Cabergoline (Synonyms: FCE 21336) |
カタログ番号GC10441
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カベルゴリンは、麦角由来のドーパミン D2 様受容体アゴニストであり、D2、D3、および 5-HT2B 受容体に高い親和性を持っています (Ki = 0.7、1.5、および 1.2、それぞれ)。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 81409-90-7
Sample solution is provided at 25 µL, 10mM.
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Cabergoline is a long-acting, ergot-derived dopamine receptor agonist[1]. Cabergoline acts by directly binding to D2 receptors in the brain and inhibiting prolactin secretion, and is commonly used in the treatment and research of hyperprolactinemia, Parkinson's disease, and disorders related to abnormal prolactin secretion (such as amenorrhea and infertility, etc.)[2,3,4].
In vitro, Cabergoline (10, 20μM) pretreatment of lipopolysaccharide (LPS, 1μg/mL)-stimulated human brain microvascular endothelial cells (HBMECs) for 24h significantly reduced cell monolayer permeability[5]. Cabergoline (0.01, 0.1, 1, 10, and 50μM) pretreatment of DIV6-7 rat primary cortical neurons for 24h, followed by exposure to 50μM H2O2 to induce oxidative stress injury, dose-dependently inhibited H2O2-induced neuronal cell death[6].
In vivo, Cabergoline (0.25mg/kg/day) was administered intraperitoneally to mice for 7 consecutive days, and the striatum was examined 1h after the final dose, Cabergoline significantly reduced the levels of lipid peroxidation products induced by auto-oxidation[7]. Cabergoline (0.1mg/kg/day) was orally administered to rats with surgically induced endometriosis for 30 days, and the mean surface area of endometriotic implant was significantly reduced from 20.83 ± 3.97mm2 before treatment to 10.41 ± 3.17mm2 after treatment[8].
References:
[1] MIYAGI M, ARAI N, TAYA F, et al. Effect of cabergoline, a long-acting dopamine D2 agonist, on reserpine-treated rodents[J]. Biological and Pharmaceutical Bulletin, 1996, 19(11): 1499-1502.
[2] Su Q Q, Xiang Z F, Qin J, et al. Effects of cabergoline on the fertility of female mice during early and late pregnancy, and potential for its use in mouse control[J]. Crop Protection, 2014, 56: 69-73.
[3] Curran M P, Perry C M. Cabergoline: a review of its use in the treatment of Parkinson’s disease[J]. Drugs, 2004, 64(18): 2125-2141.
[4] Auriemma R S, Granieri L, Galdiero M, et al. Effect of cabergoline on metabolism in prolactinomas[J]. Neuroendocrinology, 2014, 98(4): 299-310.
[5] You L, Jiang H. Cabergoline possesses a beneficial effect on blood-brain barrier (BBB) integrity against lipopolysaccharide (LPS)[J]. Bioengineered, 2021, 12(1): 8358-8369.
[6] Odaka H, Numakawa T, Adachi N, et al. Cabergoline, dopamine D2 receptor agonist, prevents neuronal cell death under oxidative stress via reducing excitotoxicity[J]. PloS one, 2014, 9(6): e99271.
[7] Yoshioka M, Tanaka K, Miyazaki I, et al. The dopamine agonist cabergoline provides neuroprotection by activation of the glutathione system and scavenging free radicals[J]. Neuroscience research, 2002, 43(3): 259-267.
[8] Ercan C M, Kayaalp O, Cengiz M, et al. Comparison of efficacy of bromocriptine and cabergoline to GnRH agonist in a rat endometriosis model[J]. Archives of gynecology and obstetrics, 2015, 291(5): 1103-1111.
| Cell experiment [1]: | |
Cell lines | HBMECs |
Preparation Method | HBMECs (1×105 cells/well) were seeded onto 24-well trans-well inserts and then challenged with 1µg/mL LPS for 24h in the presence and absence of Cabergoline (10, 20μM). After treatment, endothelial monolayer permeability was evaluated by measuring the apparent permeability coefficient (Papp) of fluorescein sodium across the HBMECs monolayer using a Transwell system. |
Reaction Conditions | 10, 20μM; 24h |
Applications | Cabergoline attenuates HBMECs monolayer permeability induced by LPS in HBMECs. |
| Animal experiment [2]: | |
Animal models | Surgically induced endometriosis model rats |
Preparation Method | Rats with surgically induced endometriosis were orally administered Cabergoline (0.1mg/kg/day) for 30 days, and the surface areas of endometriotic implants were measured before and after treatment. |
Dosage form | 0.1mg/kg/day; 30 days; p.o. |
Applications | Treatment of Cabergoline significantly reduced the size of endometriotic implant from 20.83 ± 3.97mm2 to 10.41 ± 3.17mm2. |
References: | |
| Cas No. | 81409-90-7 | SDF | |
| 同義語 | FCE 21336 | ||
| Chemical Name | (6aR,9R,10aR)-7-allyl-N-(3-(dimethylamino)propyl)-N-(ethylcarbamoyl)-4,6,6a,7,8,9,10,10a-octahydroindolo[4,3-fg]quinoline-9-carboxamide | ||
| Canonical SMILES | C=CCN1[C@@]2([H])[C@](C3=C4C(C2)=CNC4=CC=C3)([H])C[C@@H](C(N(C(NCC)=O)CCCN(C)C)=O)C1 | ||
| Formula | C26H37N5O2 | M.Wt | 451.6 |
| 溶解度 | DMSO : 250 mg/mL (553.59 mM; Need ultrasonic) | 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 | 2.2143 mL | 11.0717 mL | 22.1435 mL |
| 5 mM | 442.9 μL | 2.2143 mL | 4.4287 mL |
| 10 mM | 221.4 μL | 1.1072 mL | 2.2143 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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 34 reference(s) in Google Scholar.)