规格 | 价格 | 库存 | 数量 |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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10g |
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Other Sizes |
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靶点 |
progestogen Receptor
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体外研究 (In Vitro) |
屈螺酮(10-150 μM,24-48 小时)对 PLHC-1 细胞的毒性作用的有效浓度限值(EC50 值)为 105-119 μM(持续 24 小时)和 51-58 μM(持续 48 小时)[1]。 Drospirenone(0.01-10 µM,24 小时)可抑制 HEEC 水溶液中的 PAI-1 和 tPA [2]。 PLHC-1 中细胞 ROS 在 -200 µM 下生成 15-120 分钟 [2]。在小鼠模型 S9 组分中添加 100 µM(72 小时)可能会损坏 MCF-7 细胞中的 DNA [3]。
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体内研究 (In Vivo) |
在雄性和雌性小鼠中,连续五天口服多螺酮(10-100 mg/kg)会损害骨髓细胞中的 DNA [3]。
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细胞实验 |
细胞毒性测定 [1]
细胞类型: PLHC-1 细胞 测试浓度: 10-150 µM 孵育时间: 24 hrs(小时)、48 hrs(小时) 实验结果:细胞活力降低50%,24 hrs(小时后有效浓度)浓度为102-119μM,48小时后有效浓度为51-58μM。 |
动物实验 |
Animal/Disease Models: Adult female mice [3]
Doses: 10 mg/kg, 100mg/kg Route of Administration: po (oral gavage) Experimental Results: DNA damage was induced at dose rates of 10 and 100 mg/kg. Concomitant use with ethinyl estradiol enhances genotoxicity. |
参考文献 |
[1]. Marqueño A, et al. Drospirenone induces the accumulation of triacylglycerides in the fish hepatoma cell line, PLHC-1 [J]. Science of The Total Environment, 2019, 692: 653-659.
[2]. Sabouni R, et al. Drospirenone effects on the plasminogen activator system in immortalized human endometrial endothelial cells [J]. Reproductive sciences, 2021, 28: 1974-1980. [3]. Mir A H, et al. Genotoxic effects of drospirenone and ethinylestradiol in human breast cells (in vitro) and bone marrow cells of female mice (in vivo) [J]. Drug and Chemical Toxicology, 2022, 45(4): 1493-1499. [4]. Motivala A, et al. Drospirenone for oral contraception and hormone replacement therapy: are its cardiovascular risks and benefits the same as other progestogens? [J]. Drugs, 2007, 67: 647-655. [5]. Fuhrmann, U., et al., The novel progestin drospirenone and its natural counterpart progesterone: biochemical profile and antiandrogenic potential. Contraception, 1996. 54(4): p. 243-51. [6]. Muhn, P., et al., Drospirenone: a novel progestogen with antimineralocorticoid and antiandrogenic activity. Pharmacological characterization in animal models. Contraception, 1995. 51(2): p. 99-110. [7]. Warming, L., et al., Safety and efficacy of drospirenone used in a continuous combination with 17beta-estradiol for prevention of postmenopausal osteoporosis. Climacteric, 2004. 7(1): p. 103-11. |
分子式 |
C24H30O3
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分子量 |
366.49
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精确质量 |
366.21949
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元素分析 |
C, 78.65; H, 8.25; O, 13.10
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CAS号 |
67392-87-4
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外观&性状 |
Solid powder
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SMILES |
C[C@]12CCC(=O)C=C1[C@@H]3C[C@@H]3[C@@H]4[C@@H]2CC[C@]5([C@H]4[C@@H]6C[C@@H]6[C@@]57CCC(=O)O7)C
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InChi Key |
METQSPRSQINEEU-HXCATZOESA-N
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InChi Code |
InChI=1S/C24H30O3/c1-22-6-3-12(25)9-17(22)13-10-14(13)20-16(22)4-7-23(2)21(20)15-11-18(15)24(23)8-5-19(26)27-24/h9,13-16,18,20-21H,3-8,10-11H2,1-2H3/t13-,14+,15-,16+,18+,20-,21+,22-,23+,24+/m1/s1
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化学名 |
(1R,2R,4R,10R,11S,14S,15S,16S,18S,19S)-10,14-dimethylspiro[hexacyclo[9.8.0.02,4.05,10.014,19.016,18]nonadec-5-ene-15,5'-oxolane]-2',7-dione
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别名 |
Drospirenona; Drospirenone; Dehydrospirorenone; dihydrospirorenone; drospirenone; Drospirenonum; ZK 3059; ZK30595
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HS Tariff Code |
2934.99.9001
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
DMSO: 50~73 mg/mL (136.4~199.2 mM)
Ethanol: ~12 mg/mL (~32.7 mM) |
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制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 2.7286 mL | 13.6429 mL | 27.2859 mL | |
5 mM | 0.5457 mL | 2.7286 mL | 5.4572 mL | |
10 mM | 0.2729 mL | 1.3643 mL | 2.7286 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
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)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT06039826 | Recruiting | Drug: Drospirenone Drug: Ethinyl Estradiol |
Overweight | Eli Lilly and Company | September 12, 2023 | Phase 1 |
NCT04792385 | Active Recruiting |
Drug: E4/DRSP 15/3 mg combined tablet |
Safety | Estetra | December 28, 2020 | Phase 3 |
NCT05675644 | Not yet recruiting | Drug: Drospirenone-only pill | Contraception | University of Colorado, Denver | February 2023 | Phase 2 |
NCT05461573 | Recruiting | Drug: Drospirenone | Contraception Change in Bone Mineral Density |
Insud Pharma | August 2, 2022 | Phase 3 |
NCT05156879 | Recruiting | Drug: Drospirenone ethinyl estradiol Drug: Aspirin |
Pelvic Pain | Women's Hospital School Of Medicine Zhejiang University |
December 23, 2021 | Phase 4 |