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Relugolix (RVT-601) 是口服有活性的非肽性促性腺激素释放激素的拮抗剂。同 TAK-013 相比,它对人和猴子的受体具有高亲和力和强拮抗活性,它们的 IC50值分别为0.33 nM 和0.32 nM。它可用于研究性激素依赖性疾病,如子宫肌瘤、子宫内膜异位症、前列腺癌等。
Relugolix (RVT-601) 是口服有活性的非肽性促性腺激素释放激素的拮抗剂。同 TAK-013 相比,它对人和猴子的受体具有高亲和力和强拮抗活性,它们的 IC50值分别为0.33 nM 和0.32 nM。它可用于研究性激素依赖性疾病,如子宫肌瘤、子宫内膜异位症、前列腺癌等。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 251 | 现货 | |
5 mg | ¥ 557 | 现货 | |
10 mg | ¥ 797 | 现货 | |
25 mg | ¥ 1,430 | 现货 | |
50 mg | ¥ 2,310 | 现货 | |
100 mg | ¥ 3,470 | 现货 | |
500 mg | ¥ 7,580 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 768 | 现货 |
产品描述 | Relugolix (RVT-601) is an orally available, non-peptide gonadotropin-releasing hormone (GnRH or luteinizing hormone-releasing hormone (LHRH)) antagonist, with potential antineoplastic activity. Relugolix competitively binds to and blocks the GnRH receptor in the anterior pituitary gland, which both prevents GnRH binding to the GnRH receptor and inhibits the secretion and release of both luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone from Leydig cells in the testes. Since testosterone is required to sustain prostate growth, reducing testosterone levels may inhibit hormone-dependent prostate cancer cell proliferation. |
靶点活性 | TNK2 (D163E mutations):38nM, TNK2 (R806Q mutations):113 nM |
别名 | 瑞卢戈利, TAK-385, RVT-601 |
分子量 | 623.63 |
分子式 | C29H27F2N7O5S |
CAS No. | 737789-87-6 |
Smiles | CONC(=O)Nc1ccc(cc1)-c1sc2n(Cc3c(F)cccc3F)c(=O)n(-c3ccc(OC)nn3)c(=O)c2c1CN(C)C |
密度 | 1.442 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 50 mg/mL (80.18 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
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