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Enclomiphene citrate Sale

(Synonyms: 恩氯米芬柠檬酸盐; (E)-Clomiphene citrate; trans-Clomiphene citrate; Enclomifene citrate) 目录号 : GC35985

An ER modulator

Enclomiphene citrate Chemical Structure

Cas No.:7599-79-3

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10mM (in 1mL DMSO)
¥651.00
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5mg
¥495.00
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10mg
¥765.00
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50mg
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100mg
¥2,295.00
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产品描述

Enclomiphene is an estrogen receptor (ER) modulator.1,2,3 It acts as an ER antagonist in humans, sheep, and rabbits and an ER agonist in rats.1,2,3 Enclomiphene (0.34 ?M) inhibits binding of 17β-estradiol in isolated rabbit uterus.2 It decreases E2-induced inhibition of follicle stimulating hormone (FSH) secretion in primary sheep pituitary cells in a concentration-dependent manner.3 Enclomiphene (0.25 and 0.5 mg/animal) inhibits spermatogenesis and decreases serum luteinizing hormone (LH) and testosterone levels in intact or castrated rats.4 Formulations containing enclomiphene have been used in the treatment of ovarian dysfunction.

1.Hill, S., Arutchelvam, V., and Quinton, R.Enclomiphene, an estrogen receptor antagonist for the treatment of testosterone deficiency in menIDrugs12(2)109-119(2009) 2.Wyss, R.H., Karsznia, R., Heinrichs, W.L., et al.Inhibition of uterine receptor binding of estradiol by anti-estrogens (clomiphene and CL-868)J. Clin. Endocrinol. Metab.28(12)1824-1828(1968) 3.Huang, S.-R., and Miller, W.L.Estrogenic and antiestrogenic effects of enclomiphene and zuclomiphene on gonadotropin secretion by ovine pituitary cells in cultureEndocrinology112(2)442-448(1983) 4.Weissenberg, R., Dar, Y., and Lunenfeld, B.The effect of clomiphene citrate and its Zu or En isomers on the reproductive system of the immature male ratAndrologia24(3)161-165(1992)

Chemical Properties

Cas No. 7599-79-3 SDF
别名 恩氯米芬柠檬酸盐; (E)-Clomiphene citrate; trans-Clomiphene citrate; Enclomifene citrate
Canonical SMILES Cl/C(C1=CC=CC=C1)=C(C2=CC=C(OCCN(CC)CC)C=C2)\C3=CC=CC=C3.O=C(CC(C(O)=O)(O)CC(O)=O)O.[(E)]
分子式 C32H36ClNO8 分子量 598.08
溶解度 DMSO: ≥ 50 mg/mL (83.60 mM) 储存条件 4°C, protect from light
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1 mM 1.672 mL 8.3601 mL 16.7202 mL
5 mM 0.3344 mL 1.672 mL 3.344 mL
10 mM 0.1672 mL 0.836 mL 1.672 mL
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Research Update

Enclomiphene citrate for the treatment of secondary male hypogonadism

Expert Opin Pharmacother 2016 Aug;17(11):1561-7.PMID:27337642DOI:10.1080/14656566.2016.1204294.

Introduction: Hypogonadism is a growing concern in an aging male population. Historically treated using exogenous testosterone, concerns about possible adverse effects of testosterone have led physicians to seek alternative treatment approaches. Areas covered: Enclomiphene citrate is the trans isomer of clomiphene citrate, a non-steroidal estrogen receptor antagonist that is FDA-approved for the treatment of ovarian dysfunction in women. Clomiphene citrate has also been used off-label for many years to treat secondary male hypogonadism, particularly in the setting of male infertility. Here we review the literature examining the efficacy and safety of Enclomiphene citrate in the setting of androgen deficiency. Expert opinion: Initial results support the conclusion that Enclomiphene citrate increases serum testosterone levels by raising luteinizing hormone (LH) and follicle stimulating hormone (FSH) levels, without negatively impacting semen parameters. The ability to treat testosterone deficiency in men while maintaining fertility supports a role for Enclomiphene citrate in the treatment of men in whom testosterone therapy is not a suitable option.

Enclomiphene citrate: A treatment that maintains fertility in men with secondary hypogonadism

Expert Rev Endocrinol Metab 2019 May;14(3):157-165.PMID:31063005DOI:10.1080/17446651.2019.1612239.

Hypogonadism is an important issue among the male population. Treatments such as exogenous testosterone have become very popular. One of the adverse effects of testosterone is its suppression of fertility. This has lead to the use of alternative therapies such as selective estrogen receptor modulators (SERMs) that aim to correct hypogonadism without reducing fertility. Areas covered: The SERM, clomiphene citrate, which is approved by the FDA for the treatment of ovarian dysfunction, has been shown to have beneficial effects on male hypogonadism. Clomiphene citrate exists as a mixture of both the cis-isomer (zuclomiphene) and the trans-isomer (enclomiphene). The literature has suggested that most of the beneficial effects of clomiphene are due to the trans-isomer enclomiphene. Zuclomiphene contributes little to the intended outcomes. The purpose of this drug profile is to examine the available literature on the trans-isomer enclomiphene. Expert opinion: Enclomiphene has been shown to increase testosterone levels while stimulating FSH and LH production. Initial studies demonstrated that enclomiphene maintains the androgenic benefit of clomiphene citrate without the undesirable effects attributable to zuclomiphene. This article reviews the difficulties associated with the FDA approval of a new molecular entity related to the treatment of hypogonadism.

