RHC 80267是一种有效的、选择性二酰基甘油脂酶（DAGL）抑制剂，RHC 80267还能够抑制胆碱酯酶活性（IC₅₀=4μM），可抑制环氧化酶（COX）活性和磷脂酰胆碱的水解。
Cas No.:83654-05-1
Sample solution is provided at 25 µL, 10mM.
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RHC 80267 is a potent and selective diacylglycerol lipase (DAGL) inhibitor. RHC 80267 can also inhibit cholinesterase activity (IC₅₀= 4µM), suppress cyclooxygenase (COX) activity, and inhibit phosphatidylcholine hydrolysis[1-2]. RHC 80267 functions by inhibiting diacylglycerol lipase, and RHC 80267 can be used in research related to the nervous system, cardiovascular system, and metabolic diseases[3-4].
In vitro, RHC 80267 (100µM) was used to pretreat rat cortical astrocytes for 2-6 hours, followed by culture under combined glucose-oxygen deprivation conditions. RHC 80267 significantly inhibited ischemia-induced arachidonic acid metabolite release but exacerbated cellular damage[5]. RHC 80267 (10–100µM) was used to treat GH3 pituitary cells for 1-4 hours. RHC 80267 inhibited prolactin secretion from the cells and blocked potassium-stimulated calcium influx[6].
In vivo, in a mouse model of temporal lobe epilepsy induced by pilocarpine, RHC 80267 (1.3µmol/animal; for 7 consecutive days) was administered via intracerebroventricular injection. RHC 80267 significantly reduced the incidence and duration of spontaneous recurrent seizures during the chronic phase, improved anxiety- and depression-like behaviors, enhanced spatial learning and memory capacity, and inhibited neuronal loss in the hippocampal CA1 region[7].
References:
[1] Chuang M, Severson DL. Inhibition of diacylglycerol metabolism in isolated cardiac myocytes by U-57 908 (RHC 80267), a diacylglycerol lipase inhibitor. J Mol Cell Cardiol. 1990 Sep;22(9):1009-16.
[2] Sutherland CA, Amin D. Relative activities of rat and dog platelet phospholipase A2 and diglyceride lipase. Selective inhibition of diglyceride lipase by RHC 80267. J Biol Chem. 1982 Dec 10;257(23):14006-10.
[3] Ghisdal P, Vandenberg G, Hamaide MC, et al. The diacylglycerol lipase inhibitor RHC-80267 potentiates the relaxation to acetylcholine in rat mesenteric artery by anti-cholinesterase action. Eur J Pharmacol. 2005 Jul 4;517(1-2):97-102.
[4] Oglesby TD, Gorman RR. The inhibition of arachidonic acid metabolism in human platelets by RHC 80267, a diacylglycerol lipase inhibitor. Biochim Biophys Acta. 1984 Apr 18;793(2):269-77.
[5] Haun SE, Trapp VL, Clotz MA, et al. Nordihydroguaiaretic acid and RHC 80267 potentiate astroglial injury during combined glucose-oxygen deprivation. Mol Chem Neuropathol. 1995 May;25(1):35-49.
[6] Camoratto AM, Grandison L. Effects of RHC 80267, a diglyceride lipase inhibitor, on prolactin secretion and calcium uptake in GH3 pituitary cells. Life Sci. 1987 Jan 19;40(3):275-81.
[7] Ma L, Wang L, Yang F, et al. Disease-modifying effects of RHC80267 and JZL184 in a pilocarpine mouse model of temporal lobe epilepsy. CNS Neurosci Ther. 2014 Oct;20(10):905-15.
