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Buserelin Acetate

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(Des-Gly10,D-Ser(tBu)6,Pro-NHEt9)-LHRH; Bigonist; HOE-766; HOE766; HOE 766; Profact; Receptal; Suprecur; Suprefact; Tiloryth; Hoe-766 MP; Hoe766 MP
57982-77-1 (net)
Pyr-His-Trp-Ser-Tyr-D-Ser(tBu)-Leu-Arg-Pro-NHEt acetate salt
Molecular Formula
Long-term Storage Conditions
Buserelin may be used in the treatment of hormone-responsive cancers such as prostate cancer or breast cancer, estrogen-dependent conditions (such as endometriosis or uterine fibroids), and in assisted reproduction.
Buserelin is a potent LHRH agonist. After a transient increase, continuous administration results in downregulation of LH and FSH levels followed by a suppression of ovarian and testicular steroid biosynthesis.
Areas of Interest
Hormonal therapy
  • Background
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Buserelin is a synthetic analog of gonadotropin-releasing hormone (GnRH). It binds to and activates pituitary gonadotropin releasing hormone (GnRH) receptors. Prolonged administration of buserelin results in sustained inhibition of gonadotropin production, suppression of testicular and ovarian steroidogenesis, and reduced levels of circulating gonadotropin and gonadal steroids. Buserelin is more potent that GnRH.

CAS: 57773-65-6 (net)
Sequence: Pyr-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-NHEt acetate salt
M.W: 1281.64
Molecular Formula: C64H83N17O12
CAS: 16679-58-6
Sequence: 3-Mercaptopropionyl-Tyr-Phe-Gln-Asn-Cys-Pro-D-Arg-Gly-NH2 acetate salt (Disulfide bond)
M.W: 1069.2
Molecular Formula: C46H64N14O12S2
CAS: 38234-21-8 (net)
Sequence: Pyr-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-NHEt acetate salt
M.W: 1153.31
Molecular Formula: C55H76N16O12
CAS: 123246-29-7
Sequence: Ac-DNal-DCpa-DPal-Ser-Tyr-DHar(Et2)-Leu-Har(Et2)-Pro-DAla -NH2
M.W: 1570.4
Molecular Formula: C80H113ClN18O13
CAS: 34973-08-5
Sequence: Pyr-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2 acetate salt
M.W: 1242.36
Molecular Formula: C55H75N17O13.C2H4O2

Buserelin acetate appears to cause a progressive blockade of gonadotrophin secretion when administered to female rats for four, eight or 12 days, and an important rebound effect, with accentuated estrogen release already apparent in the first estrous cycle following treatment.

Trindade C R, Camargos A F, Pereira F E L. The effect of buserelin acetate on the uterus of adult rats: morphological aspects[J]. Clin Exp Obstet Gynecol, 2008, 3: 198-201.

A comparison has been established retrospectively between clomiphene citrate-human menopausal gonadotropin (CC-hMG) and buserelin acetate-hMG treatments in in vitro fertilization trials performed over a 3-year period. The analysis of 466 CC-hMG and 319 buserelin acetate-hMG trials shows that buserelin acetate-hMG stimulation generates a greater ovarian response resulting in higher numbers of oocytes being retrieved (6.2 + 3.8 versus 9.3 + 5.2) and fertilized (2.8 + 2.7 versus 4.3 + 3.8). More embryos are thus obtained, allowing a wider choice for intrauterine replacement and cryopreservation. Mean embryonic vitality scores do not differ (4.33 + 1.51 versus 4.44 + 1.54), implying that the embryonic quality remains similar in both treatments. A premature demise of the corpus luteum occurs in a large proportion of buserelin acetate-hMG cycles. However, when suppletive progesterone treatment is given, there is a trend toward a better implantation rate per embryo, and a significantly higher ongoing pregnancy rate is observed in relation to buserelin acetate-hMG treatment (20%) as compared with CC-hMG cycles (14%).

Lejeune B, Barlow P, Puissant F, et al. Use of buserelin acetate in an in vitro fertilization program: a comparison with classical clomiphene citrate-human menopausal gonadotropin treatment[J]. Fertility and sterility, 1990, 54(3): 475-481.

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