- 商品介绍
- 规格参数
- 包装参数
Biochem/physiol Actions
Rupatadine (UR-12592) is an orally active, dual histamine H1 and platelet-activating factor (PAF) receptor antagonist (Ki(app) = 100/550 nM against pyrilamine/WEB2086 binding to guinea pig cerebellum/rabbit platelet membranes) that inhibits histamine-induced guinea pig ileum contraction (pA2 = 9.29) and PAF-induced platelet aggregation (IC50 = 0.68 μM/human PRP). Rupatadine blocks histamine-/PAF-induced hypotension (ID50 = 1.4/0.44 mg/kg i.v. rats) and bronchoconstriction (ID50 = 113/9.6 μg/kg i.v. guinea pigs), as well as prevents mortality caused by PAF (ID50 = 0.31 mg/kg i.v. or 3.0 mg/kg p.o. mice) and endotoxin (mice/rats ID50 = 1.6/0.66 mg/kg i.v.) in vivo.
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | 2-8°C |
| SMILES string | Clc1cc2c(cc1)C(=C4CCN(CC4)Cc5cncc(c5)C)c3ncccc3CC2.OC(=O)\C=C\C(=O)O |
| InChI | 1S/C26H26ClN3.C4H4O4/c1-18-13-19(16-28-15-18)17-30-11-8-20(9-12-30)25-24-7-6-23(27)14-22(24)5-4-21-3-2-10-29-26(21)25;5-3(6)1-2-4(7)8/h2-3,6-7,10,13-16H,4-5,8-9,11-12,17H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1+ |
| InChI key | JYBLCDXVHQWMSU-WLHGVMLRSA-N |
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¥ 2019.57
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¥ 9207.92
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¥ 8293.41
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¥ 3275.78
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¥ 4968.78
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¥ 3812.28
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¥ 14407.09
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¥ 10277.12
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