Khoom Taw Qhia
Khoom Khoom
Daim ntawv hnub nyab xeeb (SDS)

Khoom npe:Liraglutide

Cas No.204656-20-2

SequenceH-His-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys(N-ε-(N -Palmitoyl -L- -glutamyl))-Glu-Phe-Ile-Ala-Trp-Leu-Val-Arg-Gly-Arg-Gly-OH

Molecular FormulaC₁₇₂H₂₆₅N₄₃O₅₁

Molar Mass3751.20

Qhov siab tshaj plaws uas tsis tau teev tseg tsawg dua lossis sib npaug rau 0.2%

Cia kub 5 degree ± 3 degree

Packing Size100G / Lub raj mis lossis ntawm cov neeg siv khoom xav tau.

Liraglutide, ib qho analog ntawm tib neeg GLP-1, thiab ua raws li GLP-1 receptor agonist. Lub recombinant peptide precursor ntawm liraglutide, tsim los ntawm nws cov lus qhia hauv Saccharomyces cerevisiae, tau raug tsim los ua 97% homologous rau haiv neeg GLP-1 los ntawm kev hloov R rau K ntawm txoj hauj lwm 34. Liraglutide tau tsim los ntawm kev txuas C{{ 5}} fatty acid (palmitic acid) nrog glutamic acid spacer ntawm qhov seem lysine residue ntawm txoj hauj lwm 26 ntawm peptide precursor.

Qhov taw qhia

Rau kev siv / kho mob ntshav qab zib mellitus hom 2.

Pharmacodynamics

Liraglutide yog GLP ib hnub ib zaug -1 derivative rau kev kho mob ntshav qab zib hom 2. GLP-1, nyob rau hauv nws daim ntawv ntuj, yog luv luv nyob rau hauv lub cev (ib nrab-lub neej tom qab txhaj tshuaj subcutaneous yog kwv yees li ib teev), yog li nws tsis muaj txiaj ntsig zoo li tus neeg sawv cev kho. Txawm li cas los xij, liraglutide muaj ib nrab-lub neej tom qab txhaj tshuaj subcutaneous ntawm 11â€ "15 teev, ua rau nws tsim nyog rau kev noj ib hnub ib zaug. } molecule, ua kom nws khi rau albumin nyob rau hauv cov ntaub so ntswg subcutaneous thiab cov hlab ntsha Lub active GLP-1 ces tso tawm los ntawm albumin ntawm qeeb, zoo ib yam ntawm kev khi nrog albumin kuj ua rau qeeb degradation thiab txo kev tshem tawm ntawm liraglutide kev ncig ntawm ob lub raum piv rau GLP-1.

Mechanism ntawm Action

Liraglutide yog ib qho acylated GLP -1 (Glucagon-zoo li Peptide -1) receptor agonist. Liraglutide upregulates intracellular cAMP ua rau kev tso tawm ntawm insulin muab cov ntshav qabzib ntau ntxiv. Glucagon secretion kuj txo qis hauv cov piam thaj-dependant zam los ntawm liraglutide.

Metabolism

Hauv thawj 24 teev tom qab kev tswj hwm ntawm ib zaug [3H]-liraglutide koob tshuaj rau cov neeg noj qab haus huv, cov khoom tseem ceeb hauv cov ntshav yog liraglutide tsis zoo. Liraglutide yog endogenously metabolized zoo ib yam li cov proteins loj uas tsis muaj lub cev tshwj xeeb raws li txoj hauv kev tseem ceeb ntawm kev tshem tawm.

Liraglutide ua ntu zus: H-His-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys(-Glu-palmitoyl)-Glu- Phe-Ile-Ala-Trp-Leu-Val-Arg-Gly-Arg-Gly-OH
Molecular Luj: 3751.20 g / mol	Cov mis mos molecular: C₁₇₂H₂₆₅N₄₃O₅₁
CAS Nr.: [204656-20-2]	Ib nrab neej: kwv yees. 13 hnu

Kev nqus

Qhov siab tshaj plaws ntawm liraglutide tau ua tiav ntawm {{0}} teev tom qab noj tshuaj. Qhov nruab nrab qhov siab tshaj plaws thiab tag nrho kev nthuav tawm ntawm liraglutide yog 35 ng / mL thiab 960 ng·h / mL, raws li, rau subQ ib koob ntawm 0.6 mg. Tom qab kev tswj hwm subcutaneous ib zaug, Cmax thiab AUC ntawm liraglutide tau nce qhov sib npaug ntawm cov tshuaj kho ntau ntawm 0.6 mg rau 1.8 mg. Ntawm 1.8 mg Victoza, qhov nruab nrab nyob rau hauv lub xeev cov concentration ntawm liraglutide tshaj 24 teev yog kwv yees li 128 ng / mL AUC0-∞ yog sib npaug ntawm sab caj npab thiab lub plab, thiab nruab nrab ntawm caj npab thiab ncej puab. AUC0-∞ ntawm tus ncej puab yog 22% qis dua li ntawm lub plab. Qhov tseeb bioavailability ntawm liraglutide tom qab kev tswj hwm subcutaneous yog kwv yees li 55%.

Cim npe nrov: Tuam Tshoj liraglutide manufacturers, hoobkas