Alarelin (acetate)

Alarelin is a peptide agonist of gonadotropin-releasing hormone (GnRH). It binds to the GnRH receptor (GnRHR) with a Kd value of 0.2 nM. Alarelin (6 ng, i.c.v.) decreases the expression of GnRH in the preoptic area and GnRHR in the posterior mediobasal hypothalamus (pMBH) of ovariectomized estradiol-treated rats, indicating an ultrashort negative feedback loop on GnRH and GnRHR gene expression. It induces desensitization in the pituitary and decreases serum estradiol levels and ovarian and uterine weight in neonatal and adult female rats. Alarelin reduces tumor growth in an HEC-1-B human endometrial carcinoma mouse xenograft model when administered at doses of 20, 40, and 80 µg/kg.Formal Name: 6-D-alanine-9-(N-ethyl-L-prolinamide)-1-9-luteinizing hormone-releasing factor (swine), diacetate. CAS Number: 79561-22-1. Synonyms: pGlu-HWSYALRP-NHEt, [D-Ala6, des-Gly10]GnRH-ethylamide, des-Gly GnRH. Molecular Formula: C56H78N16O12 . 2C2H4O2. Formula Weight: 1287.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/ml, DMSO: 5 mg/ml, PBS (pH 7.2): 5 mg/ml. lambdamax: 221 nm. SMILES: O=C(N[C@@H](CO)C(N[C@H](C(N[C@H](C)C(N[C@@H](CC(C)C)C(N[C@@H](CCCNC(N)=N)C(N(CCC1)[C@@H]1C(NCC)=O)=O)=O)=O)=O)CC(C=C2)=CC=C2O)=O)[C@@H](NC([C@@H](NC([C@H](CC3)NC3=O)=O)CC4=CN=CN4)=O)CC5=CNC6=CC=CC=C56.CC(O)=O.CC(O)=O. InChi Code: InChI=1S/C56H78N16O12.2C2H4O2/c1-5-60-54(83)45-13-9-21-72(45)55(84)39(12-8-20-61-56(57)58)66-50(79)40(22-30(2)3)67-47(76)31(4)64-49(78)41(23-32-14-16-35(74)17-15-32)68-53(82)44(28-73)71-51(80)42(24-33-26-62-37-11-7-6-10-36(33)37)69-52(81)43(25-34-27-59-29-63-34)70-48(77)38-18-19-46(75)65-38,2*1-2(3)4/h6-7,10-11,14-17,26-27,29-31,38-45,62,73-74H,5,8-9,12-13,18-25,28H2,1-4H3,(H,59,63)(H,60,83)(H,64,78)(H,65,75)(H,66,79)(H,67,76)(H,68,82)(H,69,81)(H,70,77)(H,71,80)(H4,57,58,61),2*1H3,(H,3,4)/t31-,38+,39+,40+,41+,42+,43+,44+,45+,,/m1../s1. InChi Key: DPWSRXJWCYEGIV-PFHUABGLSA-N.