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ELN-441958是一种B1受体拮抗剂,能够抑制B1激动剂配体[3H] DAKD 与IMR-90细胞结合(Ki:0.26 nM),相较于B2受体,它对B1受体的抑制作用具有更高的选择性,且比抑制μ阿片受体选择性高500多倍,比抑制δ阿片受体选择性高2000多倍。
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ELN-441958是一种B1受体拮抗剂,能够抑制B1激动剂配体[3H] DAKD 与IMR-90细胞结合(Ki:0.26 nM),相较于B2受体,它对B1受体的抑制作用具有更高的选择性,且比抑制μ阿片受体选择性高500多倍,比抑制δ阿片受体选择性高2000多倍。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 473 | 现货 | |
5 mg | ¥ 1,180 | 现货 | |
10 mg | ¥ 1,900 | 现货 | |
25 mg | ¥ 3,160 | 现货 | |
50 mg | ¥ 4,470 | 现货 | |
100 mg | ¥ 5,910 | 现货 | |
200 mg | ¥ 7,960 | 现货 |
产品描述 | ELN-441958 is a potent, neutral antagonist of B1 receptor, inhibits the binding of the B1 agonist ligand [3H]DAKD to IMR-90 cells with Ki of 0.26 nM. ELN-441958(ELN 441958) is highly selective for B1 over B2 receptors. |
靶点活性 | Bradykinin B1:0.26 nM(ki) |
激酶实验 | IGF-IR Peptide Autophosphorylation: One microgram of constitutively active IGF-IR kinase domain peptide isincubated +/? varying concentrations of PQ 401 in 2% DMSO in 40 mM Tris (pH 7.4), 80 μMEGTA, 0.25% 2-mercaptoethanol, 80 μM Na3VO4, 10 mM MgCl2, and 2 mM MnCl2 for 20 minutes. ATP isthen added at a final concentration of 20 μM. Autophosphorylation of the kinase domain peptide isallowed to occur for 20 minutes at 22℃. The reaction isstopped by the addition of SDS-reducing buffer and the samples are run on SDS-PAGE. Following transfer to nitrocellulose membrane, peptide autophosphorylation isdetermined by Western blotting employing an antibody against phosphotyrosine (PY20). |
别名 | ELN 441958 |
分子量 | 501.02 |
分子式 | C29H29ClN4O2 |
CAS No. | 913064-47-8 |
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: 5.01 mg/mL (10 mM) | ||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||
DMSO
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