| BetamethasoneGlucocorticoid receptor agonist |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 99.76%
- COA (Certificate Of Analysis)
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Chemical structure
| Cell experiment [1]: | |
Cell lines | Human astrocytoma |
Preparation method | The solubility of this compound in DMSO is >19.6 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | 10 μg/ml |
Applications | Bexamethasone (1.3-50 μg/ml) decreased cloning efficiency and colony size in cultured human astrocytoma. In MRC5 human diploid fibroblasts, betamethasone (8 μg/ml) increased cloning efficiency by two-fold. Betamethasone (2-16 μg/ml) did not affect colony size. |
| Animal experiment [2,3]: | |
Animal models | Pregnant rabbits, Pregnant ewes |
Dosage form | 0.5 mg/kg |
Application | Pregnant rabbits were injected with either 0.8 mg of betamethasone on days 24 and 25 of gestation and delivered by cesarean section on day 26. Bexamethasone significantly reduced the weight of fetuses and fetal brain, lungs, liver, and placenta. In pregnant ewes, BET (0.5 mg/kg) decreased fetal (121–146 dG) and placental (121 dG) weights. Maternal plasma oPL levels in controls increased across gestation; fetal plasma oPL levels decreased. BNCs were reduced by 24% to 47% after BET. Placental oPL protein levels, maternal and fetal plasma oPL levels were also reduced after BET injections, but recovered to values that were not different to controls near term. BET (0.5 mg/kg) disrupted the normal distribution of BNCs within the placentome. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Guner M, Freshney R I, Morgan D, et al. Effects of dexamethasone and betamethasone on in vitro cultures from human astrocytoma[J]. British journal of cancer, 1977, 35(4): 439. [2]. Barrada M I, Blomquist C H, Kotts C. The effects of betamethasone on fetal development in the rabbit[J]. American journal of obstetrics and gynecology, 1980, 136(2): 234-238. [3]. Braun T, Li S, Moss T J M, et al. Maternal betamethasone administration reduces binucleate cell number and placental lactogen in sheep[J]. Journal of Endocrinology, 2007, 194(2): 337-347. | |
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| Cas No. | 378-44-9 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | (8S,9R,10S,11S,13S,14S,16S,17R)-9-fluoro-11,17-dihydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-3-one | ||
| Canonical SMILES | CC1CC2C3CCC4=CC(=O)C=CC4(C3(C(CC2(C1(C(=O)CO)O)C)O)F)C | ||
| Formula | C22H29FO5 | M.Wt | 392.46 |
| Solubility | ≥19.6mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Betamethasone is a synthetic corticosteroid and agonist of glucocorticoid receptor [1].
Betamethasone has shown the inflammatory response by the betamethasone-receptor complex modulated the activity of certain genes, altering the production and activity of proteins. These proteins include phospholipase A2, cyclooxygenase-2 and NO-synthase. Betamethasone has been reported to inhibit the expression of these enzymes results in reduced production of such inflammatory mediators as prostaglandins, leukotrienes and nitric oxide. In addition betamethasone has also revealed to inhibit keratinocyte proliferation [1].
References:[1] Pharmacology Review(s)-FDA.
http://www.accessdata.fda.gov/drugsatfda_docs/nda/2006/021852s000_PharmR.pdf
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要是能上传一些真实药厂设备，也许对大家都有帮助。
下面上传《常用制剂设备》的图扫描。
http://www.k65.net/mail/url.php?n=eXpmMzcyMT0v
code:37217613
比较电泳设备.pdf(425.0k)
先说出自己这几天学习注射剂的心得：
关于注射剂仿制，先对照原研处方，处方设计尽量和原研一致，通过考察评价外观、色泽、澄明度、pH、含量、有关物质、细菌内毒素或热原、不溶性微粒和稳定性等，确定一个符合标准的相关标准高于原研药的处方。也就是说注射剂仿制就是通过处方和工艺的筛选找出一个满足标准（pH、含量、有关物质、细菌内毒素或热原等）的处方和工艺，这个是不是仿制的基本思路？
而这其中有还很多问题。只有思路还不进行实际研发。
比如处方设计中，一般常用辅料有哪些？
一般在什么情况下需要加入什么特殊的辅料？比如pH调节剂，抑菌剂等。
做研发的实验步骤是如何。有了一个初步的处方，我们第一步是配溶液？还有灭菌、封口这个步骤是怎样的？每一步都用什么设备，有几种工艺可以选，还一般的操作条件如温度速度时间等。
很多细节问题和思路问题，做注射剂的高手和新手们都来说说哦。这是一个开放的交流大家可以说的更远，说出自己的精华。
另外版主给加个积分呗，很多帖子我看不了！！！
下面是我觉得做注射剂必须了解的基本法规链接，给新手看滴，希望有帮助
http://www.sfda.gov.cn/WS01/CL0058/9348.html
关于印发《可见异物检查法补充规定》的通知
http://www.sfda.gov.cn/WS01/CL0055/27800.html
关于发布化学药品注射剂和多组分生化药注射剂基本技术要求的通知
http://www.sfda.gov.cn/WS01/CL0055/24969_9.html
关于开展注射剂类药品生产工艺和处方核查工作的通知
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