Taw qhia

PT1412

musclepic 8

Khoom Description

1. Kev faib tawm thiab kev tsim qauv

Los ntawm cov khoom muag, PT-141 tuaj yeem muab faib ua pawg hauv qab no:

Pharmaceutical-qib raw khoom peptides: Cov PT-141 peptides feem ntau muaj qhov purity ntawm ntau dua 98%, yog tsim raws li GMP tus qauv, thiab tau ua raws HPLC nruj thiab kuaj spectrometry. Lawv tsuas yog muab rau cov tuam txhab tshuaj thiab cov chaw tshawb fawb rau kev tsim kho lossis kev tshawb fawb tshuaj. Cov khoom no muaj cov kev xav tau siab heev rau purity, aseptic tswj, thiab cov kuab tshuaj residual.

Kev tshawb fawb-qib raw khoom peptides: Cov PT-141 peptides yog tsim los rau kev tshawb fawb hauv chaw soj nstuam, nrog rau kev purity feem ntau ntawm 95% thiab 98%. Lawv feem ntau yog siv hauv xovtooj ntawm tes lossis tsiaj sim. Lawv tsis yog siv rau tib neeg kev txhaj tshuaj tab sis ua lub luag haujlwm tseem ceeb hauv cov tshuaj pharmacokinetic thiab cov txheej txheem - ntawm kev ua haujlwm.

Cov qauv ua tiav: Qee lub tebchaws tau pom zoo PT-141 txhaj tshuaj lossis tshuaj tsuag qhov ntswg ua tshuaj, xws li FDA- pom zoo Bremlanotide (lub npe lag luam Vyleesi) hauv Tebchaws Meskas. Cov formulations no feem ntau yog nyob rau hauv lyophilized hmoov los yog kua daim ntawv, ua rau lawv yooj yim rau cov neeg siv kawg siv ncaj qha, thiab muab kev ruaj ntseg thiab ruaj khov dua.

2. Chemical thiab Physical Properties

PT-141 yog cyclic heptapeptide nrog cov mis mos molecular C50H68N14O10 thiab qhov hnyav molecular ntawm kwv yees li 1025.2 g / mol. Nws cov qauv yog muab los ntawm -melanocyte- stimulating hormone (-MSH), thiab kev ua kom zoo tshaj plaws ntawm cov saw peptide ntuj txhim kho nws txoj kev ruaj ntseg thiab receptor selectivity.

Cov tsos mob thiab xim: High- zoo PT-141 raw khoom hmoov yog feem ntau yog dawb los tawm- cov hmoov dawb lyophilized nrog cov xim zoo nkauj, tsis muaj pob, thiab qis hygroscopicity. Cov hmoov daj daj lossis greyish-dawb feem ntau yog vim qhov tsis zoo cia lossis me ntsis oxidation los ntawm batch impurities.

Solubility: Soluble nyob rau hauv dej, acetate tsis, los yog sterile physiological saline, tsim ib tug ntshiab, pob tshab kua. Nws yog ib qho ruaj khov nyob rau hauv nruab nrab los yog tsis muaj zog acidic ib puag ncig tab sis yooj yim degrades nyob rau hauv muaj zog alkaline tej yam kev mob.

Kev ruaj ntseg thiab Cia: PT-141 yog rhiab rau qhov kub thiab txias thiab yuav tsum khaws cia ntawm -20℃hauv qhov tsaus ntuj. Lub xeev lyophilized muaj lub sijhawm ruaj khov txog li 24 lub hlis, thaum lub xeev cov tshuaj tau pom zoo rau kev siv sijhawm luv.

Physicochemical Properties: Vim nws cov qauv cyclic peptide, nws muaj zog tiv thaiv enzymatic hydrolysis, qeeb metabolism hauv vivo, thiab siab bioavailability. Nws yuav siv sijhawm li ntawm 30 mus rau 60 feeb tom qab txhaj tshuaj lossis kev tswj qhov ntswg, nrog lub sijhawm ua haujlwm ntev li 8 txog 12 teev.

3. Mechanism ntawm Action thiab Pharmacological yam ntxwv

PT-141 yog tshwj xeeb nyob rau hauv uas nws ncaj qha activates MC3R thiab MC4R (melanocortin receptor subtypes) nyob rau hauv lub hlwb, yog li cuam tshuam rau cov hypothalamic neural txoj kev cuam tshuam nrog libido. Cov txheej txheem ntawm kev ua no tso cai rau nws los txhim kho kev sib deev arousal thiab muaj siab tsis hloov ntshav siab lossis lub plawv dhia.

Tsis zoo li cov tshuaj txhim kho kev sib deev ib txwm muaj, PT-141 tsis tso siab rau peripheral vasodilation, ua rau nws tsim nyog rau qee tus neeg mob plawv lossis cov uas tsis teb rau PDE5 inhibitors. Tsis tas li ntawd, nws tau kawm txog kev txhim kho kev xav tsis zoo thiab tswj lub zog metabolism thiab kev sib npaug ntawm cov neuroendocrine.

