Tom ntej: PT-141 Acetateyog ib qho tshuaj tshiab nrog cov qauv tshuaj tshwj xeeb thiab cov tshuaj pharmacological. Nws yog ib qho hluavtaws molecule uas muaj peb yam tseem ceeb: ib qho N-methyl-D-aspartate (NMDA) receptor antagonist, 5-HT2 receptor antagonist, thiab ib - Adrenergic receptor agonists. Cov khoom xyaw sib txawv no ua rau lawv siv cov tshuaj analgesic thaum ua kom tsis txhob muaj kev phiv. Cov qauv tshuaj ntawm Bremelanotide acetate yog qhov tshwj xeeb, thiab nws qhov tseem ceeb yog N-methyl-D-aspartate (NMDA) receptor antagonist. NMDA receptors yog ib qho tseem ceeb heev ion channel nyob rau hauv lub paj hlwb, koom nrog ntau yam tseem ceeb neural txheej txheem, xws li kev kawm thiab kev nco, kev loj hlob ntawm neural, thiab paj hlwb regeneration. Antagonizing NMDA receptors tuaj yeem cuam tshuam zoo rau kev sib kis ntawm cov cim mob, yog li ua rau muaj kev phom sij. Txawm li cas los xij, yooj yim NMDA antagonists yuav muaj kev phiv loj xws li kev puas siab puas ntsws, xeev siab, ntuav, thiab kev vam khom. Yog li ntawd, Bremelanotide acetate khi rau 5-HT2 receptor antagonists thiab - Adrenergic receptor agonists tsom txo qhov tshwm sim ntawm cov kev mob tshwm sim.
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Customized Bottle Caps Thiab Corks:
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Tom ntej: PT-141 Acetateyog ib qho hluavtaws peptide compound raws li melanocyte stimulating hormone (MSH). Nws cov qauv tseem ceeb yog cyclic heptapeptide, npaj los ntawm cov khoom siv -theem peptide synthesis thev naus laus zis, nrog lub cev hnyav ntawm 1025.18 thiab lub ntsej muag dawb rau cov hmoov dawb. Cov tshuaj no nthuav tawm cov txiaj ntsig tshwj xeeb hauv cov tshuaj, kev tshawb fawb tshawb fawb, thiab kev lag luam vim nws cov kev xaiv ua kom zoo ntawm melanocortin receptor type 4 (MC4R).
1. Cov ntsiab lus tseem ceeb: Tsawg yam tsis muaj kev xav deev tsis zoo (HSDD)
PT-141 hydrochloride yog lub ntiaj teb thawj cov tshuaj uas tswj kev sib deev muaj siab los ntawm activating endogenous txoj kev nyob rau hauv lub hauv paus paj hlwb, thiab nws cov txheej txheem ntawm kev txiav txim yog kiag li txawv los ntawm ib txwm lub zos tshuaj estrogen los yog androgen hloov kho. Los ntawm kev tsom mus rau MC4R receptor, cov tshuaj no tuaj yeem hla cov hlab ntsha peripheral thiab ua ncaj qha rau ntawm hypothalamic pituitary gonadal axis, txhawb kev tso tawm ntawm dopamine thiab norepinephrine, yog li txhawb kev sib deev thiab kev teb.
Clinical trial data:
Hauv Phase I mus sib hais, cov poj niam premenopausal uas tau txais ib qho kev txhaj tshuaj subcutaneous ntawm 1.25-20mg tau pom tias muaj qhov nce ntxiv ntawm qhov zaus ntawm kev sib deev (SES) tau qhab nia thiab tsis muaj kev cuam tshuam loj heev.
Theem III kev sim tau pom tias tom qab 12 lub lis piam ntawm kev siv tas li, kev txhim kho tus neeg mob qhov kev xav tau kev sib deev (FSDS-DAO) tau mus txog 62%, uas zoo dua li 31% hauv pawg placebo.
Kev tshawb fawb txog kev nyab xeeb ntev ntev tau lees paub tias nws txoj kev pheej hmoo ntawm cov hlab plawv thiab qhov tshwm sim ntawm cov kev mob tshwm sim ntawm metabolic yog qis dua li cov tshuaj phosphodiesterase inhibitors (xws li sildenafil).