Oral Enclomiphene citrate raises testosterone and preserves sperm counts in obese hypogonadal men, unlike topical testosterone: restoration instead of replacement

BJU Int 2016 Apr;117(4):677-85.PMID:26496621DOI:10.1111/bju.13337.

Objectives: To determine the effects of daily oral doses of Enclomiphene citrate compared with topical testosterone gel treatment on serum total testosterone (TT), luteinising hormone (LH), follicle-stimulating hormone (FSH), and sperm counts in men with secondary hypogonadism. Patients and methods: Two parallel randomised, double-blind, double-dummy, placebo-controlled, multicentre, phase III studies were undertaken to evaluate two doses of Enclomiphene citrate vs testosterone gel (AndroGel(®) 1.62%) on TT, LH, FSH, and sperm counts in overweight men aged 18-60 years with secondary hypogonadism. Men were screened and enrolled in the trials (ZA-304 and ZA-305). All enrolled men had early morning serum TT levels in the low or low normal range (≤300 ng/dL; ≤10.4 nmol/L) and had low or normal LH (<9.4 IU/L) levels measured on two separate occasions 2-10 days apart. Serum samples were obtained over the course of the study to determine relevant hormone levels at baseline and after 16 weeks of treatment. Men provided semen samples twice to enroll at the beginning and twice at the end of the study. Results: TT levels increased between baseline and after 16 weeks of treatment in all the treatment groups. FSH and LH levels increased in the Enclomiphene citrate groups and decreased in the testosterone gel group at 16 weeks. Enclomiphene citrate maintained sperm concentration in the normal range over the treatment period, while there was a marked reduction in spermatogenesis in the testosterone gel group. Conclusions: Enclomiphene citrate consistently increased serum TT, LH and FSH, restoring normal levels of serum TT. Enclomiphene citrate treatment maintained sperm concentrations in the normal range. The effects on TT were also seen with testosterone replacement via testosterone gel but sperm counts were not maintained.

Oral Enclomiphene citrate stimulates the endogenous production of testosterone and sperm counts in men with low testosterone: comparison with testosterone gel

J Sex Med 2013 Jun;10(6):1628-35.PMID:23530575DOI:10.1111/jsm.12116.

Introduction: Clomiphene citrate is employed off-label in men who have low testosterone and for the restoration of sperm counts in men who have used exogenous testosterone. Clomiphene is a mixture of two diastereoisomers: zuclomiphene and enclomiphene. We evaluated Enclomiphene citrate in men with secondary hypogonadism. Aim: Our aim was to compare oral Enclomiphene citrate as an alternative to topical testosterone. Main outcome measures: Blood levels of total testosterone (TT), estradiol, follicle-stimulating hormone (FSH), luteinizing hormone (LH), sex hormone binding globulin, thyroid stimulation hormone, prolactin, and insulin-like growth factor 1 IGF-1 were measured at certain times after treatment with each agent. Sperm parameters were determined at the same visits. Free testosterone (FT) was calculated. Methods: This was a proof-of-principle, randomized, open-label, fixed dose, active-control, two-center phase IIB study in 12 men with secondary hypogonadism treated previously with topical testosterone. Results: After discontinuation of topical testosterone, morning TT values averaged 165 ± 66 pg/dL. After 3 months, there was a significant rise in men receiving Enclomiphene citrate and gel that was sustained for 3 months. At 6 months, TT levels were 545 ± 268 and 525 ± 256 pg/dL for groups receiving the gel and Enclomiphene citrate, respectively. Only men in the Enclomiphene citrate group demonstrated increased LH and FSH. TT decreased one month posttreatment to pretreatment values. Enclomiphene citrate elevated sperm counts in seven out of seven men at 3 months and six out of six men at 6 months with sperm concentrations in the 75-334 × 10(6) /mL range. The gel was ineffective in raising sperm counts above 20 × 10(6) /mL for all five men at 3 months and raised counts in only two or five men at 6 months. At follow-up, only Enclomiphene citrate treatment was associated with elevated sperm counts. Conclusions: Enclomiphene citrate increased testosterone and sperm counts. Concomitant changes in LH and FSH suggest normalization of endogenous testosterone production and restoration of sperm counts through the hypothalamic-pituitary-testicular axis.

Enclomiphene citrate stimulates testosterone production while preventing oligospermia: a randomized phase II clinical trial comparing topical testosterone

Fertil Steril 2014 Sep;102(3):720-7.PMID:25044085DOI:10.1016/j.fertnstert.2014.06.004.

Objective: To determine the effect of Enclomiphene citrate in men with secondary hypogonadism. Design: Phase II clinical trial. Setting: Community dwelling men making visits to physician offices. Patient(s): Men with secondary hypogonadism. Intervention(s): Oral administration of Enclomiphene citrate or 1% topical T gel. Main outcome measure(s): Luteinizing hormone, FSH, T, and semen analysis. Result(s): Treatment with Enclomiphene citrate resulted in increased morning serum T, E2, and LH levels similar to those obtained with a topical T gel in men with secondary hypogonadism. Follicle-stimulating hormone and LH were increased with enclomiphene, and sperm counts were conserved. Conclusion(s): Enclomiphene citrate reverses the two hallmarks of secondary hypogonadism, namely, low serum total T and low or inappropriately normal LH while preserving sperm production. Clinical trial registration number: NCT01270841 (ClinicalTrials.gov Identifier NCT01270841).