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| CAS:934246-14-7:Degarelix acetate hydrate | |
| Degarelix is a new‑generation long‑acting GnRH receptor antagonist with significantly improved receptor affinity and metabolic stability via multiple unnatural amino acid modifications. It binds GnRH receptors in the pituitary with high affinity, rapidly and sustainably suppresses the secretion of LH, FSH and testosterone/estradiol, with no initial flare‑up effect. It rapidly achieves castration levels after administration and maintains them long‑term. The acetate hydrate formulation forms a subcutaneous drug depot after injection and releases slowly to achieve a long‑acting effect of 1‑3 months. Applied in mechanism research of sex hormone‑dependent diseases such as prostate cancer and endometriosis, as well as long‑acting peptide formulation development. | |
| 95%/98%/99% | |
| 1632.26, higher for acetate hydrate | |
| Function Tags (comma-separated) | ||||||||
| Long-acting GnRH antagonism,Rapid castration,No flare-up effect,Prostate cancer study,Subcutaneous depot sustained release,Sex hormone suppression | 1631.75 | 1632.26 (free peptide) | 10 |
| Long-term Storage Conditions | Short-term Storage Conditions | ||||
| PEP-DEG001 | Store at -20℃, sealed, dry & protected from light, aliquoted; avoid high temperature and humidity | Stable for 2 months at 2-8℃ sealed & dry; avoid freeze-thaw and high temperature | Stable for 7 days at 4℃; suspensions must be prepared freshly before use. Limited water solubility, forming suspension in water for injection. D-amino acids and side-chain modifications significantly enhance enzymatic resistance. Hydrate crystal is stable | Stable for 3 years at -20℃ under dry & dark conditions |
| Applicable Research Areas (comma-separated) | ||||
| PEP-DEG001 | Long-acting GnRH antagonist that rapidly and sustainably inhibits gonadotropins with no flare-up, achieving long-term castration via subcutaneous depot | Degarelix optimizes the binding mode with GnRH receptors through multiple hydrophobic and polar modifications, binds pituitary GnRH receptors with high affinity and competitiveness, completely blocks endogenous GnRH signal transduction. It rapidly inhibits LH and testosterone secretion within 24-72 hours after administration to reach castration levels, without the initial testosterone elevation flare-up common with GnRH agonists. After subcutaneous injection, its acetate hydrate formulation forms a micro-precipitation drug depot at the injection site, releases drug continuously via slow dissolution, and achieves a long-acting inhibitory effect of weeks to months. The drug effect is reversible, and pituitary-gonadal axis function gradually recovers after discontinuation. It is one of the core drugs for endocrine therapy of prostate cancer. | Prostate cancer study,Endometriosis research,Sex hormone-dependent tumors,Pituitary-gonadal axis regulation,Long-acting formulation R&D,GnRH pathway study | Gonadotropin-Releasing Hormone Receptor (GnRHR); Sustained gonadotropin secretion inhibitory pathway; Subcutaneous depot long-acting release pathway |
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