A GnRHR antagonist
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Antide (acetate)

Item No. 31486

Technical Information
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
Purity
≥98%
Formulation
A solid
DMSO: SolubleEthanol: Soluble
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    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 (Item No. 12014) in rats.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Danforth, D.R., Williams, R.F., Gordon, K., et alInhibition of pituitary gonadotropin secretion by the gonadotropin-releasing hormone antagonist antide. I. In vitro studies on mechanism of action. Endocrinology 128(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). Andrologia 25(3), 141-147 (1993).

    3. Flouret, G., Arnold, Z.S., Majewski, T., et alAntiovulatory antagonists of LHRH related to antide. J. Pept. Sci. 1(2), 89-108 (1995).

    4. Umathe, S.N., Wanjari, M.M., Manna, S.S.S., et alA possible participation of gonadotropin-releasing hormone in the neuroleptic and cataleptic effect of haloperidol. Neuropeptides 43(3), 251-257 (2009).