2,3-Butanedione Monoxime (BDM) 是一种肌球蛋白 ATP 酶 (myosin ATPase) 抑制剂，是一种骨骼肌和心肌收缩抑制剂。2,3-Butanedione Monoxime (BDM) 诱导肌质网 Ca2+ 释放。
别名：Biacetyl monoxime; Diacetyl monoxime; DAM
2,3-Butanedione monoxime (BDM) chemically removes phosphate groups from many proteins, and its action on DRK1 channels was examined after expression of DRK1 cRNA in Xenopus oocytes. In two-microelectrode voltage-clamp experiments, the application of 2,3-Butanedione monoxime to the bath inhibited DRK1 current (ki = 16.6 mM, H = 0.96) rapidly and reversibly, with a time course similar to the time course of solution change within the bath. DRK1 current was inhibited at all potentials; the time course of current activation, deactivation and inactivation were unaffected by 2,3-Butanedione monoxime. In inside-out patch-clamp experiments, the application of 2,3-Butanedione monoxime to the cytoplasmic surface similarly inhibited channel activity rapidly and reversibly (ki = 10.7 mM, H = 1.01) in the absence of rephosphorylating substrates. These results are inconsistent with a phosphatase effect, because such an effect should be irreversible in cell-free, ATP-free patches. Instead, the results suggest that 2,3-Butanedione monoxime can inhibit DRK1 channels directly from inside or outside of the membrane.
近来，一种可以使心肌肌球蛋白与肌动蛋白解偶联的药物2，3-丁二酮单肟(2，3-butanedionemonoxime，BDM)作为心肌保护Chemicalbook的“第三种概念”，越来越引人注目。一些研究证实，BDM可以增加兔、鼠和人的心脏对冷缺血的耐受性，可促进L-型Ca2+通道失活，减少心肌能耗。
| 分子量 | 101.1 |
| 分子式 | C4H7NO2 |
| CAS号 | 57-71-6 |
| 溶解性（25°C） | DMSO ≥ 30 mg/mL |
| 储存条件 | 2-8°C, dry, sealed |
| 运输方式 | 冰袋运输，根据产品的不同，可能会有相应调整。 |
*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 9.8912 mL | 49.456 mL | 98.912 mL |
| 5 mM | 1.9782 mL | 9.8912 mL | 19.7824 mL |
| 10 mM | 0.9891 mL | 4.9456 mL | 9.8912 mL |
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km 系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
[3] Arthur Forer, et al. Does 2,3-butanedione monoxime inhibit nonmuscle myosin?
[5] L C Sellin, et al. Multiple effects of 2,3-butanedione monoxime
| 其他相关的Myosin产品 |
|---|
| Myosin Light Chain Kinase Substrate (smooth muscle)
Myosin Light Chain Kinase Substrate (smooth muscle) 是平滑肌肌球蛋白轻链激酶 (MLCK) 合成肽底物。 |
| Kemptamide
Kemptamide，一个 13 个氨基酸的片段，其序列对应于砂囊轻链的第 11-23 位残基。 |
| MYK-224
MYK-224是一种心肌肌球蛋白复合体（Cardiac myosin）调节剂，可用于心血管疾病的相关研究。 |
| Myosin V-IN-1
Myosin V-IN-1 是一种有效的选择性的 Myosin V 抑制剂，Ki 为 6 μM。 |
| 16-38-Thymosin β4 (cattle) TFA
16-38-Thymosin β4 (cattle) TFA 是一种具有高亲和力的非 Ca2+ 依赖性 MLCK 激活剂。 |
产品仅供科学研究或药证申报的用途使用，不为任何个人或者非科研性质的其他用途提供服务。
Copyright © 2010-2022 AbMole版权所有 沪ICP备16047849号 沪公网安备 31011502012228号
蛋白质研究