Antide (acetate)

Antide is a third generation gonadotropin-releasing hormone receptor (GnRHR) antagonist. It inhibits GnRH-induced secretion of luteinizing hormone (LH), follicle-stimulating hormone (FSH), and gonadotropin in isolated rat pituitary cells when used at concentrations ranging from 0.001 to 1,000 nM but does not induce histamine release in isolated rat mast cells (EC50 = >300 µg/ml). Antide (250 µg/kg, i.v.) reduces serum LH and FSH levels in orchidectomized cynomolgus monkeys. It inhibits ovulation in rats when administered at a dose of 2 µg/animal. Antide (10 µg/animal, s.c.) reduces the intensity and duration of catalepsy induced by haloperidol (Cay-12014) in rats.Formal Name: N-acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-N6-(3-pyridinylcarbonyl)-L-lysyl-N6-(3-pyridinylcarbonyl)-D-lysyl-L-leucyl-N6-(1-methylethyl)-L-lysyl-L-prolyl-D-alaninamide, monoacetate. CAS Number: 625092-10-6. Molecular Formula: C82H108ClN17O14 . C2H4O2. Formula Weight: 1651.3. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble, Ethanol: Soluble. lambdamax: 226 nm. SMILES: ClC(C=C1)=CC=C1C[C@@H](NC([C@H](NC(C)=O)CC2=CC3=C(C=CC=C3)C=C2)=O)C(N[C@H](CC4=CN=CC=C4)C(N[C@@H](CO)C(N[C@@H](CCCCNC(C5=CN=CC=C5)=O)C(N[C@H](CCCCNC(C6=CN=CC=C6)=O)C(N[C@@H](CC(C)C)C(N[C@@H](CCCCNC(C)C)C(N7[C@@H](CCC7)C(N[C@H](C)C(N)=O)=O)=O)=O)=O)=O)=O)=O)=O.O=C(C)O. InChi Code: InChI=1S/C82H108ClN17O14.C2H4O2/c1-50(2)41-65(76(108)95-64(26-11-12-37-88-51(3)4)82(114)100-40-18-27-70(100)81(113)91-52(5)71(84)103)96-75(107)63(25-10-14-39-90-73(105)60-23-17-36-87-48-60)93-74(106)62(24-9-13-38-89-72(104)59-22-16-35-86-47-59)94-80(112)69(49-101)99-79(111)68(45-56-19-15-34-85-46-56)98-78(110)67(43-54-29-32-61(83)33-30-54)97-77(109)66(92-53(6)102)44-55-28-31-57-20-7-8-21-58(57)42-55,1-2(3)4/h7-8,15-17,19-23,28-36,42,46-48,50-52,62-70,88,101H,9-14,18,24-27,37-41,43-45,49H2,1-6H3,(H2,84,103)(H,89,104)(H,90,105)(H,91,113)(H,92,102)(H,93,106)(H,94,112)(H,95,108)(H,96,107)(H,97,109)(H,98,110)(H,99,111),1H3,(H,3,4)/t52-,62+,63-,64+,65+,66-,67-,68-,69+,70+,/m1./s1. InChi Key: RHBDDEILKDGLGU-OHURHHEJSA-N.