Allylestrenol
(Synonyms: 烯丙雌醇) 目录号 : GC39337
Allylestrenol is an orally active progestagen of the 19-nortestosterone series resembling progesterone.
Cas No.:432-60-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Allylestrenol is an orally active progestagen of the 19-nortestosterone series resembling progesterone.
[1] E W Bergink, et al. J Steroid Biochem. 1985 Aug;23(2):165-8.
| Cas No. | 432-60-0 | SDF | |
| 别名 | 烯丙雌醇 | ||
| Canonical SMILES | C[C@@]12[C@](O)(CC=C)CC[C@@]1([H])[C@]3([H])CCC4=CCCC[C@]4([H])[C@@]3([H])CC2 | ||
| 分子式 | C21H32O | 分子量 | 300.48 |
| 溶解度 | DMSO: ≥ 50 mg/mL (166.40 mM) | 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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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.328 mL | 16.64 mL | 33.2801 mL |
| 5 mM | 0.6656 mL | 3.328 mL | 6.656 mL |
| 10 mM | 0.3328 mL | 1.664 mL | 3.328 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，
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 saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Efficacy of Allylestrenol combined with ritodrine on threatened premature labor and its influence on inflammatory factors in peripheral blood
Exp Ther Med 2020 Feb;19(2):907-912.PMID:32010251DOI:10.3892/etm.2019.8273.
Efficacy of Allylestrenol combined with ritodrine on threatened premature labor (TPTL) and its influence on inflammatory factors in peripheral blood were investigated. A total of 206 cases of TPTL patients from 2014 to 2016 were collected in Zhongshan Hospital Affiliated to Fudan University, and 106 cases were treated with Allylestrenol combined with ritodrine as a research group and 100 cases were treated with Allylestrenol combined with magnesium sulfate as a control group. General information of patients was collected, and changes in the expression levels of IL-17, IL-10 and IL-6 were detected by enzyme-linked immunosorbent assay. Prolonged pregnancy time, success rate of fetal protection and average delivery time of patients were recorded. The adverse pregnancy conditions were compared, including the Apgar score of newborns, birth weight and adverse conditions, and postpartum hemorrhage volume and postpartum hospital stays in the two groups were recorded. Prolonged pregnancy time, success rate of fetal protection and average delivery time in the research group were significantly higher than those in the control group (P<0.05). After treatment, the levels of IL-17, IL-10 and IL-6 in serum of the two groups were significantly lower than those before treatment (P<0.05), and were significantly lower in the research group than in the control group (P<0.05). The average neonatal weight and Apgar score in the research group were significantly better than those in the control group (P<0.05). Postpartum hemorrhage, postpartum hospital stays and incidence rate of toxic side effects, neonatal death, malformation and asphyxia in the research group were significantly lower than those in the control group (P<0.05). Allylestrenol combined with ritodrine can significantly reduce the expression levels of IL-17, IL-10 and IL-6 in TPTL, reduce adverse pregnancy conditions, prolong gestational weeks, and has higher safety and better application value.
A case-control study to evaluate the risk of congenital anomalies as a result of Allylestrenol therapy during pregnancy
Clin Ther 1988;10(6):725-39.PMID:3219686doi
The 1980-1984 data base of the Hungarian Case Control Surveillance System for Congenital Anomalies was used to evaluate possible teratogenicity of Allylestrenol therapy during pregnancy. In an initial global analysis, three of the 24 congenital anomaly groups studied (ie, clubfoot, multiple anomalies, and hypospadias) had a significantly higher incidence of Allylestrenol use. A case control analysis, however, excluded a pathogenetic role for Allylestrenol in the etiology of clubfoot and multiple congenital anomalies. A greater use of Allylestrenol in the first global evaluation was explained by a higher incidence in these groups of impending miscarriage and preterm labor, which are indications for Allylestrenol therapy. The case control analysis did indicate a greater use of Allylestrenol in the hypospadias group, but this difference was not statistically significant in the critical period for induction of hypospadias (ie, the third and fourth months of gestation). The causal role of subfertility in the etiology of hypospadias was an indirect factor, explaining the greater use of Allylestrenol during pregnancy in this group; in Hungary, women with a history of infertility frequently receive hormonal support in the first trimester. The authors conclude that the data analyzed do not indicate any teratogenic effects of the use of Allylestrenol during pregnancy.
Receptor binding of Allylestrenol, a progestagen of the 19-nortestosterone series without androgenic properties
J Steroid Biochem 1985 Aug;23(2):165-8.PMID:3928974DOI:10.1016/0022-4731(85)90232-8.
Allylestrenol (17 alpha-allyl-17 beta-hydroxy-4-estren) is an orally active progestagen of the 19-nortestosterone series resembling progesterone since it has no detectable androgenic activity in animal studies and in the human. In the present study, the affinity of its 3-keto metabolite for the transformed progesterone receptor in intact MCF-7 cells was about twice that of progesterone and cyproterone acetate and about 2-3 times less than that of medroxyprogesterone acetate and norethisterone, reflecting the known progestational activity of Allylestrenol. The affinity of 3-ketoallylestrenol for the transformed androgen receptor in intact MCF-7 cells was weak (like other progestagens lacking androgenic activity or possessing anti-androgenic activity) and lower than that of weakly androgenic progestagens. On the other hand, the relatively high affinity of 3-keto-allylestrenol for the non-transformed androgen receptor at 4 degrees C in the cytosol fraction did not reflect the known lack of androgenic activity of Allylestrenol. Thus competitive studies carried out with transformed receptor complexes in intact cells at 37 degrees C and non-transformed complexes in cytosol distinguish progestagen with weak androgenic activity (e.g. norethisterone) from those displaying no androgenic activity or possessing anti-androgenic activity (e.g. 3-keto-allylestrenol, progesterone, cyproterone acetate and spironolactone).
The effect of estradiol valerate and Allylestrenol on endometrial transformation in hypergonadotropic hypogonadic women
Eur J Obstet Gynecol Reprod Biol 1987 Jul;25(3):221-9.PMID:3609436DOI:10.1016/0028-2243(87)90102-x.
The effect of estradiol valerate and Allylestrenol on the endometrial transformation of five hypergonadotropic hypogonadic women was evaluated. Estradiol valerate was administered throughout the whole induced cycle (28 days), while Allylestrenol was added during the second half of the cycle. Endometrial biopsies were performed during Allylestrenol treatment and were evaluated histologically. Samples of endometrium were also subjected to one-dimensional SDS electrophoresis. Of ten biopsies performed, only one was interpreted to be in-phase, while the others were dated proliferative (4 biopsies) or showed abortive or out-of-phase secretory transformation. The highest mean serum progesterone level, detected under Allylestrenol treatment, was 1.5 ng/ml. Protein electrophoresis demonstrated relative sequential changes in the protein patterns of the 115 kDa and 150 kDa protein bands. It is concluded that Allylestrenol, although having gestagen properties, may not be efficient for the induction of an adequate secretory transformation of human endometrium in the absence of ovaries.
Allylestrenol: three years of experience with Gestanon in threatened abortion and premature labor
Clin Ther 1980;3(3):200-8.PMID:7459930doi
Allylestrenol was used to treat 375 women with threatened pregnancies. Results show that this drug is capable of maintaining pregnancy in a large series of ambulant patients and is safe for both mother and child. Allylestrenol does not maintain pregnancy if placental dysfunction is present, however. Newborns whose mothers are treated with Allylestrenol have slightly higher birth weights than controls. The possible role of Allylestrenol in this process is discussed. At high doses, Allylestrenol effectively stops premature labor, suggesting a selective action on the myometrium.