Clomiphene Citrate

Melting point: 116.5-118°C

Storage temp: 2-8°C

Solubility: Slightly soluble in water, methanol, chloroform, and DMSO. Insoluble in ether.

Form: Powder

Color: White to Off-white

Stability: Hygroscopicity; Light Sensitive

1. Cell Experiment

Solubility in DMSO: ≥ 50 mg/mL (83.60 mM; Hygroscopic DMSO significantly affects product solubility, so use freshly opened DMSO.)

Solubility in H2O: 1 mg/mL (1.67 mM; solubilized with ultrasound)

* "≥" means soluble, but saturation unknown.

Preparing Stock Solutions：

Please prepare the stock solution based on the product's solubility in different solvents. Once prepared, aliquot and store to avoid product degradation caused by repeated freeze-thaw cycles.

Stock solution storage and expiration date: -80°C, 6 months; -20°C, 1 month (sealed, moisture-free). When stored at -80°C, use within 6 months; when stored at -20°C, use within 1 month.

Note: If you choose water as the stock solution, please dilute it to the working solution and then filter it through a 0.22 μm filter membrane for sterilization before use.

2. Animal Experiment

Please select the appropriate dissolution method based on your experimental animal and administration method.

For the following dissolution methods, first prepare a clear stock solution in vitro, then add cosolvents in sequence:

To ensure reliable experimental results, the clear stock solution can be stored appropriately according to storage conditions. For in vivo experiments, it is recommended that you prepare the working solution immediately and use it the same day.

The percentage displayed before the solvent below refers to the volume percentage of the solvent in the final solution. If precipitation or precipitation occurs during preparation, heating and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent in order: 10% DMSO, 40% PEG300, 5% Tween-80, 45% Saline.

Solubility: ≥ 2.5 mg/mL (4.18 mM); Clear Solution

This protocol produces a clear solution with a concentration of ≥ 2.5 mg/mL (saturation unknown).

For a 1 mL working solution, add 100 μL of the 25.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix thoroughly. Add 50 μL of Tween-80 to the solution and mix thoroughly. Then, add 450 μL of normal saline to bring the volume to 1 mL.

To prepare normal saline, dissolve 0.9 g of sodium chloride in ddH₂O and dilute to 100 mL. This will yield a clear, transparent normal saline solution.

Protocol 2

Add each solvent one by one: 10% DMSO, 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

Protocol 3

Add each solvent one by one: 10% DMSO, 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one:  PBS

Solubility: 7.14 mg/mL (11.94 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

Clomifene (previously clomiphene) is an orally administered, non steroidal, ovulatory stimulant that acts as a selective estrogen receptor modulator (SERM). Clomifene can lead to multiple ovulation, and hence increase the risk of conceiving twins. In comparison to purified FSH, the rate of ovarian hyperstimulation syndrome is low. There may be an increased risk of ovarian cancer and weight gain. Clomifene is capable of interacting with estrogen-receptor-containing tissues, including the hypothalamus, pituitary, ovary, endometrium, vagina, and cervix. It may compete with estrogen for estrogen-receptor-binding sites and may delay replenishment of intracellular estrogen receptors. Clomifene initiates a series of endocrine events culminating in a preovulatory gonadotropin surge and subsequent follicular rupture. The first endocrine event, in response to a course of clomifene therapy, is an increase in the release of pituitary gonadotropins. This initiates steroidogenesis and folliculogenesis resulting in growth of the ovarian follicle and an increase in the circulating level of estradiol. Following ovulation, plasma progesterone and estradiol rise and fall as they would in a normal ovulatory cycle.

Clomifene has both estrogenic and anti-estrogenic properties, but its precise mechanism of action has not been determined. Clomifene appears to stumulate the release of gonadotropins, follicle-stimulating hormone (FSH), and leuteinizing hormone (LH), which leads to the development and maturation of ovarian follicle, ovulation, and subsequent development and function of the coprus luteum, thus resulting in pregnancy. Gonadotropin release may result from direct stimulation of the hypothalamic-pituitary axis or from a decreased inhibitory influence of estrogens on the hypothalamic-pituitary axis by competing with the endogenous estrogens of the uterus, pituitary, or hypothalamus. Clomifene has no apparent progestational, androgenic, or antrandrogenic effects and does not appear to interfere with pituitary-adrenal or pituitary-thyroid function.