TAK-683 TFA;
TAK-683 TFA 是一种有效的完全 KISS1R 激动剂 (IC50=170 pM)，具有改善的代谢稳定性。TAK-683 TFA 是一个九肽 metastin 的类似物，对 KISS1R 具有激动作用，针对人与大鼠 EC50 值分别为 0.96 nM 和 1.6 nM。 TAK-683 TFA 消耗下丘脑 GnRH，降低血浆 FSH、LH、睾酮水平，具有研究激素依赖性前列腺癌的潜力。
TAK-683 TFA Chemical Structure
| 规格 | 是否有货 | ||
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| 100 mg | ; | 询价 | ; |
| 250 mg | ; | 询价 | ; |
| 500 mg | ; | 询价 | ; |
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TAK-683 TFA 的其他形式现货产品:
| 生物活性 |
TAK-683 TFA is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 TFA is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively[1]. TAK-683 TFA depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer[1][2][3]. |
IC50 Target |
IC50: 170 pM (metastin/GPR54)[1] |
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| 体内研究 (In Vivo) |
TAK-683 (subcutaneous injection; 0.008, 0.08, 0.8, or 8 μmol/ml/kg; once daily; 7 days) induces an increase in plasma luteinizing hormone and testosterone levels; however, after day 7, plasma hormone levels and genital organ weights are reduced[1].TAK-683 (subcutaneous injection; 10, 30, or 100 pmol/h; once daily; 4 weeks) provides a promising for suppressing reproductive functions and hormone-related diseases such as prostate cancer[1].TAK-683 (subcutaneous injection; 2.1-21 nmol/kg/day; once daily; 12 weeks) has a longer-term evaluation in prostate cancer model, serum concentrations of PSA is reduced in rats, PSA concentrations are reduced to below the limit of detection (0.5 ng/ml)) in all rats by day 14[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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| 分子量 |
1412.47 |
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| Formula |
C66H84F3N17O15 |
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| Sequence Shortening |
N-Acetyl-YWNTF{aza}L{Met-R}W-NH2 |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis. |
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| 参考文献 |
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