| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 1g | |||
| Other Sizes |
| Targets |
Linzagolix choline targets the gonadotropin-releasing hormone (GnRH) receptor, a G protein-coupled receptor located on pituitary gonadotropes. As a non-peptide antagonist, it binds to the GnRH receptor and blocks the binding of endogenous GnRH. This prevents the receptor from activating its downstream signaling pathway, which is responsible for the synthesis and release of LH and FSH. By inhibiting the release of these gonadotropins, Linzagolix choline effectively reduces the production of sex hormones, such as estrogen and progesterone, from the ovaries.
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| ln Vitro |
In vitro, Linzagolix choline demonstrates potent antagonism of the GnRH receptor. Its activity is assessed by measuring its ability to inhibit GnRH-stimulated signaling in cells expressing the receptor. Detailed IC₅₀ values for receptor antagonism are not extensively reported in the available literature. Its activity is confirmed through functional assays measuring the inhibition of LH and FSH release from pituitary cells in response to GnRH stimulation.
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| ln Vivo |
In vivo, Linzagolix choline is an orally active GnRH antagonist. By inhibiting the release of gonadotropins and reducing sex hormone production, it can be used to study sex hormone-dependent diseases such as endometriosis and uterine fibroids. Its oral activity makes it a practical tool for investigating the effects of GnRH antagonism in animal models and for developing new therapeutic strategies for these conditions.
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| Enzyme Assay |
Non-cell-based receptor binding assays for Linzagolix choline involve radioligand binding studies using membrane preparations from cells expressing the human GnRH receptor. The receptor is incubated with a radiolabeled GnRH ligand and varying concentrations of Linzagolix choline. Its binding affinity (Ki) is determined by measuring the displacement of the radiolabeled ligand. IC₅₀ values for receptor antagonism are determined from functional assays measuring GnRH-stimulated signaling.
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| Cell Assay |
Cellular assays for Linzagolix choline are performed using cells expressing the GnRH receptor. Cells are treated with the compound at various concentrations, followed by stimulation with GnRH. Downstream signaling, such as calcium mobilization or the release of LH and FSH, is measured. The compound's ability to inhibit GnRH-stimulated signaling is quantified. IC₅₀ values for receptor antagonism are determined from dose-response curves.
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| Animal Protocol |
In vivo animal models for Linzagolix choline include models of endometriosis and uterine fibroids. The compound is administered orally at various doses. Efficacy is assessed by measuring the reduction in lesion size (for endometriosis) or tumor volume (for uterine fibroids), as well as serum LH, FSH, and sex hormone levels. These studies confirm the compound's in vivo efficacy and its mechanism of action.
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| ADME/Pharmacokinetics |
Linzagolix choline has a molecular weight of 611.59 g/mol and a molecular formula of C₂₇H₂₈F₃N₃O₈S. Its CAS number is 1321816-57-2. The compound is supplied as a solid with a purity of >98%. It is soluble in DMSO. Storage conditions: -20°C. The compound is an orally available non-peptide GnRH antagonist. Detailed pharmacokinetic parameters such as half-life and bioavailability are not extensively reported.
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| Toxicity/Toxicokinetics |
Detailed toxicological data for Linzagolix choline are not extensively reported in the available literature. As a research compound, its safety profile would need to be established through standard preclinical toxicity assessments. The compound is intended for research use only and is not for human consumption. Standard laboratory safety precautions should be followed when handling the compound.
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| References | |
| Additional Infomation |
See also: Linzagolix (with active ingredient).
Drug Indications Yselty is indicated for the treatment of moderate to severe uterine fibroids in adult women of reproductive age. Linzagolix choline is also known as KLH-2109 choline. It is a non-peptide gonadotropin-releasing hormone (GnRH) antagonist with oral activity. It inhibits the release of LH and FSH by binding to the GnRH receptor in the pituitary gland. Linzagolix choline can be used in the study of sex hormone-dependent diseases such as endometriosis and uterine fibroids. Its CAS number is 1321816-57-2. |
| Molecular Formula |
C27H28F3N3O8S
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|---|---|
| Molecular Weight |
611.59
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| Exact Mass |
611.154
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| CAS # |
1321816-57-2
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| Related CAS # |
935283-04-8 (free);1321816-57-2 (choline);
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| PubChem CID |
53357800
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
42
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| Complexity |
867
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
IAIVRTFCYOGNBW-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C22H15F3N2O7S.C5H14NO/c1-32-14-4-3-10(23)18(25)9(14)7-34-16-6-13(11(24)5-15(16)33-2)27-20(28)17-12(26-22(27)31)8-35-19(17)21(29)30;1-6(2,3)4-5-7/h3-6,8H,7H2,1-2H3,(H,26,31)(H,29,30);7H,4-5H2,1-3H3/q;+1/p-1
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| Chemical Name |
3-[5-[(2,3-difluoro-6-methoxyphenyl)methoxy]-2-fluoro-4-methoxyphenyl]-2,4-dioxo-1H-thieno[3,4-d]pyrimidine-5-carboxylate;2-hydroxyethyl(trimethyl)azanium
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 1.6351 mL | 8.1754 mL | 16.3508 mL | |
| 5 mM | 0.3270 mL | 1.6351 mL | 3.2702 mL | |
| 10 mM | 0.1635 mL | 0.8175 mL | 1.6351 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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