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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Enclomiphene citrate, formerly known as ICI-46476, RMI-16289 and trans-Clomiphene, is a non-steroidal estrogen receptor antagonist that can be taken orally that is being developed as a treatment for secondary hypogonadism in overweight men who want to get their testicles back to normal. Unlike replacement, orally bioavailable enclomiphene citrate increases testosterone and maintains sperm counts in obese hypogonadal men.
| Targets |
estrogen receptor
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|---|---|---|---|
| ln Vitro |
Enclomiphene citrate (0-100 μM, 6 h) suppresses gonadotrophin- and basal-stimulated small- and large-scale ovine luteal cell progesterone secretion in a dose-dependent manner[2].
Enclomiphene citrate (0-100 μg/mL, 24 h) dose-dependently suppresses the rates of blastocyst formation, degeneration, and fertilization in mouse oocytes[3]. Enclomiphene citrate (1 nM-10 μM, 6 h) dose-dependently reduces E2-induced inhibition of follicle stimulating hormone (FSH) secretion in primary sheep pituitary cells[4]. |
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| ln Vivo |
In intact or castrated rats, clomiphene citrate (subcutaneous injection, 0.25 and 0.5 mg/animal, daily) inhibits spermatogenesis and lowers serum levels of testosterone and luteinizing hormone (LH)[5].
Enclomiphene citrate reduces serum cholesterol and body weight to sham levels when administered orally at a dose of 0.03–3 mg/kg per day for 90 days[6]. |
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| Animal Protocol |
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| References |
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| Additional Infomation |
Clomiphene Citrate can cause cancer and developmental toxicity according to state or federal government labeling requirements.
Enclomiphene Citrate is the orally bioavailable citrate salt of enclomiphene, the trans-isomer of the nonsteroidal triphenylethylene compound clomiphene, with tissue-selective estrogenic and antiestrogenic activities. As a selective estrogen receptor modulator (SERM), enclomiphene binds to hypothalamic estrogen receptors, blocking the negative feedback of endogenous estrogens and stimulating the release of gonadotropin-releasing hormone (GnRH) from the hypothalamus; released GnRH subsequently stimulates the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) from the anterior pituitary, resulting in ovulation. In addition, this agent may bind to estrogen receptors on breast cancer cells, resulting in the inhibition of estrogen-stimulated proliferation in susceptible cell populations. The trans or (E)-isomer of clomiphene. See also: Clomiphene Citrate (annotation moved to). |
| Molecular Formula |
C32H36CLNO8
|
|---|---|
| Molecular Weight |
598.089
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| Exact Mass |
597.213
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| Elemental Analysis |
C, 64.26; H, 6.07; Cl, 5.93; N, 2.34; O, 21.40
|
| CAS # |
7599-79-3
|
| Related CAS # |
Enclomiphene;15690-57-0;Clomiphene-d5 citrate;1217200-17-3;Enclomiphene hydrochloride;14158-65-7
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| PubChem CID |
6420009
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| Appearance |
White to off-white solid powder
|
| Boiling Point |
509ºC at 760mmHg
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| Flash Point |
261.6ºC
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| LogP |
5.314
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| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
14
|
| Heavy Atom Count |
42
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| Complexity |
708
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
Cl/C(/C1C=CC=CC=1)=C(\C1C=CC=CC=1)/C1C=CC(=CC=1)OCCN(CC)CC.OC(C(=O)O)(CC(=O)O)CC(=O)O
|
| InChi Key |
PYTMYKVIJXPNBD-BTKVJIOYSA-N
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| InChi Code |
InChI=1S/C26H28ClNO.C6H8O7/c1-3-28(4-2)19-20-29-24-17-15-22(16-18-24)25(21-11-7-5-8-12-21)26(27)23-13-9-6-10-14-23;7-3(8)1-6(13,5(11)12)2-4(9)10/h5-18H,3-4,19-20H2,1-2H3;13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)/b26-25+
|
| Chemical Name |
2-[4-[(E)-2-chloro-1,2-diphenylethenyl]phenoxy]-N,N-diethylethanamine;2-hydroxypropane-1,2,3-tricarboxylic acid
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| Synonyms |
ICI-46476; ICI 46476; ICI46476; RMI-16289; RMI 16289; RMI16289; (E)-Clomiphene citrate; Androxal; Enclomiphene citrate; Enclomid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
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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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~167.2 mM)
Ethanol: ~2 mg/mL (~3.3 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.83 mg/mL (1.39 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.83 mg/mL (1.39 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.83 mg/mL (1.39 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6720 mL | 8.3599 mL | 16.7199 mL | |
| 5 mM | 0.3344 mL | 1.6720 mL | 3.3440 mL | |
| 10 mM | 0.1672 mL | 0.8360 mL | 1.6720 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04887402 | Recruiting | Drug: Clomiphene Citrate | PCO Clomiphene Citrate |
Ain Shams Maternity Hospital | January 1, 2021 | |
| NCT05206448 | Recruiting | Drug: Letrozole Drug: Clomiphene Citrate |
PCOS Infertility |
Rachel Mejia | October 26, 2020 | Phase 4 |
| NCT03615547 | Not yet recruiting | Other: Placebo Drug: Clomiphene Citrate |
Azoospermia, Nonobstructive | Hospices Civils de Lyon | January 2023 | Phase 3 |
| NCT05106712 | Not yet recruiting | Drug: Vitamin D3 Drug: Clomiphene Citrate |
IVF Vitamin D Deficiency |
Umm Al-Qura University | November 1, 2021 | Not Applicable |
| NCT04944836 | Not yet recruiting | Procedure: Rotator Cuff Repair Drug: Clomiphene Citrate |
Rotator Cuff Tears | University of Utah | December 2022 | Phase 2 |
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