生物活性
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.
化学数据
| 分子量 | 1416.46 |
| 分子式 | C63H83N17O14.C2HF3O2 |
| CAS号 | 374675-21-5 (free base) |
| 纯度 | >98% |
| 溶解性（25°C） | DMSO 80 mg/mL |
| 储存和运输条件 | 固体粉末： -20°C 冷藏长期储存
常温运输及临时存放 |
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 0.706 mL | 3.5299 mL | 7.0599 mL |
| 5 mM | 0.1412 mL | 0.706 mL | 1.412 mL |
| 10 mM | 0.0706 mL | 0.353 mL | 0.706 mL |
