| Identification | Back Directory | [Name]
Antide Acetate | [CAS]
625092-10-6 | [Synonyms]
N-((4R,7R,10R,13S,16S,19R)-19-(((S)-1-(((S)-1-((S)-2-(((R)-1-Amino-1-oxopropan-2-yl)carbamoyl)pyrrolidin-1-yl)-6-(isopropylamino)-1-oxohexan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)carbamoyl)-7-(4-chlorobenzyl)-13-(hydroxymethyl)-4-(naphthalen-2-ylmethyl)-16-(4-(nicotinamido)butyl)-2,5,8,11,14,17-hexaoxo-10-(pyridin-3-ylmethyl)-3,6,9,12,15,18-hexaazatricosan-23-yl)nicotinamide acetate | [Molecular Formula]
C84H112ClN17O16 | [MOL File]
625092-10-6.mol | [Molecular Weight]
1651.37 |
| Hazard Information | Back Directory | [Uses]
Antide (D-21074) acetate is a potent LHRH antagonist. Antide also can be used for the research of prostatic cancer[1]. | [Biological Activity]
Antide is a third generation gonadotropin-releasing hormone receptor (GnRHR) antagonist.1,2,3,4 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).1,3 Antide (250 μg/kg, i.v.) reduces serum LH and FSH levels in orchidectomized cynomolgus monkeys.2 It inhibits ovulation in rats when administered at a dose of 2 μg/animal.3 Antide (10 μg/animal, s.c.) reduces the intensity and duration of catalepsy induced by haloperidol in rats.4 | [in vivo]
Antide (subcutaneously; 1, 3, 6, 10 and 15 mg/kg; once or on 5 consecutive days) can induce a long-term chemical castration in adult male rats and cynomolgus monkeys[1]. | Animal Model: | Cynomolgus monkey and rat[1] | | Dosage: | 1, 3, 6, 10 and 15 mg/kg | | Administration: | Subcutaneous, once or on 5 consecutive days | | Result: | Had a dose-dependent inhibitory effect on serum concentration of LH (only rat) and testosterone and on the weights of the testes, prostates and seminal vesicles.
Achieved long-lasting castration-like effects at concentrations between 6 (less than or equal to 8 weeks) and 15 mg/kg (greater than 8 weeks) in the rat.
Induced a prolonged inhibitory effect only at 15 mg/kg and the duration was only 2-3 weeks in the cynomolgus monkey. |
| [References]
1.Danforth, D.R., Williams, R.F., Gordon, K., et al.Inhibition of pituitary gonadotropin secretion by the gonadotropin-releasing hormone antagonist antide. I. In vitro studies on mechanism of actionEndocrinology128(4)2036-2040(1991)
2.Weinbauer, G.F., and Nieschlag, E.Comparison of the antigonadotropic activity of three GnRH antagonists (Nal-Glu, Antide and Cetrorelix) in a non-human primate model (Macaca fascicularis)Andrologia25(3)141-147(1993)
3.Flouret, G., Arnold, Z.S., Majewski, T., et al.Antiovulatory antagonists of LHRH related to antideJ. Pept. Sci.1(2)89-108(1995)
4.Umathe, S.N., Wanjari, M.M., Manna, S.S.S., et al.A possible participation of gonadotropin-releasing hormone in the neuroleptic and cataleptic effect of haloperidolNeuropeptides43(3)251-257(2009)
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