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Midaglizole hydrochloride ((±)-DG5128) (DG5128) 是有效的 α2-肾上腺素受体拮抗剂。Midaglizole hydrochloride (DG5128) 对 α2-肾上腺素能受体的亲和力 (pKi= 6.28) 比 α1-肾上腺素能受体高 7.4 倍。
Midaglizole hydrochloride ((±)-DG5128) (DG5128) 是有效的 α2-肾上腺素受体拮抗剂。Midaglizole hydrochloride (DG5128) 对 α2-肾上腺素能受体的亲和力 (pKi= 6.28) 比 α1-肾上腺素能受体高 7.4 倍。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 497 | 现货 | |
5 mg | ¥ 1,270 | 现货 | |
10 mg | ¥ 1,780 | 现货 | |
25 mg | ¥ 2,820 | 现货 | |
50 mg | ¥ 3,880 | 现货 | |
100 mg | ¥ 5,220 | 现货 | |
200 mg | ¥ 6,900 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,390 | 现货 |
产品描述 | Midaglizole hydrochloride ((±)-DG5128) (DG5128) is a preferred α2-adrenoceptor antagonist. Midazolazole hydrochloride (DG5128) has an affinity for α2-adrenoceptor (pKi = 6.28) 7.4 times higher than that of α1-adrenoceptor. |
靶点活性 | α2-adrenoceptor:6.28(pKi ) |
体外活性 | Midaglizole hydrochloride (DG-5128)在浓度高达10μM时,对脑膜中[3H]克隆定的抑制作用优于[3H]帕唑辛。Midaglizole hydrochloride 诱导大鼠胰岛及MIN6β细胞线胰岛素释放的EC50值分别为200 nM和24μM。Midaglizole hydrochloride 对Kir6.2与Kir6.2/SUR1诱导的KATP电流的IC50值分别为3.8μM和4.4μM。 |
体内活性 | Midaglizole(3 和 30 mg/kg,静脉注射)能够提高去髓大鼠的血压[1]。 |
别名 | DG5128 hydrochloride, (±)-DG5128 hydrochloride |
分子量 | 324.25 |
分子式 | C16H19Cl2N3 |
CAS No. | 79689-25-1 |
Smiles | C1(C(CC2=NCCN2)C3=CC=CC=C3)=NC=CC=C1.Cl.Cl |
密度 | 1.31g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 45 mg/mL (138.78 mM), Sonication and heating to 60℃ are recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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