TAK-385, CAS 737789-87-6

Formulation: A crystalline solid

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

Purity: ≥98%

Formula Markup: C29H27F2N7O5S

Formula Weight: 623,6

Shelf life (days): 1460

CAS Number: 737789-87-6

Notes: 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}

• Artikelnummer: CAY29512-1
• Hersteller: Cayman Chemical
• Hersteller Artikelnummer: 29512-1
• Green Labware: Nein
• Verpackungseinheit: 1 mg
• Mengeneinheit: STK