Histrelin is a nonapeptide analog of GnRH (gonadotropin-releasing hormone) with added potency. When present in the bloodstream, it can act on gonadotropes. Histrelin can stimulate these cells to release luteinizing hormone and follicle-stimulating hormone. Histrelin is considered a GnRH agonist. Histrelin acetate is used as a subcutaneous hydrogel implant for the treatment of prostate cancer and for the suppression of gonadal sex hormone production in children with central precocious puberty.
| Molecular Weight | 1383.58 |
| Formula | C66H86N18O12.XC2H4O2 |
| CAS Number | 220810-26-4 |
| Solubility (25°C) | Water |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related LHRH/GnRH Products |
|---|
| Kisspeptin-54(human)
Kisspeptin-54(human) (Metastin(human)) is an endogenous ligand for kisspeptin receptor (KISS1, GPR54). |
| Luteinizing Hormone Releasing Hormone (LH-RH), salmon
Luteinizing Hormone Releasing Hormone (LH-RH), salmon (Salmon GnRH) is the hypophysiotropic decapeptide synthesized in the hypothalamus that plays a crucial role in the control of reproductive functions. |
| Phoenixin-14
Phoenixin-14 (PNX-14) is one of the endogenous active isoform, and generates anxiolytic effect via the activation of the AHA GnRH system in mice. |
| LGnRH-III, lamprey
LGnRH-III, lamprey, an isoform of GnRH isolated from the sea lamprey, is a weak GnRH agonist with antitumor activities. |
| (D-Trp6)-LHRH free acid
(D-Trp6)-LHRH free acid is a luteinizing hormone-releasing hormone (LHRH) agonist. |
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