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Merck
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SML2919

Sigma-Aldrich

Abarelix acetate

Sinónimos:

N-Ac-D-Nal-4-Cl-D-Phe-D-Pal-Ser-N-Me-Tyr-D-Asn-Leu-Lys(iPr)-Pro-D-Ala-NH2, acetate salt, N-Ac-DNal-DCpa-DPal-Ser-Nα-Me-Tyr-DAsn-Leu-ILys-Pro-DAla-NH2, acetate salt, N-Acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-N-methyl-L-tyrosyl-D-asparaginyl-L-leucyl-N6-(1-methylethyl)-L-lysyl-L-prolyl-D-alaninamide, acetate salt, PPI 149 acetate, PPI-149 acetate, PPI149 acetate, R 3827 acetate, R-3827 acetate, R3827 acetate

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About This Item

Fórmula empírica (notación de Hill):
C72H95ClN14O14 · xC2H4O2
Número de CAS:
785804-17-3
Peso molecular:
1416.06 (free base basis)
UNSPSC Code:
12352200
NACRES:
NA.77

assay

≥97% (HPLC)

Quality Level

100

form

film or powder

color

white to beige

storage temp.

−20°C

Biochem/physiol Actions

Abarelix (PPI-149) is a gonadotropin releasing hormone (GnRH)/luteinizing hormone releasing hormone (LHRH) receptor (GnRHR, LHRHR) antagonist with low histamine release induction propensity (EC50 = 100 μg/mL; rat mast cells). Abarelix exhibits good in vivo efficacy via iv. or sc. in suppressing LH levels in castrated male rats (plasma LH = 12/1.2/0.9/1.2 ng/mL 6 hrs post 0/12.5/50/200 μg/kg in 5% mannitol sc.) and in lowering testosterone among intact male rats (plasma testosterone = 1.64/0.29 ng/mL 6 hrs post 0/3 μg/kg sc.).

pictograms

Health hazard
GHS08

signalword

Warning

hcodes

H361d

Hazard Classifications

Repr. 2

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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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
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
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

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