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化學性質:
規格 | 5mg 25mg 100mg |
CAS | 289905-88-0 |
別名 |
|
化學名 | 1-[(2-chlorophenyl)-diphenylmethyl]pyrazole |
分子式 | C22H17ClN2 |
分子量 | 344.84 |
溶解度 | ≥ 17.25mg/mL in DMSO |
儲存條件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述:
TRAM-34 is a highly selective inhibitor of KCa3.1 channel with IC50 value of 20 nM [1].
The Ca (2+)-binding protein calmodulin (CaM) confers Ca (2+) sensitivity to KCa3.1 of KCa3.1. On the basis of crystal structure obtained for the C-terminal region of the rat KCa2.2 channel (rSK2) with CaM that the binding of Ca (2+) to the CaM N-lobe results in CaM interlocking the C-terminal regions of two adjacent KCa3.1 subunits, leading to the formation of a dimeric structure. It is reported that many factors can increase KCa3.1, like balloon injury [2].
TRAM-34 is a KCa3.1 channel inhibitor and plays an important role in many diseases. When tested with human T cells, TRAM-34 treatment inhibited cells mobility and migration via blocking KCa3.1 channel [3]. In coronary smooth muscle cells isolated by laser capture microdissection, delivery of TRAM-34 via balloon catheter significantly blocked the KCa3.1 increase [4]. When tested with COS-7 cells, TRAM-34 inhibited KCa3.1 channel with Kd of 20 ± 3 nM and a Hill coefficient of 1.2 with 1 μM calcium in the pipette [1].
In male Wistar rat model of ischemic stroke, administration of TRAM-34 intraperitoneal (10 or 40 mg/kg, twice daily) for 7 days reduced infarction, neuronal death, microglia activation and neurological deficit via blocking KCa3.1 channel [5].
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原創作者:上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名:上海生物
開 戶 行:中國銀行山東省分行營業部
賬 號:2169 2341 6278