| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Lecirelin targets the gonadotropin-releasing hormone (GnRH) receptor on the anterior pituitary gland. As a GnRH agonist, it binds to and activates the GnRH receptor, stimulating the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH). This leads to increased production of sex hormones, including estrogen and progesterone in females and testosterone in males. The compound's effects on the hypothalamic-pituitary-gonadal axis make it useful for the management of reproductive disorders in animals. Lecirelin is a synthetic peptide analog of the natural GnRH, with modifications that enhance its stability and biological activity.
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| ln Vitro |
The tone and frequency of contraction of preovulatory follicles (PF), small follicular cysts (FC-S), and large follicular cysts (FC-L) are dramatically increased by lecirelin (2.07 μM) [1]. Preovulatory follicle strips contract much more when lecirelin is administered than when cyst strips shrink [1].
In vitro studies have demonstrated that Lecirelin binds to the GnRH receptor on pituitary cells and stimulates the release of FSH and LH. The compound's affinity for the GnRH receptor and its ability to activate receptor signaling have been characterized using radioligand binding assays and cell-based reporter systems. Lecirelin is a potent GnRH agonist, and its in vitro activity is comparable to that of natural GnRH. The compound's stability and resistance to enzymatic degradation have also been studied, as these properties are important for its in vivo efficacy. |
| ln Vivo |
In vivo studies have demonstrated that Lecirelin effectively stimulates the release of FSH and LH and induces ovulation in animals. In veterinary practice, Lecirelin is used for the treatment of ovarian cysts, induction of ovulation, and synchronization of estrus in cattle, horses, and other animals. The compound is administered by intramuscular or intravenous injection and produces rapid effects on reproductive hormone levels. Clinical studies have shown that Lecirelin is effective in improving reproductive performance in animals with various reproductive disorders. The compound is widely used in veterinary medicine and is available in various formulations for different animal species.
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| Enzyme Assay |
The in vitro receptor binding assay for Lecirelin typically involves measuring the compound's affinity for the GnRH receptor using radioligand binding techniques. Membrane preparations from cells expressing the GnRH receptor are incubated with a radiolabeled GnRH analog and varying concentrations of Lecirelin. Nonspecific binding is determined in the presence of excess unlabeled ligand. The compound's affinity (Ki value) for the GnRH receptor is calculated from competition binding experiments. Cell-based functional assays are also used to measure the compound's ability to activate GnRH receptor signaling and stimulate FSH and LH release.
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| Cell Assay |
Cellular assays for Lecirelin are conducted using pituitary cell lines or primary pituitary cells that express the GnRH receptor. Cells are treated with varying concentrations of Lecirelin, and the release of FSH and LH is measured using immunoassays. The compound's potency (EC50) for stimulating hormone release is determined from dose-response curves. Receptor activation can also be assessed by measuring downstream signaling pathways, such as calcium mobilization or MAP kinase activation. These cell-based assays confirm the compound's activity as a GnRH agonist and provide information about its potency and efficacy.
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| Animal Protocol |
In vivo animal studies for Lecirelin are conducted in cattle, horses, and other animals. The compound is administered by intramuscular or intravenous injection, and its effects on reproductive hormone levels and reproductive function are assessed. In cattle, Lecirelin is used for the treatment of ovarian cysts and for the synchronization of estrus. Blood samples are collected to measure FSH, LH, and progesterone levels. Ovulation is confirmed by ultrasound or by monitoring estrus behavior. These studies confirm the compound's efficacy in veterinary applications and help to determine the optimal dose and treatment regimen.
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| ADME/Pharmacokinetics |
Lecirelin is administered by intramuscular or intravenous injection. The compound is rapidly absorbed and has a short half-life in the circulation. The time to peak effect on LH release is approximately 30-60 minutes after injection. Lecirelin is metabolized by peptidases and is cleared from the circulation within a few hours. The compound's pharmacokinetics are similar to those of natural GnRH. The compound is typically administered as a single injection or as part of a treatment regimen for reproductive disorders. The dose and route of administration depend on the animal species and the specific indication.
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| Toxicity/Toxicokinetics |
Toxicological data for Lecirelin indicate that the compound is well-tolerated in animals at therapeutic doses. As a peptide hormone analog, Lecirelin has a low potential for toxicity, and adverse effects are rare. The compound may cause transient changes in reproductive hormone levels, which are the intended pharmacological effects. No significant toxicity has been reported with the use of Lecirelin in veterinary medicine. Standard safety precautions should be followed when handling the compound, and it should be used only as directed by a veterinarian.
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| References | |
| Additional Infomation |
Lecirelin is a synthetic GnRH analog used in veterinary medicine for the treatment of reproductive disorders in animals. It functions as a GnRH agonist, stimulating the release of FSH and LH and promoting ovulation. The compound has a molecular formula of C59H79N17O12 and a molecular weight of approximately 1194.37. Lecirelin is administered by injection and is available in various formulations for use in cattle, horses, and other animals. It is an important tool for the management of reproductive disorders in veterinary practice. The compound is available by prescription only and should be used under the supervision of a veterinarian.
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| Molecular Formula |
C59H84N16O12
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| Molecular Weight |
1209.3983
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| Exact Mass |
1208.645
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| CAS # |
61012-19-9
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| PubChem CID |
66577115
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.678
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| LogP |
0.23
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| Hydrogen Bond Donor Count |
15
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
31
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| Heavy Atom Count |
87
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| Complexity |
2420
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| Defined Atom Stereocenter Count |
9
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| SMILES |
CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](C(C)(C)C)NC(=O)[C@H](CC2=CC=C(C=C2)O)NC(=O)[C@H](CO)NC(=O)[C@H](CC3=CNC4=CC=CC=C43)NC(=O)[C@H](CC5=CN=CN5)NC(=O)[C@@H]6CCC(=O)N6
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| InChi Key |
XJWIEWPGHRSZJM-MGZASHDBSA-N
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| InChi Code |
InChI=1S/C59H84N16O12/c1-7-63-55(85)46-15-11-23-75(46)57(87)40(14-10-22-64-58(60)61)68-50(80)41(24-32(2)3)72-56(86)48(59(4,5)6)74-53(83)42(25-33-16-18-36(77)19-17-33)69-54(84)45(30-76)73-51(81)43(26-34-28-65-38-13-9-8-12-37(34)38)70-52(82)44(27-35-29-62-31-66-35)71-49(79)39-20-21-47(78)67-39/h8-9,12-13,16-19,28-29,31-32,39-46,48,65,76-77H,7,10-11,14-15,20-27,30H2,1-6H3,(H,62,66)(H,63,85)(H,67,78)(H,68,80)(H,69,84)(H,70,82)(H,71,79)(H,72,86)(H,73,81)(H,74,83)(H4,60,61,64)/t39-,40-,41-,42-,43-,44-,45-,46-,48-/m0/s1
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| Chemical Name |
(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-5-(diaminomethylideneamino)-1-[(2S)-2-(ethylcarbamoyl)pyrrolidin-1-yl]-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3,3-dimethyl-1-oxobutan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
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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, avoid exposure to moisture. |
| 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) |
H2O : ~25 mg/mL (~20.67 mM)
DMSO : ~12.1 mg/mL (~10.00 mM) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.8269 mL | 4.1343 mL | 8.2686 mL | |
| 5 mM | 0.1654 mL | 0.8269 mL | 1.6537 mL | |
| 10 mM | 0.0827 mL | 0.4134 mL | 0.8269 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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