2. Qhov zoo piv rau cov kev kho mob ib txwm muaj
Parameter PT-141 hydrochloride hauv zos tshuaj hormone kho qhov ncauj PDE5 inhibitor
Lub hom phiaj: Central nervous system MC4R, peripheral reproductive organs, corpus cavernosum smooth nqaij ntawm noov
Lub sijhawm ua haujlwm zoo yog 30-60 feeb, thiab nws yuav tsum tau siv tsis tu ncua rau ob peb lub lis piam rau 30-45 feeb
Ib nrab neej 2-3 teev 24-48 teev 4-6 teev
Cov kev mob tshwm sim tseem ceeb: xeev siab, lub ntsej muag dej, qhov chaw mos khaus, muaj feem yuav mob qog noj ntshav, mob taub hau, pom kev txawv txav
Muaj cov pej xeem: premenopausal / postmenopausal cov poj niam, tsuas yog cov poj niam postmenopausal, txiv neej erectile kawg
3. Cov ntawv thov tshwj xeeb scenario
Kev ua haujlwm ntawm kev sib deev ntawm cov neeg mob qog noj ntshav: cov neeg mob qog noj ntshav tom qab phais tau txo qis kev sib deev vim kev kho mob endocrine. PT-141 hydrochloride tuaj yeem txhim kho lawv txoj kev sib deev kev noj qab haus huv ntsig txog lub neej (QoL), thiab tsis cuam tshuam nrog cov txheej txheem ntawm kev kho tshuaj hormone.
Kev raug mob ntawm tus txha caj qaum tsis ua haujlwm: Cov kev sim tsiaj tau pom tias cov tshuaj no tuaj yeem txhawb nqa tus cwj pwm mating hauv nas nrog tus txha caj qaum raug mob, muab txoj hauv kev kho tshiab rau kev ua haujlwm neurogenic.
Adjuvant therapy rau poj niam txiv neej tsis meej pem: Cov poj niam hloov pauv feem ntau muaj kev hloov pauv ntawm kev sib deev muaj siab thaum lub sij hawm kho tshuaj hormone hloov, thiab PT-141 hydrochloride tuaj yeem siv los ua ib qho ntxiv los tswj kev sib deev.
1. Cov cuab yeej tshawb fawb neurobiological
MC4R signaling txoj kev tsom xam: Raws li kev xaiv MC4R agonist,Tom ntej: PT-141 Acetateyog dav siv los kawm txog lub luag haujlwm ntawm cov receptor no hauv kev sib npaug ntawm lub zog, kev coj tus cwj pwm kev ntxhov siab, thiab kev quav tshuaj. Piv txwv li, kev sim nas tau pom tias nws tuaj yeem cuam tshuam morphine induced conditioned place preference (CPP) los ntawm activating MC4R.
Kev sib deev tus cwj pwm neural circuit mapping: Ua ke nrog optogenetic thev naus laus zis, cov khoom no tuaj yeem nrhiav qhov tseeb ntawm dopaminergic txoj hauv kev los ntawm ventral tegmental cheeb tsam (VTA) ntawm hypothalamus mus rau nucleus accumbens (NAc), nthuav tawm lub hauv paus neural ntawm kev sib deev.
2. Daim tawv nqaij pigmentation qauv
Txawm hais tias PT-141 hydrochloride muaj qhov tsis sib xws rau MC1R (cov tawv nqaij muaj feem xyuam rau cov receptor), nws tseem siv los tsim cov qauv kev tswj hwm melanin synthesis. Piv txwv li, nyob rau hauv lub reconstruction ntawm epidermal qauv, cov tshuaj no yuav induce lub migration ntawm melanocytes, muab ib tug in vitro kev tshawb fawb platform rau kev kho mob ntawm vitiligo.
3. Kev tshuaj xyuas tshuaj thiab tshuaj xyuas
MC4R antagonist txoj kev loj hlob: Raws li cov cuab yeej siv tshuaj, PT-141 hydrochloride tuaj yeem siv los txheeb xyuas cov haujlwm ntawm MC4R antagonists tshiab thiab ua kom cov txheej txheem kev txhim kho ntawm cov tshuaj kho mob rog.
Kev ntsuam xyuas kev ruaj ntseg ntawm cov tshuaj peptide: Cov yam ntxwv kho dua tshiab ntawm lawv qhov khov - cov qauv qhuav (ultrasonic dissolution hauv dej) yog siv los ua tus qauv siv los ntsuas qhov chaw cia khoom ntawm peptide raw khoom.
Kev lag luam sector: Diversified daim ntawv thov ntawm siab -purity raw khoom
1. Kev tsim cov tshuaj intermediates
PT-141 hydrochloride, uas yog ib qho tseem ceeb nruab nrab, tuaj yeem siv los ua ke ntau dua MC4R modulators. Piv txwv li, ntev - ua kom ruaj khov- cov qauv tso tawm tuaj yeem tau txais los ntawm kev hloov kho cov saw hlau sab, nrog ib nrab - lub neej uas tuaj yeem txuas ntxiv mus rau 12 teev, ua tau raws li kev kho mob xav tau rau kev saib xyuas mus ntev ntawm kev ua tau zoo.
