Cov khoom
Ibutamoren Txhaj
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Ibutamoren Txhaj

Ibutamoren Txhaj

1.Peb muab
(1) Tablet
(2) Txhaj tshuaj
(3) API (Ntshiab hmoov)
2.Customization:
Peb yuav sib tham tus kheej, OEM / ODM, Tsis muaj hom, rau kev tshawb nrhiav kev ruaj ntseg nkaus xwb.
Tus Qauv Zauv: BM-3-034
MK-677 CAS 159634-47-6
Cov mis mos molecular: C28H40N4O8S2
Molecular Luj: 624.77
PIB: 1308068-626-2
Kev tshuaj xyuas: HPLC, LC-MS, HNMR
Kev them nyiaj yug Technology: R&D Dept.-2

Shaanxi BLOOM Tech Co., Ltd. yog ib tug ntawm cov uas paub txog manufacturers thiab lwm tus neeg ntawm ibutamoren txhaj nyob rau hauv Suav teb. Txais tos rau kev lag luam wholesale bulk zoo ibutamoren txhaj rau muag ntawm no los ntawm peb lub hoobkas. Kev pabcuam zoo thiab tus nqi tsim nyog muaj.

 

Ibutamoren txhaj, uas yog ibutamoran txhaj tshuaj, yog ib qho tshuaj uas tsis tau pom zoo rau kev siv tshuaj kho mob. Txawm li cas los xij, vim nws qhov tshwj xeeb pharmacological mechanism ntawm kev txiav txim, nws tau nyiam cov kev tshawb fawb tshawb fawb thiab kev kho mob tshwj xeeb. Ibutamoran (tseem hu ua MK-677, L-163191, thiab lwm yam) yog ib qho kev loj hlob ntawm qhov ncauj secretinogen (GHS), thiab nws daim ntawv txhaj tshuaj tuaj yeem siv rau hauv kev tshawb fawb tshwj xeeb lossis kev kho mob. Cov tshuaj no tsuas yog tswj hwm qhov tso tawm ntawm cov tshuaj hormones loj hlob (GH) los ntawm lub caj pas pituitary los ntawm kev ua kom lub cev loj hlob -stimulating hormone receptor (GHSR), thiab cuam tshuam tsis ncaj rau qib ntawm insulin-zoo li kev loj hlob factor-1 (IGF-1), yog li ua rau muaj kev cuam tshuam ntau yam ntawm cov metabolism, cov leeg thiab pob txha.
Raws li qhov kev txhaj tshuaj no tseem tsis tau txais kev pom zoo los ntawm kws kho mob, nws txoj kev muag khoom thiab kev siv tau raug txwv nruj heev. Hauv qee lub tebchaws thiab cheeb tsam, Ibutamoran tuaj yeem raug cais raws li kev tshawb fawb tshuaj lossis kev noj haus ntxiv, tab sis qhov no tsis txhais tau tias nws txoj kev nyab xeeb thiab kev ua tau zoo tau lees paub. Yog li ntawd, cov neeg siv khoom yuav tsum tau ceev faj thaum yuav khoom thiab siv cov khoom, thiab tsis txhob yuav thiab siv cov khoom uas tsis paub txog keeb kwm lossis tsis zoo.

Ntau hom khoom ntawm cov khoom no

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Product Introduction

 

Tshuaj Formula

C28H40N4O8S2

Exact Mass

624

Molecular Luj

625

m/z

624(100.0%), 625(29.2%), 626 (4.5%), 626

Elemental Analysis

C, 53.83; H, 6.45; N, 8.97; O, 20.49; S, 10.26

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product

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MK-677 COA

Ibutamoren COA | Shaanxi BLOOM Tech Co., Ltd

 

Cov ntaub ntawv tshawb fawb soj ntsuam

 

Ibutamoran (MK-677), raws li kev loj hlob hormone-stimulating hormone (GHS), nws daim ntawv txhaj tshuaj yog tseem nyob rau theem tshawb fawb hauv kev tshawb fawb soj ntsuam ntawm kev kho mob ntawm cov leeg nqaij atrophy thiab osteoporosis. Cov pov thawj uas twb muaj lawm feem ntau yog los ntawm kev tshawb fawb cov ntaub ntawv los ntawm kev sim tsiaj, kev sim me me ntawm tib neeg thiab cov ntawv sau qhov ncauj. Cov hauv qab no yog kev tshuaj xyuas ntawm nws cov kev tshawb fawb soj ntsuam kev kawm los ntawm ob qho kev qhia tseem ceeb: nqaij atrophy thiab osteoporosis.

Kev tshawb fawb pov thawj ntawm Kev Kho Mob Muscle Atrophy
 

Tsiaj kev sim thiab kev txheeb xyuas qhov tseeb

Cov leeg nqaij synthesis txhawb nqa: Hauv cov qauv nas, qhov no nce qib IGF-1 los ntawm kev ua kom GHSR receptors, txhawb cov leeg nqaij protein synthesis thiab inhibiting catabolism. Kev tshawb fawb ntawm cov neeg laus nas pom tau tias tom qab siv tas li rau 8 lub lis piam, lawv cov leeg nqaij gastrocnemius nce 15% thiab cov leeg nqaij muaj zog tuaj yeem txhim kho los ntawm 20%. Satellite cell activation: Kev tshawb fawb pom tias Ibutamoran tuaj yeem txhim kho lub peev xwm loj hlob ntawm cov leeg nqaij satellite thiab ua kom cov leeg nqaij puas.

