| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
GnRH receptor (Gonadotropin-releasing hormone receptor).
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| ln Vitro |
Acyline competitively binds to the GnRH receptor on pituitary gonadotropes without activating it. By blocking endogenous GnRH signaling, it inhibits the synthesis and release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to a rapid and sustained suppression of sex steroid production (testosterone in males, estradiol in females).
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| ln Vivo |
Acyline (50 μg, sc, twice daily, 5 days) TFA disrupted vaginal estrus, decreased uterine weight, and increased luteinizing hormone concentrations in female rats that were Kiss1−/− and Gpr54−/−. decrease[1]. Acyline (50 μg, sc, once) TFA lowers the amounts of follicle-stimulating growth hormone in male Kiss1−/− and Gpr54−/− cells.
In male Kiss1-/- and Gpr54-/- mice, Acyline (50 ug, sc, once) reduces levels of follicle-stimulating hormone. In female mice, it disrupts vaginal estrus and reduces uterine weights. It also decreases luteinizing hormone (LH) concentrations, demonstrating its potent anti-gonadal effects in vivo. |
| Enzyme Assay |
A direct receptor binding assay is performed using membrane preparations from pituitary cells expressing the GnRH receptor. The membranes are incubated with a labeled GnRH agonist (e.g., [125I]-Buserelin) and increasing concentrations of unlabeled Acyline. Bound ligand is separated by filtration, and the IC50/Ki is calculated from the competition curve.
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| Cell Assay |
Primary cultures of rat pituitary cells are seeded in 24-well plates. The cells are pre-incubated with Acyline for 2 hours, then stimulated with GnRH. After incubation, the culture medium is collected, and the concentration of luteinizing hormone (LH) is measured by radioimmunoassay (RIA) or ELISA to determine the extent of GnRH antagonism.
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| Animal Protocol |
Animal/Disease Models: Female Kiss1−/−and Gpr54−/− mice[1]
Doses: 50 μg (1 mg/mL in PBS) Route of Administration: subcutaneous (sc) injection; twice (two times) daily; 5 days Experimental Results: 12 Kiss1−/− mice left oestrus within 4 days of 13 mice received acyline while only 2 of 17 mice received vehicle left oestrus. Also, 7 of 8 Gpr54−/− mice received acyline left oestrus compared to 1 of 7 received vehicle. decreased uterine weights of Kiss1−/−and Gpr54 −/− mice in treated group compared to the vehicle group, and decreased serum LH concentrations in Kiss1−/− mice. Adult male rats are housed individually and receive subcutaneous (SC) injections of Acyline TFA (e.g., 50 ug, twice daily) for 5 days. Blood samples are collected via tail vein at baseline and various time points post-dosing. Serum is separated, and serum LH, FSH, and testosterone levels are measured by ELISA. |
| ADME/Pharmacokinetics |
Specific PK parameters for Acyline are not published. As a synthetic GnRH analog, it is more stable than native GnRH but still has a relatively short half-life in circulation (hours). It is administered via injection (subcutaneous or intramuscular) and is designed to resist rapid degradation by peptidases.
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| Toxicity/Toxicokinetics |
No formal toxicology studies are reported for this research compound. At high doses or with chronic use, the sustained suppression of sex hormones can lead to hypogonadism, including loss of libido, infertility, and bone mineral density loss. This product is for research use only and not approved for human therapy.
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| References | |
| Additional Infomation |
Acyline is a third-generation GnRH antagonist. It is characterized by high water solubility and low histamine release, which reduces the risk of allergic reactions compared to earlier antagonists. It is used as a research tool to achieve rapid, reversible chemical castration in animal models, allowing the study of hormone-dependent physiological and pathological processes (e.g., prostate cancer, endometriosis) without surgical removal of the gonads.
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| Molecular Formula |
C82H103CLF3N15O16
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|---|---|
| Molecular Weight |
1647.23
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| Related CAS # |
Acyline;170157-13-8
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| Appearance |
White to off-white solid powder
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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 (~60.71 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (1.52 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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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: ≥ 2.5 mg/mL (1.52 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 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.6071 mL | 3.0354 mL | 6.0708 mL | |
| 5 mM | 0.1214 mL | 0.6071 mL | 1.2142 mL | |
| 10 mM | 0.0607 mL | 0.3035 mL | 0.6071 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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