Biacetyl monoxime (Diacetyl monoxime) 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。Biacetyl monoxime 也是一种特征良好的骨骼肌肌球蛋白 II（myosin-II）的化学和运动活性的非竞争性抑制剂。Biacetyl monoxime 诱导肌质网 Ca2+释放。
| 生物活性 | Biacetyl monoxime (Diacetyl monoxime), amyosinATPaseinhibitor, is a skeletal and cardiac muscle contraction inhibitor. Biacetyl monoxime is also a well-characterized non-competitive inhibitor of chemical and motile activity of skeletal musclemyosin-II. Biacetyl monoxime induces sarcoplasmic reticulum Ca2+release[1][2][3]. |
体外研究
(In Vitro) | Biacetyl monoxime (Diacetyl monoxime) (50 mM, 6 and 48 h) decreases cellulase secretion inC. cinerea[1].
Biacetyl monoxime (50 mM, 2 and 4 h) disrupts the localization of the Golgi apparatus, but not that of the endoplasmic reticulum[1].
Biacetyl monoxime (0-30 mM) induces SR Ca2+release (no efflux inhibitors) in a concentration-dependent manner, with a maximal reduction of 72% of SR Ca2+at pCa 6.0[2].
Biacetyl monoxime acts as a chemical phosphatase, which has led to speculation that dephosphorylation of key Ca2+channel proteins may be involved in its inhibition of contraction[2].
Biacetyl monoxime does not inhibit the ATPase activity of two different myosin-I isoforms, myosin-V, or myosin-VI[3].
Biacetyl monoxime (0-50 mM) suppresses L-type Ca2+current of single cardiac myocytes isolated from SHR and WKY rats[4].
Biacetyl monoxime significantly reduces the duration of both spontaneous and electrically stimulated action potentials of cultured neonatal rat cardiomyocytes[4].
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体内研究
(In Vivo) | Biacetyl monoxime (0-200 mg/kg; i.v.; once) shows hypotensive effect[4].
Biacetyl monoxime (0-205 mg/kg; i.p.; once) shows anticonvulsant effect against Picrotoxin (HY-101391)-induced convulsions[5].
| Animal Model: | Male SHR and age-matched WKY rat[4] | | Dosage: | 5, 30, I00 and 200 mg/kg | | Administration: | Intravenous administration, 1 mL/kg, once | | Result: | Decreased arterial blood pressure for both strains, the SHR was significantly more responsive. |
| Animal Model: | Male mice (20 to 25 g)[5] | | Dosage: | 51, 103 and 205 mg/kg in combination with intraperitoneal injection of 3.0 mg/kg Picrotoxin (HY-101391) | | Administration: | Intraperitoneal injection, once | | Result: | Showed dose-dependent anticonvulsant effect against Picrotoxin-induced convulsions. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 125 mg/mL(1236.40 mM;Need ultrasonic) 配制储备液 | 1 mM | 9.8912 mL | 49.4560 mL | 98.9120 mL | | 5 mM | 1.9782 mL | 9.8912 mL | 19.7824 mL | | 10 mM | 0.9891 mL | 4.9456 mL | 9.8912 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (20.57 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (20.57 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (20.57 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (20.57 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (20.57 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (20.57 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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