2. Kev tsim kho cov tshuaj tiv thaiv kab mob
Immunoassay tus qauv: Siab purity (Ntau dua lossis sib npaug li 99%) PT-141 hydrochloride tuaj yeem siv los ua tus qauv ntsuas rau ELISA cov khoom siv txhawm rau txheeb xyuas qhov concentration ntawm MC4R ntsig txog ligands hauv cov qauv tshuaj lom neeg.
Cell kab lis kev cai additive: Nyob rau hauv MC4R overexpressing cell kab, cov tshuaj no muaj peev xwm tswj tau cov kev ua receptor thiab xyuas kom meej qhov kev cia siab ntawm kev sim tau.
3. Muaj kev sib xyaw ua kom zoo
Kev txhim kho cov txheej txheem txheej txheej txheej txheej txheej txheej: PT-141 hydrochloride muaj cov kauj ruam nyuaj xws li cyclization thiab deprotection. Nws cov txheej txheem tsim khoom lag luam (xws li kev xaiv resin thiab txiav reagent piv) muab kev siv rau kev sib txuas ntawm lwm cov tshuaj peptide.
Green Chemistry Practice: Siv cov pa roj carbon dioxide supercritical raws li qhov nruab nrab cov tshuaj tiv thaiv tuaj yeem txo kev siv cov kuab tshuaj organic thiab txo cov ntsiab lus organic hauv cov kua khib nyiab los ntawm 82%, uas ua tau raws li kev tiv thaiv ib puag ncig.
PT-141 yog cov tshuaj uas muaj cov qauv tshuaj tshwj xeeb thiab cov tshuaj pharmacological, thiab nws txoj kev sib xyaw ua ke kuj yog qhov nyuaj heev. Cov hauv qab no yog ib txoj kev sib txuas ntawm Bremelanotide acetate:
Cov khoom pib:
Cov khoom pib rau kev sib txuas PT-141 feem ntau suav nrog cov amino acids xws li D-aspartic acid, D-alanine, glycine, N-methyl-D-aspartate thiab lawv cov derivatives, nrog rau qee cov organic solvents thiab catalysts.
Synthesis cov kauj ruam:
1. Tiv thaiv cov amino acids
Ua ntej, nws yog ib qho tsim nyog los qhib cov pab pawg tiv thaiv ntawm cov amino acids xws li D-aspartic acid, D-alanine, thiab glycine thiaj li ua rau muaj kev cuam tshuam nrog lwm cov tshuaj. Cov pab pawg tiv thaiv feem ntau suav nrog Boc (tert butoxycarbonyl) thiab Fmoc (fluorene methoxycarbonyl).
2. Activated amino acids
Reacted activated amino acids nrog rau lwm cov amino acid derivatives xws li N-methyl-D-aspartate los tsim peptide chains uas muaj ntau yam amino acid residues. Cov kauj ruam no yuav tsum tau siv cov catalysts thiab cov kuab tshuaj uas tsim nyog.
3. Cov tshuaj tiv thaiv condensation
Condensate cov saw peptide generated nrog cov amino acids xws li glycine los tsim cov saw ntev peptide saw. Cov kauj ruam no yuav tsum tau siv cov condensation reagents thiab catalysts.
4. Tsis muaj kev tiv thaiv thiab acid txiav
Tom qab cov tshuaj tiv thaiv condensation tiav, pawg tiv thaiv ntawm cov amino acid yuav tsum tau muab tshem tawm thiab cov saw peptide yuav tsum tau tso tawm los ntawm cov resin. Cov kauj ruam no yuav tsum tau siv cov tshuaj tiv thaiv tsim nyog thiab cov kua qaub txiav reagents.
5. Purification thiab crystallization
Thaum kawg, tus tsim PT-141 yuav tsum tau purified thiab crystallized kom tshem tawm impurities thiab unreacted raw khoom. Cov kauj ruam no feem ntau yuav tsum tau siv ntau yam txheej txheem chromatographic rau kev sib cais thiab kev huv, nrog rau kev siv cov kuab tshuaj tsim nyog rau crystallization.
Cov kev ceev faj:
Nyob rau hauv tus txheej txheem ntawm synthesizingTom ntej: PT-141 Acetate, cov ntsiab lus hauv qab no yuav tsum tau sau tseg:
Qhov zoo thiab purity ntawm raw cov ntaub ntawv muaj feem xyuam rau cov synthesis tshwm sim, yog li ntawd nws yog tsim nyog los nruj me ntsis tswj qhov zoo thiab purity ntawm raw cov ntaub ntawv.
