A GnRHR antagonist (IC50s = 0.33 and 0.32 nM for the human and monkey receptors

TAK-385 – 1 mg

Brand:
Cayman
CAS:
737789-87-6
Storage:
-20
UN-No:
Non-Hazardous - /

TAK-385 is an orally bioavailable gonadotropin-releasing hormone receptor (GnRHR) antagonist (IC50s = 0.33 and 0.32 nM for the human and monkey receptors, respectively).{49487} It is selective for these receptors over the rat GnRHR receptor (IC50 = 9,800 nM), as well as a panel of 134 enzymes and receptors at 10 µM. TAK-385 is 95-fold more potent at inhibiting GnRH-induced arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607) release in CHO cells expressing human GnRHR compared with those expressing monkey GnRHR. It decreases testis, ventral prostate, ovary, and uterus weight in human GNRHR knock-in mice when administered at doses ranging from 3 to 200 mg/kg per day for 28 days.{49488} TAK-385 (1 and 3 mg/kg) also decreases plasma luteinizing hormone levels in castrated cynomolgus monkeys.{49487}  

 

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SKU: 29512 - 1 mg Category:

Description

A GnRHR antagonist (IC50s = 0.33 and 0.32 nM for the human and monkey receptors, respectively); selective for these receptors over the rat GnRHR receptor (IC50 = 9,800 nM), as well as a panel of 134 enzymes and receptors at 10 µM; 95-fold more potent at inhibiting GnRH-induced arachidonic acid release in CHO cells expressing human GnRHR compared with those expressing monkey GnRHR; decreases testis, ventral prostate, ovary, and uterus weight in human GNRHR knock-in mice at 3-200 mg/kg per day for 28 days; decreases plasma luteinizing hormone levels in castrated cynomolgus monkeys at 1 and 3 mg/kg

Formal name: N-[4-[1-[(2,6-difluorophenyl)methyl]-5-[(dimethylamino)methyl]-1,2,3,4-tetrahydro-3-(6-methoxy-3-pyridazinyl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-N-methoxy-urea

Synonyms:  Relugolix

Molecular weight: 623.6

CAS: 737789-87-6

Purity: ≥98%

Formulation: A crystalline solid

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