4. Kev soj ntsuam zoo

Qhov pib nrawm nrawm ntawm Kev Ua Haujlwm thiab Ntuj Ncua Sijhawm: Nws yuav siv sijhawm li 30 mus rau 45 feeb tom qab kev tswj hwm, nrog rau lub sijhawm ntev ntawm kev ua haujlwm uas tsis muaj kev ywj pheej ntawm sab nraud stimuli, uas ua rau cov lus teb zoo ib yam li lub cev lub cev. Central Mechanism of Action: Tsis zoo li cov tshuaj vascular, PT-141 tswj kev sib deev impulses los ntawm lub hauv nruab nrab lub paj hlwb, uas qhia tau hais tias zoo rau hypoactive kev sib deev muaj siab teeb meem (tshwj xeeb tshaj yog poj niam kev sib deev dysfunction).

Kev siv zog ntawm poj niam txiv neej: Hauv kev sim tshuaj, ob tus txiv neej thiab poj niam tau pom cov lus teb zoo, nrog rau kev ua tau zoo tshwj xeeb hauv cov neeg mob uas muaj poj niam tsis muaj zog kev sib deev (HSDD).

Zoo Tolerability thiab me me tshwm sim: Cov kev mob tshwm sim me me muaj xws li lub ntsej muag yaug, xeev siab me ntsis, thiab kev nce siab hauv cov ntshav siab, uas feem ntau tshwm sim nyob rau hauv ob peb teev.

Ntau hom qauv: Nws tuaj yeem tsim rau hauv ntau txoj kev xa khoom xws li kev txhaj tshuaj, tshuaj tsuag qhov ntswg, thiab cov gels transdermal kom tau raws li qhov xav tau ntawm cov neeg siv sib txawv.

5. Cov txheej txheem ntau lawm thiab purification

PT-141 yog tsim los ntawm cov khoom siv-theem peptide synthesis (SPPS) technology. Los ntawm txoj kev Fmoc tshuaj, cov amino acid chains tau txuas ntxiv mus thiab cyclized los tsim cov qauv ruaj khov. Tom qab kev sib xyaw ua ke, nws dhau los ntawm TFA deprotection, nag lossis daus, purification, thiab lyophilization txheej txheem. High- zoo PT-141 feem ntau yog purified siv high-performance kua chromatography (HPLC) thiab huab hwm coj spectrometry (MS) kom paub meej tias nws molecular hnyav, kom ib tug purity siab tshaj 98%. Tsis tas li ntawd, qee cov khoom lag luam qib tshuaj yuav tsum tau kuaj endotoxin, kuaj tsis muaj menyuam, thiab kev tshawb fawb ruaj khov.

6. Cov cheeb tsam thov

Cov ntawv thov kev kho mob: PT-141 tau raug pom zoo rau kev kho mob ntawm hyposexuality disorder (HSDD) hauv cov poj niam thiab tau pom tias muaj txiaj ntsig zoo hauv erectile kawg (ED) hauv cov txiv neej.

Kev Siv Kev Tshawb Fawb: Siv los kawm txog lub luag haujlwm ntawm melanocortin system hauv kev tswj hwm neuroendocrine, mus ob peb vas, thiab tswj kev metabolic; Nws kuj tseem tuaj yeem ua tus qauv sib xyaw rau neuroactive peptides.

Muaj peev xwm nthuav dav: Cov kev tshawb fawb tsis ntev los no tau pom tias PT-141 muaj peev xwm txhim kho kev nyuaj siab, txhawb lub zog metabolism, thiab tswj kev qab los noj mov, muab kev muaj peev xwm rau nws txoj kev nthuav dav yav tom ntej rau hauv thaj chaw ntawm neuropsychiatric mob.

7. Cia thiab siv ceev faj

PT-141 lyophilized hmoov yuav tsum muab cia rau hauv lub thawv kaw hauv qab -20 degree, tiv thaiv los ntawm lub teeb thiab noo noo. Ua ntej siv, nws yuav tsum maj mam warmed rau hauv chav tsev kub thiab yaj nyob rau hauv sterile dej rau kev txhaj tshuaj los yog physiological saline. Cov tshuaj npaj yuav tsum tau siv tam sim ntawd lossis tso rau hauv tub yees tsis pub dhau 48 teev. Tsis txhob sib xyaw nrog cov tshuaj alkaline lossis cov kuab tshuaj uas muaj cov tshuaj tiv thaiv kom tsis txhob muaj cov saw peptide degradation.

8. Cov ntsiab lus

Nyob rau hauv xaus, PT-141, raws li ib tug siab -peptide khoom, muaj siab purity, zoo stability, thiab ib tug tshwj xeeb pharmacological mechanism. Nws cov khoom lag luam tau tsim cov txheej txheem ntau lawm los ntawm kev siv tshuaj mus rau kev tshawb fawb-qib. Chemically, nws muaj qhov zoo xws li cyclic peptide stability, tsis kam mus rau enzymatic degradation, thiab zoo solubility. Nyob rau hauv cov nqe lus ntawm daim ntawv thov, nws tsis tsuas yog zoo txhim kho libido tsawg tab sis kuj muaj lub hauv paus tswj kev muaj peev xwm thiab kev nyab xeeb zoo. Nrog rau kev nce qib ntawm kev siv tshuaj peptide thiab cov txheej txheem bioengineering, PT-141 yuav tsum pom cov ntawv thov dav dua hauv kev tswj hwm neuroendocrine, kev noj qab haus huv ntawm lub hlwb, thiab kev tswj hwm cov metabolism, dhau los ua tus neeg sawv cev ntawm tiam tom ntej ntawm kev ua haujlwm biopeptides tom qab cov tshuaj steroids thiab tshuaj hormones.