibits HFFD-induced obesity and decreases leukocyte-endothelial interactions in mice[3].
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