ORM-15341 CAS Nr .: 1297537-33-7

ORM-15341 yog dab tsi?

Ketodarolutamide (ORM-15341) tau txais kev saib xyuas tseem ceeb hauv kev kho mob qog noj ntshav prostate. Nws yog ib qho muaj zog thiab muaj kev sib raug zoo heev nonsteroidal androgen receptor kev sib tw ua tiav antagonist. Qhov tseem ceeb, nws yog qhov tseem ceeb tshaj plaws metabolite ntawm tom ntej - tiam anti-androgen khoom ODM-201 hauv tib neeg lub cev. Hauv lwm lo lus, tom qab cov neeg mob siv ODM-201, qhov sib xyaw ua haujlwm tau hloov pauv ib nrab rauAWM-15341, uas kuj pom muaj zog heev inhibitory nyhuv ntawm kev ua mob qog noj ntshav.

Ketodarolutamide inhibits testosterone{0}} ntxias AR nuclear translocation. Nws qhov tshwj xeeb zoo cuam tshuam nrog kev loj hlob ntawm AR-cov qog nqaij hlav qog noj ntshav nyob ntawm prostate thiab ua kom pom kev ua haujlwm ntawm cov qog nqaij hlav hauv castration-cov qauv qog nqaij hlav qog nqaij hlav.

tiv tauj peb ntawm Email :sales6@faithfulbio.com

Dab tsi yog qhov mechanism ntawm kev txiav txim ntawm ORM-15341?

ORM-15341 yog nonsteroidal androgen receptor regulatory molecule thiab lub ntsiab active metabolite tsim tom qab lub qhov ncauj compound ODM-201 nkag mus rau tib neeg lub cev. Tom qab noj qhov ncauj ntawm ODM-201, nws yog metabolized nyob rau hauv lub cev mus rau hauv Ketodarolutamide, uas yog cov tseem ceeb active tshuaj rau nws androgen receptor regulatory muaj nuj nqi.

Nws feem ntau ua rau ntawm androgen receptor, lub hom phiaj tseem ceeb rau kev loj hlob ntawm prostate cancer hlwb. Cov ntaub ntawv tshawb fawb cuam tshuam tau lees paub tias ORM-15341 (Ketodarolutamide) muaj kev sib raug zoo rau cov androgen receptor, nrog ib nrab-qhov siab tshaj plaws inhibitory concentration (IC50) ntawm 38 nanomoles ib liter thiab kev sib tw binding tas li ntawm 8 nanomoles ib liter, ua kom pom kev zoo dua thiab efficacy.

Txawm tias tawm tsam androgen receptor mutants nrog tsis muaj zog ua tau zoo hauv ntau cov khoom siv feem ntau,AWM-15341tseem tuaj yeem siv nws txoj cai tswjfwm ib txwm muaj, tso lub hauv paus kev sim rau nws daim ntawv thov hauv castration- tiv thaiv qog noj ntshav prostate. Tib lub sijhawm, nws tuaj yeem cuam tshuam androgen-induced androgen receptor nuclear translocation, tswj kev ruaj khov autoregulatory kev ua haujlwm txawm nyob rau hauv cov qog nqaij hlav qog nqaij hlav nrog androgen receptor overexpression.

Vim cov ntshav qis- lub hlwb thaiv kev nkag mus ntawm nws cov niam txiv compound ODM-201, Ketodarolutamide tsim yuav luag tsis muaj qhov tseem ceeb hauv lub paj hlwb- cuam tshuam hauv vivo thiab tsis cuam tshuam rau tib neeg androgen tawm tswv yim voj voog. Cov kev tshawb fawb soj ntsuam tau pom tias nyob rau hauv metastatic castration-cov neeg mob qog nqaij hlav qog noj ntshav uas tau kho nrog ODM-201 uas tsis tau txais lwm yam kev kho mob, 86% ntawm cov neeg mob tau ntsib 50% lossis ntau dua qhov txo qis hauv prostate-specific antigen (PSA) qib piv rau lawv cov txiaj ntsig pib. Cov txiaj ntsig zoo no muaj feem cuam tshuam nrog androgen receptor kev tswj hwm kev ua haujlwm hauv ORM-15341 nws tus kheej.

Puas yuav ORM-15341 cuam tshuam rau cov qib androgen hauv lub cev?

Raws li kev tshawb fawb uas twb muaj lawm, ORM-15341 tsis cuam tshuam rau qib androgen hauv lub cev.

Hauv kev tshawb fawb tsiaj tsom rau nws cov niam txiv compound, ODM-201, nws tau pom tias qhov sib xyaw no tsis cuam tshuam nrog androgen tawm tswv yim voj ntawm hypothalamus-pituitary-gonadal axis. Hauv lwm lo lus, ODM-201 thiab nws cov metabolite ORM-15341 (Ketodarolutamide), thaum cuam tshuam nrog androgen receptor signaling, tsis cuam tshuam rau lub cev cov chaw tswj hwm cov tshuaj hormones, thiab yog li ntawd tsis ua rau muaj qhov txawv txav hauv cov qib testosterone qib.

Nws yog ib qho androgen receptor antagonist. Nws cov txheej txheem ntawm kev ua haujlwm yog txhawm rau khi ncaj qha rau androgen receptors, thaiv lub sijhawm rau androgens los khi rau cov receptors, tsis yog cuam tshuam rau androgen synthesis lossis secretion. Cias muab tso, nws tsis txo cov nqi ntawm androgens, tab sis theej occupies lub androgen receptors, tiv thaiv androgens los ntawm khi.

