| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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| Other Sizes |
| Targets |
Estrogen receptor; Dengue virus
Cyclofenil targets estrogen receptors, particularly ERβ. It acts as a selective estrogen receptor modulator. By modulating estrogen receptor activity, it influences gonadotropin secretion and ovulation. It also has anti-dengue virus activity. |
|---|---|
| ln Vitro |
Dengue virus (DENV) replication in mammalian cells is inhibited by clofenil, but not in mosquito cells[1].
Additionally, clofenil prevents the Zika virus from replicating. Cyclofenil may disrupt the translation-RNA synthesis and assembly-maturation phases of the Dengue virus (DENV) life cycle, according to a time-of-addition experiment. After treatment with clofenil, the amount of intracellular infectious particles dropped more sharply than the amount of viral RNA, suggesting that the assembly-maturation stage may be the primary target of clofenil[1]. Cyclofenil is a selective estrogen receptor modulator showing a higher affinity for ERβ than ERα. It has estrogenic properties. In Vero cells, Cyclofenil inhibits dengue virus replication with an EC50 of 1.62 μM. |
| ln Vivo |
In intact rats, the number of ERα (estrogen receptor) and ERβ (estrogen receptor)-immunoreactive (-ir) cells is counted at each stage of the estrous cycle. Furthermore, the effects of microinjecting methyl-piperidino-pyrazole (MPP) or clofenil on either side of the preoptic-anterior hypothalamic area (POA-AHA) to block ERα and ERβ on the rate of ovulation on diestrus-2 or proestrus day are assessed. In POA-AHA, the quantity of ERα-ir and ERβ-ir cells varied throughout the estrous cycle.On diestrus-2 day, the ovulation rate was decreased in rats treated with MPP on either side and with Cyclofenil on the left side of POA-AHA. On proestrus day, the ovulation rate was decreased in rats treated with MPP on either side. Progesterone and follicle stimulating hormone (FSH) increased while luteinizing hormone (LH) surge was reduced when MPP or clofenil was administered[2].
Cyclofenil is used as a gonadotropin stimulant or ovulation inducer and in menopausal hormone therapy in women. It is used to treat menstrual disturbances and anovulatory infertility. It also has anti-dengue virus activity. |
| Enzyme Assay |
Cyclofenil is evaluated in cell-free receptor binding assays to determine its affinity for estrogen receptors. Radioligand binding displacement assays are performed using membrane preparations expressing ERα and ERβ. Competition binding experiments are conducted with increasing concentrations of Cyclofenil and a fixed concentration of a labeled reference ligand.
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| Cell Assay |
Cyclofenil is assessed in cell-based assays to measure its estrogen receptor modulating activity. Cells expressing estrogen receptors are treated with Cyclofenil, and receptor activity is measured by assessing downstream signaling pathways. Its anti-dengue virus activity is assessed in Vero cells.
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| Animal Protocol |
Cyclofenil is administered in animal models to evaluate its effects on ovulation and hormone levels. However, specific animal study protocols are not extensively documented. The compound is typically formulated for in vivo administration using DMSO or other suitable vehicles.
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| ADME/Pharmacokinetics |
Cyclofenil has a molecular weight of 364.44 and a molecular formula of C23H24O4. It has a CAS number of 2624-43-3. The compound is soluble in DMSO at 3.64 mg/mL. It should be stored as a powder at -20°C for up to 3 years.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for Cyclofenil. The compound is for research use only and is not intended for human therapeutic use. Its safety profile has not been extensively characterized in the available literature.
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| References | |
| Additional Infomation |
Cyclofenil is an organic molecular entity belonging to the class of gonadal stimulants and ovulation inducers. It is used to treat infertility and amenorrhea, but its efficacy is considered less than that of clomiphene.
Cyclofenil is a selective estrogen receptor modulator. It has a CAS number of 2624-43-3. It is used as an ovulation inducer and in menopausal hormone therapy. It also has anti-dengue virus activity. It is not approved for clinical use. |
| Molecular Formula |
C23H24O4
|
|---|---|
| Molecular Weight |
364.441
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| Exact Mass |
364.167
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| Elemental Analysis |
C, 75.80; H, 6.64; O, 17.56
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| CAS # |
2624-43-3
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| Related CAS # |
5189-40-2 (diphenol);2624-43-3;
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| PubChem CID |
2898
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
509.0±30.0 °C at 760 mmHg
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| Melting Point |
133-136°C
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| Flash Point |
254.8±23.0 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.573
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| LogP |
5.9
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
27
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| Complexity |
503
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C(C([H])([H])[H])=O)C1C([H])=C([H])C(=C([H])C=1[H])/C(/C1C([H])=C([H])C(=C([H])C=1[H])OC(C([H])([H])[H])=O)=C1\C([H])([H])C([H])([H])C([H])([H])C([H])([H])C\1([H])[H]
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| InChi Key |
GVOUFPWUYJWQSK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H24O4/c1-16(24)26-21-12-8-19(9-13-21)23(18-6-4-3-5-7-18)20-10-14-22(15-11-20)27-17(2)25/h8-15H,3-7H2,1-2H3
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| Chemical Name |
4,4'-(Cyclohexylidenemethylene)diphenol diacetate ester
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| Synonyms |
Cyclofenil; H 3452; F 6066; AI3-52271
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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 |
| 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 : 21~100 mg/mL (57.62~274.39 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.86 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: 10% DMSO+90% Corn Oil: ≥ 2.5 mg/mL (6.86 mM) (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7439 mL | 13.7197 mL | 27.4394 mL | |
| 5 mM | 0.5488 mL | 2.7439 mL | 5.4879 mL | |
| 10 mM | 0.2744 mL | 1.3720 mL | 2.7439 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.
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