Kisspeptin-10, human TFA is a potent vasoconstrictor and inhibitor of angiogenesis, it acts as a tumor metastasis suppressor via its receptor GPR54. Kisspeptin-10/GPR54 signaling induces osteoblast differentiation via NFATc4-mediated BMP2 expression. Kisspeptin-10 (KP-10) and its receptor GPR54 are key components in the regulation of GnRH secretion in humans and other mammals. Kisspeptin-10 protein binds to GPR54. Activation of Kisspeptin-10 suppresses pulmonary human melanoma and Kisspeptin-10 is a metastasis suppressor in breast cancer cells.
In vivo, intravenous infusion of kisspeptin-10 (7.5, 35, and 100 nM) induces a dose-dependent increase in LH secretion. The stimulatory effect of kisspeptin-10 (100 n nM) on LH secretion is blocked by the GnRH antagonist cetrorelix, precluding a singular action on gonadotropes. Kisspeptin-10 inhibits angiogenesis in vivo. Kp-10 inhibits tumor growth in SCID mice xenografted with human prostate cancer cells (PC-3) through inhibiting tumor angiogenesis.
| Molecular Weight | 1416.46 |
| Formula | C63H83N17O14.C2HF3O2 |
| CAS Number | 374675-21-5 (free base) |
| Solubility (25°C) | DMSO 80 mg/mL |
| 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.
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