Hom kev ua no ua rauAWM-15341txawv heev los ntawm qee qhov ua ntej los tiv thaiv -androgen cov khoom, thiab yav dhau los siv tau zoo dua.

Tsis tas li ntawd, cov niam txiv sib txuas ntawm ORM-15341, ODM-201, muaj qhov tsis tshua muaj ntshav-hlwb thaiv kev nkag mus, uas ntxiv txo nws qhov cuam tshuam rau hauv nruab nrab paj hlwb thiab cov chaw tswj hwm endocrine.

Hauv cov ntsiab lus, ORM-15341 (Ketodarolutamide) qhov kev txiav txim yog raug txwv rau qib receptor, ua rau nws cov teebmeem tsis cuam tshuam tag nrho cov endocrine tshuav nyiaj li cas thiab pab tswj cov hormonal homeostasis hauv cov neeg mob.

MF ntawm ORM-15341

Melting point	210 - 212C
Boiling point	714.7 ± 60.0℃(Predicted)
Qhov ntom	1.41 ± 0.1 g / cm3 (Tshaj tawm)
Molecular hnyav	396.83
Cia tej yam kev mob	-20℃Lub Freezer, Nyob rau hauv inert cua
Acidity coefficient	8.70±0.10

Specification

Muaj ntau txoj kev xa khoom rau koj xaiv

Peb lub zog:

Peb lub tuam txhab tau dhau los ntawm FDA thiab ISO19001 kev tswj hwm qhov system ntawv pov thawj. Thiab peb muaj kev koom tes nrog kev cog lus nrog ntau lub Hoobkas thiab chaw kuaj hauv Suav teb, Peb lub tuam txhab tuaj yeem muabAWM-15341thiab lwm yam ntawm tus nqi zoo dua. Yog tias koj txaus siab, thov sau ib tsab ntawv.
Peb tsis tsuas yog muaj qhov tshwj xeeb zoo hauv kev thauj mus los, tab sis kuj txhawb ntau txoj hauv kev them nyiaj, txawm tias koj siv nyiaj US, euros, Australian las, lossis cov nyiaj hauv zos los ntawm Singapore, Malaysia, Thaib, thiab lwm yam. Peb kuj tuaj yeem txhawb cov txiaj ntsig hauv zos hauv cov cheeb tsam thiab cov tebchaws no. Tsis tas li ntawd, peb kuj txhawb nqa cov npav hauv txhab nyiaj (credit cards, thiab lwm yam) rau kev them nyiaj.

FAQ:

Q1: Yuav ua li cas zoo yog ORM-15341 hauv inhibiting androgen receptors?
Hauv vitro kev sim cov ntaub ntawv qhia tau hais tias Ketodarolutamide ua tiav ib nrab -qhov siab tshaj plaws inhibitory concentration (IC50) ntawm kwv yees li 38 nanomoles ntawm androgen receptor, sib xws rau kev khi inhibition tas li ntawm 8 nanomoles. Nyob rau hauv tib txoj kev sim, tus nqi sib thooj rau qhov zoo sib xws thib ob- tiam cov khoom xyaw yog 86 nanomoles, qhia tau tias nws txoj kev ua tau zoo rau cov receptor yog ntau dua kaum npaug. Tsis tas li ntawd, nws tswj tau qhov ruaj khov thiab muaj txiaj ntsig zoo tiv thaiv ntau yam receptor variants, ua rau nws haum rau feem ntau siv qhov kev kam rau siab tuaj yeem tsim.
Q2: Qhov zoo ntawm ORM-15341 yog dab tsi?
Cov kev tshawb fawb tau pom tias lub hlwb -rau-plasma concentration ratio ntawm ORM-15341 (Ketodarolutamide) yog qhov qis heev, yog li nws yuav luag tsis nkag mus rau hauv nruab nrab paj hlwb. Yog li ntawd, nws muaj qhov tsis tshua muaj ntshav-hlwb barrier nkag mus, uas yog nws qhov zoo tshaj plaws.
Q3: Yog ORM-15341siv tau thaum siv ib leeg?

AWM-15341tuaj yeem siv ib leeg rau txhua hnub kom siv nws cov teebmeem ncaj qha. Nws tuaj yeem ua haujlwm ruaj khov ntawm cov receptors sib raug zoo, cuam tshuam cov teeb liab cuam tshuam txog kev hloov pauv, thiab tswj hwm lub cev muaj feem cuam tshuam nrog lub cev.

Tsis lees paub: Cov ntaub ntawv luam tawm ntawm lub vev xaib no los ntawm Is Taws Nem, tsis tau txhais hais tias lub vev xaib no pom zoo nrog nws cov kev xav lossis lees paub qhov tseeb ntawm cov ntsiab lus. Thov ua tib zoo saib kom paub qhov txawv. Tsis tas li ntawd, cov khoom muab los ntawm peb lub tuam txhab tsuas yog siv rau kev tshawb fawb tshawb fawb. Peb tsis muaj lub luag haujlwm rau qhov tshwm sim ntawm kev siv tsis raug.

Yog tias koj txaus siab rau peb cov khoom, lossis muaj cov lus qhia tseem ceeb ntawm peb cov khoom lossis tsis txaus siab rau cov khoom tau txais, thov hu rau peb los ntawmEmail :sales6@faithfulbio.com . Peb pab neeg tau cog lus los ua kom tiav kev txaus siab ntawm cov neeg siv khoom.

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