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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > GPCR & G Protein > RelugolixCAS：737789-87-6
Molecular Formula：C29H27F2N7O5S
Molecular Weight：623.63
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 737789-87-6 |
| Name | Relugolix |
| Molecular Formula | C29H27F2N7O5S |
| Molecular Weight | 623.63 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD25976856 |
| SMILES | O=C(NOC)NC1=CC=C(C(S2)=C(CN(C)C)C(C(N3C4=NN=C(OC)C=C4)=O)=C2N(CC5=C(F)C=CC=C5F)C3=O)C=C1 |
| Target Point | GNRH Receptor |
| Passage | GPCR & G Protein |
| Background | Relugolix is a selective gonadotropin-releasing hormone receptor (GnRHR) antagonist. |
| Biological Activity | Relugolix (TAK-385) is a potent，orally active，nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209)[1]. Relugolix is used for the study of sex-hormone-dependent diseases，such as including endometriosis，uterine fibroids and prostate cancer et al[2]. |
| IC50 | IC50: 0.33 nM (human GnRH).IC50: 0.32 nM (monkey GnRH)[2] |
| Data Literature Source | [1]. Kazuhiro Miwa，et al. Discovery of 1-{4-[1-(2，6-Difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2，4-dioxo-1，2，3，4-tetrahydrothieno[2，3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a Potent，Orally Active，Non-Peptide Antagonis [2]. Daisuke Nakata，et al. Suppression of the hypothalamic-pituitary-gonadal axis by TAK-385 (relugolix)，a novel，investigational，orally active，small molecule gonadotropin-releasing hormone (GnRH) antagonist: studies in human GnRH receptor knock-in mice. E |
| Unit | Bottle |
| Specification | 5mg 10mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
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