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GnRH-R antagonist 1
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Catalog No. T72492Cas No. 2826273-90-7
GnRH-R antagonist 1 (Compound 21a), is an orally active, membrane-permeable agent with a high binding affinity (IC50=0.57 nM) and potent in vitro antagonistic efficacy (IC50=2.18 nM). It is utilized in research focused on advanced prostate cancer and the prevention of premature LH surges [1].
GnRH-R antagonist 1
😃Good
Catalog No. T72492Cas No. 2826273-90-7
GnRH-R antagonist 1 (Compound 21a), is an orally active, membrane-permeable agent with a high binding affinity (IC50=0.57 nM) and potent in vitro antagonistic efficacy (IC50=2.18 nM). It is utilized in research focused on advanced prostate cancer and the prevention of premature LH surges [1].
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 25 mg | $2,420 | 10-14 weeks | |
| 50 mg | $3,180 | 10-14 weeks | |
| 100 mg | $4,300 | 10-14 weeks |
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Relugolix
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Relugolix (RVT-601) is an orally available, non-peptide gonadotropin-releasing hormone (GnRH or luteinizing hormone-releasing hormone (LHRH)) antagonist, with potential antineoplastic activity. Relugolix competitively binds to and blocks the GnRH receptor in the anterior pituitary gland, which both prevents GnRH binding to the GnRH receptor and inhibits the secretion and release of both luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone from Leydig cells in the testes. Since testosterone is required to sustain prostate growth, reducing testosterone levels may inhibit hormone-dependent prostate cancer cell proliferation.
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LGnRH-III, lamprey acetate(147859-97-0 free base)
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Deslorelin acetate(57773-65-6 free base)
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Histrelin acetate
Histrelin acetate(76712-82-8 free base)
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Nafarelin acetate(76932-56-4 free base)
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Product Introduction
Bioactivity
Chemical Properties
| Description | GnRH-R antagonist 1 (Compound 21a), is an orally active, membrane-permeable agent with a high binding affinity (IC50=0.57 nM) and potent in vitro antagonistic efficacy (IC50=2.18 nM). It is utilized in research focused on advanced prostate cancer and the prevention of premature LH surges [1]. |
| In vitro | GnRH-R antagonist 1 demonstrates a cell permeability that is 140 times greater than that of Relugolix, while also showing favorable stability in both human and mouse microsomes [1]. |
| In vivo | GnRH-R antagonist 1 administered orally at a dosage of 30 mg/kg once daily for seven days exhibits a good safety profile [1]. At a single oral dose of 12 mg/kg, it demonstrates favorable pharmacokinetics and high oral bioavailability, evident from a 44.7% F% value [1]. Furthermore, this dosage effectively suppresses circulating testosterone levels in rats for over 24 hours [1]. |
| Molecular Weight | 721.65 |
| Formula | C31H28F5N7O6S |
| Cas No. | 2826273-90-7 |
Storage & Solubility Information
| Storage | Shipping with blue ice. |
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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