A synthetic GNRH agonist
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Histrelin (acetate)

Item No. 23663

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-[1-(phenylmethyl)-D-histidine]-9-(N-ethyl-L-prolinamide)-1-9-luteinizing hormone-releasing factor (swine), acetate
CAS Number
220810-26-4
Synonyms
  • [Des-Gly10,D-His(Bzl)6]-LHRHethyl amide
  • [Des-Gly10,D-His(Bzl)6,Pro-NHEt9]-LHRH
  • [(ImBzl)-d-His6,Pro9-NET]-LHRH
Molecular Formula
C66H86N18O12 • XC2H4O2
Formula Weight
1323.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 0.25 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
281 nm
SMILES
O=C([C@@H]1CCC(N1)=O)N[C@@H](CC2=CNC=N2)C(N[C@@H](CC3=CNC4=C3C=CC=C4)C(N[C@@H](CO)C(N[C@@H](CC5=CC=C(O)C=C5)C(N[C@H](CC6=CN(CC7=CC=CC=C7)C=N6)C(N[C@@H](CC(C)C)C(N[C@@H](CCCNC(N)=N)C(N8CCC[C@H]8C(NCC)=O)=O)=O)=O)=O)=O)=O)=O.OC(C)=O
InChi Code
InChI=1S/C66H86N18O12.C2H4O2/c1-4-70-64(95)55-17-11-25-84(55)65(96)48(16-10-24-71-66(67)68)76-58(89)49(26-38(2)3)77-62(93)53(30-43-34-83(37-74-43)33-40-12-6-5-7-13-40)81-59(90)50(27-39-18-20-44(86)21-19-39)78-63(94)54(35-85)82-60(91)51(28-41-31-72-46-15-9-8-14-45(41)46)79-61(92)52(29-42-32-69-36-73-42)80-57(88)47-22-23-56(87)75-47;1-2(3)4/h5-9,12-15,18-21,31-32,34,36-38,47-55,72,85-86H,4,10-11,16-17,22-30,33,35H2,1-3H3,(H,69,73)(H,70,95)(H,75,87)(H,76,89)(H,77,93)(H,78,94)(H,79,92)(H,80,88)(H,81
InChi Key
OWAUGAMNPZHEOJ-YKZVIGSYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Histrelin is a synthetic gonadotropin-releasing hormone (GNRH) agonist that binds to the GNRH receptor (GNRHR; Ki = 0.2 nM in CHO cells expressing the human receptor).1 It stimulates release of oxytocin (Item No. 11799) and vasopressin ex vivo from the isolated rat hypothalamo-neurohypophysial system at a concentration of 100 nM.2,3 In vivo, the initial dose of histrelin (100 μg) stimulates acute increases in luteinizing hormone (LH), follicle-stimulating hormone (FSH), and testosterone serum levels (50-, 2.5-, and 15-fold, respectively), while chronic treatment leads to 95% decreases in LH and FSH responses in rhesus monkeys.4 Formulations containing histrelin have been used in the treatment of advanced prostate cancer and central precocious puberty.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Nederpelt, I., Georgi, V., Schiele, F., et al. Characterization of 12 GnRH peptide agonists - a kinetic perspective. Br. J. Pharmacol. 173(1), 128-141 (2016).

    2. Juszczak, M., and Boczek-Leszczyk, E. Hypothalamic gonadotropin-releasing hormone receptor activation stimulates oxytocin release from the rat hypothalamo-neurohypophysial system while melatonin inhibits this process. Brain Res. Bull. 81(1), 185-190 (2010).

    3. Boczek-Leszczyk, E., Stempniak, B., and Juszczak, M. Vasopressin release from the rat hypothalamo-neurohypophysial system: Effects of gonadotrophin-releasing hormone (GnRH), its analogues and melatonin. J. Physiol. Pharmacol. 61(4), 459-466 (2010).

    4. Sundaram, K., Thau, R.B., Goldstein, M., et al. Effect of an LHRH agonist on pituitary and testicular function in rhesus monkeys. J. Reprod. Fertil. 72(2), 365-371 (1984).