Saltar al contenido
Merck

SML2856

Sigma-Aldrich

Degarelix acetate

≥98% (HPLC), powder, GnRH receptor antagonist

Sinónimos:

ASP3550 acetate, Ac-D2Nal-D4Cpa-D3Pal-Ser-4Aph(L-hydroorotyl)-D4Aph(carbamoyl)-Leu-ILys-Pro-DAla-NH2 acetate salt, FE 200486, FE200486, N-Acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-4-[[[(4S)-hexahydro-2,6-dioxo-4-pyrimidinyl]carbonyl]amino]-L-phenylalanyl-4-[(aminocarbonyl)amino]-D-phenylalanyl-L-leucyl-N6-(1-methylethyl)-L-lysyl-L-prolyl-D-alaninamide acetate salt

Iniciar sesiónpara Ver la Fijación de precios por contrato y de la organización


About This Item

Fórmula empírica (notación de Hill):
C82H103ClN18O16 · xC2H4O2
Número de CAS:
Peso molecular:
1632.26 (free base basis)
UNSPSC Code:
12352200
NACRES:
NA.77

Nombre del producto

Degarelix acetate, ≥98% (HPLC)

Quality Level

assay

≥98% (HPLC)

form

powder

color

white to beige

storage temp.

−20°C

SMILES string

Clc1ccc(cc1)C[C@@H](NC(=O)[C@H](NC(=O)C)Cc7cc8c(cc7)cccc8)C(=O)N[C@H](Cc6cnccc6)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc4ccc(cc4)NC(=O)[C@H]5NC(=O)NC(=O)C5)C(=O)N[C@H](Cc3ccc(cc3)NC(=O)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2[C@@H](CCC2)C(=O)N[C@H](C)

InChI

1S/C82H103ClN18O16.C2H4O2/c1-45(2)35-60(72(107)92-59(16-9-10-33-87-46(3)4)80(115)101-34-12-17-68(101)79(114)88-47(5)70(84)105)93-74(109)63(38-51-23-30-58(31-24-51)91-81(85)116)95-76(111)64(39-50-21-28-57(29-22-50)90-71(106)66-42-69(104)100-82(117)99-66)97-78(113)67(44-102)98-77(112)65(41-53-13-11-32-86-43-53)96-75(110)62(37-49-19-26-56(83)27-20-49)94-73(108)61(89-48(6)103)40-52-18-25-54-14-7-8-15-55(54)36-52;1-2(3)4/h7-8,11,13-15,18-32,36,43,45-47,59-68,87,102H,9-10,12,16-17,33-35,37-42,44H2,1-6H3,(H2,84,105)(H,88,114)(H,89,103)(H,90,106)(H,92,107)(H,93,109)(H,94,108)(H,95,111)(H,96,110)(H,97,113)(H,98,112)(H3,85,91,116)(H2,99,100,104,117);1H3,(H,3,4)/t47-,59+,60+,61-,62-,63-,64+,65-,66+,67+,68+;/m1./s1

InChI key

AUTFSFUMNFDPLH-KYMMNHPFSA-N

Biochem/physiol Actions

Degarelix acetate (FE200486) is a gonadotropin-/luteinizing hormone-/follicle-stimulating hormone-releasing hormone (GnRH, LHRH, FSH-RH) receptor antagonist that inhibits plasma testosterone for more than 40 days following a single s.c. dosage of 2 mg/kg in rats and monkeys, showing longer in vivo duration than abarelix, ganirelix, cetrorelix, azaline B or D-Trp6-LHRH, and exhibiting only weak histamine-releasing potency in isolated rat mast cells. Bi-weekly s.c. dosing (2 mg/kg) is efficacious in suppressing the growth of human prostate cancer PAC120 xenograft-derived tumors in mice in vivo.

pictograms

Health hazard

signalword

Danger

hcodes

Hazard Classifications

Repr. 1B

Storage Class

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


Elija entre una de las versiones más recientes:

Certificados de análisis (COA)

Lot/Batch Number

¿No ve la versión correcta?

Si necesita una versión concreta, puede buscar un certificado específico por el número de lote.

¿Ya tiene este producto?

Encuentre la documentación para los productos que ha comprado recientemente en la Biblioteca de documentos.

Visite la Librería de documentos

G Jiang et al.
Journal of medicinal chemistry, 44(3), 453-467 (2001-07-21)
A series of antagonists of gonadotropin-releasing hormone (GnRH) of the general formula Ac-D2Nal-D4Cpa-D3Pal-Ser-4Aph/4Amf(P)-D4Aph/D4Amf(Q)-Leu-ILys-Pro-DAla-NH2 was synthesized, characterized, and screened for duration of inhibition of luteinizing hormone release in a castrated male rat assay. Selected analogues were tested in a reporter gene
Wolfgang Koechling et al.
British journal of clinical pharmacology, 70(4), 580-587 (2010-09-16)
Early studies on gonadotrophin-releasing hormone (GnRH) antagonists pointed out histamine-mediated anaphylactic reactions as a potential adverse effect of these drug candidates. In this study we have compared the histamine-releasing potential of four approved and marketed antagonists, degarelix, cetrorelix, abarelix and
Pierre Broqua et al.
The Journal of pharmacology and experimental therapeutics, 301(1), 95-102 (2002-03-22)
We describe the pharmacological profile in rats and monkeys of degarelix (FE200486), a member of a new class of long-acting gonadotropin-releasing hormone (GnRH) antagonists. At single subcutaneous injections of 0.3 to 10 microg/kg in rats, degarelix produced a dose-dependent suppression

Nuestro equipo de científicos tiene experiencia en todas las áreas de investigación: Ciencias de la vida, Ciencia de los materiales, Síntesis química, Cromatografía, Analítica y muchas otras.

Póngase en contacto con el Servicio técnico