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| 5mg |
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| 10mg |
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| Targets |
Antide targets the gonadotropin-releasing hormone receptor (GnRHR), a G-protein coupled receptor expressed on pituitary gonadotrophs. By binding to this receptor, Antide competitively inhibits the action of endogenous GnRH, thereby blocking the secretion of LH and FSH. This mechanism makes it valuable for studying hormone-dependent processes.
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| ln Vitro |
In vitro, Antide demonstrates high affinity binding to the GnRH receptor, effectively competing with endogenous GnRH. It inhibits LH and FSH release from cultured pituitary cells in a concentration-dependent manner. The compound shows potent anti-ovulatory activity in various in vitro models of reproductive endocrinology.
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| ln Vivo |
In mature male rats and cynomolgus monkeys, subcutaneous injection of antipeptides (1, 3, 6, 10, and 15 mg/kg) once or for five consecutive days causes long-term chemical castration [1].
In vivo, Antide displays potent anti-ovulatory activity and can create a reversible chemical castration model in preclinical studies. It suppresses gonadotropin secretion and reduces circulating sex steroid levels. Its effects are reversible upon discontinuation of treatment, making it useful for studying gonadal steroid function without surgical intervention. |
| Enzyme Assay |
Receptor binding assays for Antide typically use membrane preparations from cells expressing the GnRH receptor. Radiolabeled GnRH or a GnRH analog is incubated with varying concentrations of Antide, and binding affinity is determined by competition binding curves. IC₅0 or Kᵢ values are calculated from displacement data.
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| Cell Assay |
Cellular assays for Antide utilize primary pituitary cell cultures or immortalized gonadotrope cell lines. Cells are treated with Antide in the presence of GnRH stimulation, and LH and FSH secretion into the culture medium is measured by radioimmunoassay or ELISA. Inhibition of hormone release is quantified relative to controls.
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| Animal Protocol |
Animal/Disease Models: cynomolgus monkey and rat [1]
Doses: 1, 3, 6, 10 and 15 mg/kg Route of Administration: subcutaneous injection, once or for 5 days Experimental Results: Dose-dependent inhibition of serum LH concentration (rats only) and testosterone and testicular, prostate, and seminal vesicle weights. Long-lasting castration-like effects were achieved in rats over a concentration range of 6 (less than or equal to 8 weeks) to 15 mg/kg (greater than 8 weeks). Long-term inhibition was induced at a dose of only 15 mg/kg and lasted only 2-3 weeks in cynomolgus monkeys. In vivo studies with Antide are typically conducted in rodent or primate models. The peptide is administered via subcutaneous or intraperitoneal injection. Effects on ovulation are assessed by examining ovarian histology or measuring serum LH, FSH, and sex steroid levels. Antide is used to study reproductive endocrinology and hormone-dependent cancers. |
| ADME/Pharmacokinetics |
As a peptide, Antide has a relatively short half-life in circulation due to proteolytic degradation. The compound is supplied as a lyophilized powder and should be stored under appropriate conditions to maintain stability. Its pharmacokinetic properties may be influenced by formulation and route of administration.
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| Toxicity/Toxicokinetics |
Toxicity data for Antide indicate weak histamine release activity. At therapeutic doses, it is generally well-tolerated. However, as with all peptide receptor antagonists, potential side effects related to hormone suppression should be considered. Standard safety precautions for laboratory use apply.
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| References | |
| Additional Infomation |
Antide is a research compound not approved for clinical use. It is used primarily in reproductive endocrinology research, including studies of hormone-dependent cancers such as prostate and breast cancer, endometriosis, and uterine leiomyoma. Synonyms include Iturelix, ORF 23541, and Nal-Lys-GnRH antagonist. The molecular formula is C₈2H10₈ClN1₇O14.
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| Molecular Formula |
C82H108N17O14CL
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|---|---|
| Molecular Weight |
1591.29342
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| Exact Mass |
1589.795
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| CAS # |
112568-12-4
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| PubChem CID |
16130938
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
1798.0±65.0 °C at 760 mmHg
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| Flash Point |
1041.2±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.593
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| LogP |
4.91
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| Hydrogen Bond Donor Count |
14
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| Hydrogen Bond Acceptor Count |
18
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| Rotatable Bond Count |
46
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| Heavy Atom Count |
114
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| Complexity |
3110
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| Defined Atom Stereocenter Count |
10
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| SMILES |
ClC1=CC=C(C=C1)C[C@H](C(N[C@H](CC1=CN=CC=C1)C(N[C@@H](CO)C(N[C@@H](CCCCNC(C1=CN=CC=C1)=O)C(N[C@H](CCCCNC(C1=CN=CC=C1)=O)C(N[C@@H](CC(C)C)C(N[C@@H](CCCCNC(C)C)C(N1CCC[C@H]1C(N[C@@H](C(N)=O)C)=O)=O)=O)=O)=O)=O)=O)=O)NC([C@@H](CC1C=CC2=CC=CC=C2C=1)NC(C)=O)=O
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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) |
H2O : ~10 mg/mL (~6.28 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 | 0.6284 mL | 3.1421 mL | 6.2842 mL | |
| 5 mM | 0.1257 mL | 0.6284 mL | 1.2568 mL | |
| 10 mM | 0.0628 mL | 0.3142 mL | 0.6284 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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