trans-Clomiphene Citrate

trans-Clomiphene Citrate

trans-Clomiphene CitrateWomen's health
CAS: 7599-79-3
MF: C32H36ClNO8
MW: 598.08314
适应症
Hypogonadism; Obesity; Type 2 diabetes; Infertility; Prolactinoma
作用靶点
Estrogen Receptor/ERR
用途

trans-Clomiphene Citrate, stereoisomer of Clomiphene Citrate (C587025), a synthetic estrogen agonist-antagonist. Gonad-stimulating principle.

规格标准
USP, EP
描述

概况

Enclomiphene ((E)-Clomiphene) citrate is an effective, orally available, non-steroidal estrogen receptor (rogen receptor) antagonist with anti-estrogenic effects. Enclomiphene citrate can be used for the study of ovarian dysfunction, testosterone deficiency, maleogonadism, and type 2 diabetes.

Synonyms: trans-clomifene citrate; Unii-J303A6U9Y6; (E)-Clomiphene citrate; Androxal; Clomiphene B citrate; J303A6U9Y6 (UNII code); ICI-46476 (free base); RMI-16289 (free base); enclomifene citrate; cis/trans clomiphene citrate; Enclomiphene citrate; trans-Clomiphene citrate; Triethylamine, 2-(p-(2-chloro-1,2-diphenylvinyl)phenoxy)-, citrate, (E)-

EINECS: 000-000-0

Product Categories: Amines, Aromatics, Pharmaceuticals, Intermediates & Fine Chemicals;API

Mol File: 7599-79-3.mol

物化性质

Melting point: 143-145°C

Storage temp: Amber Vial, -20°C Freezer

Solubility: DMSO (Slightly), Ethyl Acetate (Slightly, Heated, Sonicated), Methanol (Slightly)

Form: Solid

Color: White to Off-White

Stability: Light Sensitive

MSDS信息

实验数据

1. Cell Experiment

Solubility in DMSO: ≥ 50 mg/mL (83.60 mM; Hygroscopic DMSO significantly affects solubility. Use newly opened DMSO)

"≥" means soluble, but saturation unknown.

Preparing Stock Solutions:

image

Based on the solubility of the product in different solvents, choose an appropriate solvent to prepare the stock solution. Once dissolved, aliquot and store to avoid product inactivation caused by repeated freeze-thaw cycles.

Storage method and period of stock solutions: -80°C, 6 months; -20°C, 1 month (sealed storage, protected from moisture and light). When stored at -80°C, use within 6 months; when stored at -20°C, use within 1 month.


2. Animal Experiment

Please choose the appropriate dissolution scheme according to your experimental animals and administration methods. The following dissolution schemes need to be prepared with clear stock solutions according to the In Vitro method first, and then the solubilizers are added in turn:


——To ensure the of the experimental results, the clear stock solution can be properly preserved according to the storage conditions; for in vivo experiments, it is recommended to prepare the working solution for use and use it on the same day; The percentage shown before each solvent refers to the volume ratio of that solvent in the final solution you prepare; if precipitation or occurs during the preparation process, it can be solubilized by heating and/or ultrasound.


Scheme One

Please add each solvent in turn: 10%MSO 40% PEG300 5% Tween-80 45% Saline Solubility: ≥ 0.3 mg/mL (1.39 mM); clear solution This scheme can obtain a clear solution of ≥ 0.83 mg/mL (saturation unknownFor example, to prepare 1 mL of working solution, take 100 μL of clear DMSO stock solution of 8.3 mg/mL and it to 400 μL of PEG300, mix well; then add 50 μL of Tween-80 to the above, mix well; and then continue to add 450 μL of normal saline to make up to 1 mL. Preparation of normal saline: Diss 0.9 g of sodium chloride in ddH₂O and make up to 100 mL to obtain a clear and transparent normal saline solution.


Scheme Two

Please add each solvent in turn: 10% DMSO 90% (20% SBE-β-CD in Saline) Solility: ≥ 0.83 mg/mL (1.39 mM); clear solution This scheme can obtain a clear solution of ≥ 0.8 mg/mL (saturation unknown). For example, to prepare 1 mL of working solution, take 100 μL of clear DMSO stock solution 8.3 mg/mL and add it to 900 μL of 20% SBE-β-CD normal saline solution, mix well. g of SBE-β-CD (sulfobutyl ether β-cyclodextrin) powder is made up to 10 mL of normal, completely dissolved to clear and transparent.


Scheme Three

Please add each solvent in turn: 10% DMSO 90% Corn Oil Solility: ≥ 0.83 mg/mL (1.39 mM); clear solution This scheme can obtain a clear solution of ≥ 0.8 mg/mL (saturation unknown), and this scheme is used for animal experiments with an experimental cycle of more than half a month. For example, to prepare 1 of working solution, take 100 μL of clear DMSO stock solution of 8.3 mg/mL and add it to 900 μ of corn oil, mix well.

Enclomiphene citrate

Complete reserve solution preparation table

* Please choose the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is, please store it in separate containers to avoid product failure caused by repeated freezing and thawing. Storage method and shelf life of the stock solution: -80°C 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it 6 months, and when stored at -20°C, please use it within 1 month.

Pharmacodynamics

Mechanism Of Action