RHC 80267 (Synonyms: U-57908) |
رقم الكتالوجGC12411
One-Click Copy Product Info
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RHC 80267 (U-57908) هو مثبط قوي وانتقائي للدياسيل جلسرين ليباز (DAGL) (مع IC 50 من 4 ميكرومتر في الصفائح الدموية للكلاب)
Products are for research use only. Not for human use. We do not sell to patients.
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.
| Cell experiment [1]: | |
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Cell lines |
GH3 pituitary cells (rat anterior pituitary tumor cell line) |
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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. |
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Reaction Conditions |
10-100μM; 1-4h |
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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]: | |
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Animal models |
C57BL/6 mice |
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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. |
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Dosage form |
1.3μmol/animal; i.c.v.; Once daily for 7 days. |
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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. |
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References: |
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| Cas No. | 83654-05-1 | SDF | |
| المرادفات | U-57908 | ||
| Chemical Name | 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 | ||
| Formula | C20H34N4O4 | M.Wt | 394.51 |
| الذوبان | DMF: 15 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 5 mg/ml,Ethanol: 5 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 27 reference(s) in Google Scholar.)