Goserelin (acetate)

Goserelin is a synthetic gonadotropin-releasing hormone (GNRH) agonist that binds to the GNRH receptor (GNRHR, Ki = 1.6 nM, in CHO cells expressing the human receptor). It binds to mouse pituitary alphaT3-1 cells and human placenta (Kds = 2 and 580 nM, respectively) and increases intracellular calcium in alphaT3-1 cells. Goserelin induces testosterone production in vitro within 4 h in rat Leydig cells (ED50 = 83 nM) but decreases testosterone plasma level in vivo in rats over a period of 2 to 24 weeks. It inhibits tumor growth in a DU145 human prostate carcinoma mouse xenograft model when administered at a dose of 100 µg per day. Formulations containing goserelin have been used in the treatment of hormone-dependent breast and prostate cancers, as well as endometriosis and uterine fibroids.Formal Name: 2-(aminocarbonyl)hydrazide-6-[O-(1,1-dimethylethyl)-D-serine]-1-9-luteinizing hormone-releasing factor (swine), acetate. CAS Number: 145781-92-6. Molecular Formula: C59H84N18O14 . XC2H4O2. Formula Weight: 1269.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 0.25 mg/ml, PBS (pH 7.2): 10 mg/ml. lambdamax: 222, 282 nm. SMILES: O=C(N[C@H](C(N[C@@H](CC1=CC=C(O)C=C1)C(N[C@H](COC(C)(C)C)C(N[C@@H](CC(C)C)C(N[C@@H](CCCNC(N)=N)C(N2CCC[C@H]2C(NNC(N)=O)=O)=O)=O)=O)=O)=O)CO)[C@@H](NC([C@H](CC3=CNC=N3)NC([C@@H]4CCC(N4)=O)=O)=O)CC5=CNC6=C5C=CC=C6.OC(C)=O. InChi Code: InChI=1S/C59H84N18O14.C2H4O2/c1-31(2)22-40(49(82)68-39(12-8-20-64-57(60)61)56(89)77-21-9-13-46(77)55(88)75-76-58(62)90)69-54(87)45(29-91-59(3,4)5)74-50(83)41(23-32-14-16-35(79)17-15-32)70-53(86)44(28-78)73-51(84)42(24-33-26-65-37-11-7-6-10-36(33)37)71-52(85)43(25-34-27-63-30-66-34)72-48(81)38-18-19-47(80)67-38,1-2(3)4/h6-7,10-11,14-17,26-27,30-31,38-46,65,78-79H,8-9,12-13,18-25,28-29H2,1-5H3,(H,63,66)(H,67,80)(H,68,82)(H,69,87)(H,70,86)(H,71,85)(H,72,81)(H,73,84)(H,74,83)(H,75,88)(H4,60,61,64)(H. InChi Key: IKDXDQDKCZPQSZ-JHYYTBFNSA-N.