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Key Documents

SML2919

Sigma-Aldrich

Abarelix acetate

同義詞:

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

經驗公式(希爾表示法):
C72H95ClN14O14 · xC2H4O2
CAS號碼:
分子量::
1416.06 (free base basis)
分類程式碼代碼:
12352200
NACRES:
NA.77

化驗

≥97% (HPLC)

品質等級

形狀

film or powder

顏色

white to beige

儲存溫度

−20°C

生化/生理作用

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.).

象形圖

Health hazard

訊號詞

Warning

危險聲明

危險分類

Repr. 2

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


分析證明 (COA)

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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

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