RHC 80267是一种有效的、选择性二酰基甘油脂酶（DAGL）抑制剂，RHC 80267还能够抑制胆碱酯酶活性（IC₅₀=4μM），可抑制环氧化酶（COX）活性和磷脂酰胆碱的水解[1-2]。RHC 80267通过抑制二酰基甘油脂酶发挥作用，RHC 80267可用于神经系统、心血管系统以及代谢疾病的相关研究[3-4]。
在体外，RHC 80267（100μM）预处理大鼠皮质星形胶质细胞2-6小时，随后在葡萄糖-氧气联合剥夺条件下培养，RHC 80267显著抑制缺血诱导的花生四烯酸代谢物释放，加剧细胞损伤[5]。RHC 80267（10–100μM）处理GH3垂体细胞1-4小时，RHC 80267可抑制细胞的泌乳素分泌，阻断钾离子刺激的钙内流[6]。
在体内，在中，RHC 80267（1.3μmol/只；持续7天）侧脑室注射处理Pilocarpine诱导颞叶癫痫模型小鼠，RHC 80267显著降低慢性期自发性复发癫痫的发生率及发作持续时间，并改善焦虑抑郁样行为、空间学习记忆能力，同时抑制海马CA1区神经元丢失[7]。
| Cell experiment [1]: | |
Cell lines | GH3 pituitary cells (rat anterior pituitary tumor cell line) |
Preparation Method | GH3 cells were maintained in Ham's F-10 medium supplemented with 10% fetal bovine serum at 37°C, 5% CO₂. GH3 cells were treated with RHC 80267 at concentrations ranging from 10-100μM for 1-4 hours. |
Reaction Conditions | 10-100μM; 1-4h |
Applications | RHC 80267 significantly inhibited basal prolactin secretion in a dose-dependent manner, with higher concentrations (50-100μM) maintaining inhibition for up to 4 hours. RHC 80267 (10μM) completely blocked TRH-induced and phospholipase C-induced prolactin secretion but did not affect PMA-stimulated secretion. RHC 80267 (10-50μM) concentration-dependently inhibited potassium-stimulated ⁴⁵calcium influx, suggesting blockade of voltage-dependent calcium channels as an alternative mechanism for its inhibitory actions on prolactin secretion. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | Mice were administered Pilocarpine (100mg/kg; i.p.) to induce status epilepticus (SE), followed by Diazepam (10mg/kg; i.p.) after 70 minutes to terminate seizures. RHC 80267 (1.3μmol/animal) was administered intracerebroventricularly (i.c.v.) immediately after SE termination and once daily for the next 7 days. Control groups received vehicle injections. Mice were monitored for spontaneous recurrent seizures (SRS) from weeks 3-6 post-SE and underwent behavioral tests (open field, elevated plus maze, tail suspension, Morris water maze) during weeks 7-10. |
Dosage form | 1.3μmol/animal; i.c.v.; Once daily for 7 days. |
Applications | RHC 80267 treatment significantly reduced the percentage of mice experiencing SRS and decreased seizure duration. RHC 80267 attenuated depression- and anxiety-like behaviors, improved spatial learning and memory in the Morris water maze, and inhibited hippocampal neuronal loss in the CA1 region during the chronic epileptic period. |
References: | |
| Cas No. | 83654-05-1 | SDF | |
| 别名 | 1,6-双(环己基脒基羰基氨基)己烷,U-57908 | ||
| 化学名 | cyclohexanone O-((E)-((6-((E)-(((cyclohexylideneamino)oxy)(hydroxy)methylene)amino)hexyl)imino)(hydroxy)methyl) oxime | ||
| Canonical SMILES | O/C(O/N=C1CCCCC/1)=N\CCCCCC/N=C(O/N=C2CCCCC/2)\O | ||
| 分子式 | C20H34N4O4 | 分子量 | 394.51 |
| 溶解度 | DMF: 15 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 5 mg/ml,Ethanol: 5 mg/ml | 储存条件 | Store at -20°C |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5348 mL | 12.6739 mL | 25.3479 mL |
| 5 mM | 507 μL | 2.5348 mL | 5.0696 mL |
| 10 mM | 253.5 μL | 1.2674 mL | 2.5348 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
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