Kev xaiv thiab ua kom tiav qib ntawm cov pab pawg tiv thaiv muaj feem cuam tshuam rau kev tsim cov peptide chains, yog li nws yog ib qho tsim nyog los xaiv cov pab pawg tiv thaiv tsim nyog thiab kev ua kom muaj zog raws li qhov xwm txheej tshwj xeeb.
Cov xwm txheej ntawm cov tshuaj tiv thaiv condensation muaj feem cuam tshuam rau qhov ntev thiab cov qauv ntawm cov saw peptide, yog li nws yog ib qho tsim nyog los xaiv cov condensation reagents thiab catalysts, thiab tswj cov tshuaj tiv thaiv.
Kev tiv thaiv thiab kev txiav cov kua qaub yog ib qho ntawm cov kauj ruam tseem ceeb uas cuam tshuam rau kev sib xyaw ua ke thiab cov khoom zoo. Yog li ntawd, nws yog ib qho tsim nyog yuav tau xaiv cov tshuaj tiv thaiv kom tsim nyog thiab cov kua qaub txiav reagents, thiab tswj cov kev mob tshwm sim.
Purification thiab crystallization yog ib qho ntawm cov kauj ruam tseem ceeb uas cuam tshuam rau cov khoom zoo, yog li nws yog ib qho tsim nyog yuav tsum xaiv cov txheej txheem sib cais thiab kev ua kom huv, nrog rau siv cov kuab tshuaj tsim nyog rau crystallization.
Nyob rau hauv cov ntsiab lus, cov synthesis ntawm PT-141 yog ib tug complex txheej txheem uas yuav tsum tau nruj me ntsis tswj ntawm cov tshuaj tiv thaiv tej yam kev mob thiab raw khoom zoo, raws li zoo raws li xyuam xim rau cov teeb meem kev nyab xeeb. Nyob rau tib lub sijhawm, kev tshuaj xyuas thiab kev sim tsim nyog yuav tsum tau ua kom ntseeg tau tias cov khoom zoo thiab kev nyab xeeb.
Cov lus nug nquag
PT-141 puas ua rau koj tawv nqaij?
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Cov neeg uas pib ntawm qhov tsis muaj hnub ci tanning peptide pom lawv cov melanin hauv lawv cov tawv nqaij darkens nrog kev siv. Kev raug tshav ntuj ntau ntxiv yuav ua rau cov melanin ntau lawm. Lub peptide PT-141 yog ib qho derivative ntawm melanotan II.
PT-141 yog dab tsi?
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Kuj hu ua Bremelanotide, PT-141 yog amino acid peptide siv los kho Erectile Dysfunction (ED). PT-141 yog tsim los ntawmcov hluavtaws version ntawm daim tawv nqaij- tsaus nti alpha-Melanocyte stimulating hormone hu ua Melanotan 2. Nws khi rau melanocortin receptors MC1R thiab MC4R.
Kuv puas tuaj yeem noj PT-141 txhua hnub?
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Dosing zaus: Bremelanotide yog npaj raws li kev kho raws li - xav tau (PRN), tsis yog tshuaj noj txhua hnub. FDA cov lus qhia (rau cov poj niam, cov kws kho mob kuj ua raws li cov txiv neej) hais tias tsis pub ntau tshaj ib koob tshuaj hauv 24 teev, thiab tsis pub ntau tshaj 8 koob tshuaj ib hlis.
Yuav ua li cas sib tov PT-141 rau qhov ntswg?
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Kev sib xyaw: - Tso cov tub yees vial kom sov rau chav sov. -Siv cov txheej txheem aseptic thiab rov ua dua lyophilized hmoov (10mg vial) nrog 1ml bacteriostatic dej los yog tus neeg sawv cev buffering. Ib qho kev daws teeb meem rau kev kho dua tshiab yuav txhim kho kev ruaj ntseg.
Dab tsi peptide yog qhov zoo tshaj plaws rau testosterone?
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Peb cov tshuaj hormones no yog txoj hauv kev tseem ceeb uas koj lub cev ua rau testosterone. Ob tug peptides no yogkisspeptin-10 thiab gonadorelin. Hauv ib txoj kev tshawb fawb, kisspeptin-10 nce qhov nruab nrab ntawm cov tshuaj testosterone qib hauv 24 teev ntawm kev txhaj tshuaj.
Cim npe nrov: pt-141 acetate cas 1607799-13-2, lwm tus neeg, manufacturers, hoobkas, lag luam wholesale, yuav, nqe, tej, kev muag khoom