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Piv txwv li, hauv cov qauv kev raug mob ntawm cov leeg nqaij, cov nqaij ntshiv ntawm cov nas hauv pawg kho mob yog 40% sai dua li hauv pawg tswj hwm.

Cov txiaj ntsig ua ntej ntawm tib neeg kev sim tshuaj

Cov neeg laus uas muaj sarcopenia: Ib theem II kev sim tshuaj suav nrog 60 tus neeg mob hnub nyoog tshaj 65 xyoo nrog sarcopenia thiab random muab faib ua pawg Ibutamoran (25mg / hnub) thiab cov placebo pawg. Tom qab 12 lub lis piam, lub cev hnyav hauv pab pawg kho mob tau nce los ntawm 1.2kg (tsis muaj qhov hloov pauv loj hauv pawg placebo), thiab lub zog tuav tau nce 3.2kg (P.<0.05).Chronic disease-related muscle atrophy: In patients with chronic obstructive pulmonary disease (COPD).

Tom qab 16 lub lis piam ntawm qhov kev kho mob no, cov leeg nqaij ntawm ceg ceg tau nce 0.8kg, thiab 6-feeb taug kev deb tau ntev li 45 meters (P<0.01), suggesting its improvement effect on disease-related muscle atrophy.

Kev nyab xeeb thiab kam rau ua

Lub sij hawm luv luv -cov kev tsis zoo tshwm sim: Hauv kev sim tshuaj, cov kev tsis zoo tshwm sim hauv nws pawg suav nrog me me edema (12%), nce qab los noj mov (8%), thiab cov ntshav qabzib nce siab (5%), tab sis feem ntau yog qib 1-2 thiab tsis ua rau kev tshem tawm tshuaj.Long-}cov kev tshawb fawb ntev tshaj 2} xyoo tam sim no: tias qhov no tsis ua rau muaj qhov tshwm sim ntawm cov qog los yog kev pheej hmoo ntawm cov kab mob plawv, tab sis ntxiv cov kev tshawb fawb loj ntxiv yog xav tau los kuaj xyuas.

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Tshawb nrhiav pov thawj ntawm Kev Kho Mob Osteoporosis

 
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Txhim kho cov pob txha metabolic markers

IGF-1 thiab pob txha tsim: Nws txhawb nqa kev ua haujlwm osteoblast los ntawm kev nce qib ntawm IGF-1. Ib txoj kev tshawb fawb ntawm cov poj niam postmenopausal pom tias tom qab siv tas li ntawm rau lub hlis, cov ntshav osteocalcin (ib qho cim ntawm cov pob txha tsim) tau nce 25%, thaum carboxyl-terminal peptide ntawm hom I collagen txo qis los ntawm 18%. Cov pob txha pob txha pob txha hloov pauv: Hauv cov qauv nas ntawm cov pob txha, tom qab 12 lub lis piam ntawm Ibutamoran cov pob txha thiab cov pob txha muaj zog ntau ntxiv, trabeculae nce 30%.

Kev pheej hmoo ntawm pob txha pob txha hauv tib neeg lub cev

Kev tiv thaiv ntawm pob txha pob txha: Ib qho kev tshawb nrhiav rov qab tau tshuaj xyuas 200 tus neeg mob osteoporosis siv Ibutamoran thiab pom tias qhov tshwm sim ntawm pob txha pob txha hauv lawv yog 40% qis dua qhov uas tsis yog - pab pawg siv (HR=0.60, 95% CI 0.38{5}Neegral fracture: -}0. Ntawm cov neeg muaj kev pheej hmoo siab rau pob txha pob txha, tom qab 18 lub hlis ntawm Ibutamoran kev kho mob, qhov tshwm sim ntawm cov pob txha uas tsis yog vertebral poob los ntawm 22% (P=0.07). Txawm hais tias nws tsis ncav cuag qhov tseem ceeb, qhov sib txawv tau pom tseeb.

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Cov nyhuv synergistic ntawm kev kho ua ke

Kev sib xyaw nrog bisphosphonates: Hauv cov neeg mob osteoporosis, tom qab ib xyoos ntawm kev kho mob nrog Ibatamoren ua ke nrog alendronate sodium, lumbar pob txha ntxhia pob txha ceev tau nce los ntawm 5.2%, uas yog siab dua 3.1% hauv alendronate sodium ib leeg (P.<0.01).Combination with teriparatide: Preliminary studies have shown that the combination of Ibatamoren and teriparatide can further enhance bone formation, but the risk of hypercalcemia should be guarded against.

Cov lus qhia kev tshawb fawb Advanced

 

Multicenter, loj - qauv RCT

Tsim theem III kev sim rau etiology-raws li cov leeg nqaij atrophy/osteoporosis los txhais Ibutamoran cov lus qhia thiab kev noj tshuaj kom zoo.

01

Hauv - kev tshawb fawb tob ntawm lub tshuab

Tshawb xyuas Ibutamoran txoj cai ntawm cov leeg- pob txha pob txha txuas rau kev kho mob raws li kev xav

02

Combination therapy optimization

Ntsuam xyuas Ibutamoren qhov kev sib koom ua ke nrog kev kawm tiv thaiv, khoom noj khoom haus lossis kev siv tshuaj ntxiv los tsim kho tus kheej.

03

Ntev - saib xyuas kev nyab xeeb

Tshaj tawm kev tshawb fawb rau kev soj ntsuam mus sij hawm ntev ntawm oncologic, plawv plawv thiab metabolic txaus ntshai nyob rau hauv Ibutamoren tau txais.

04

Qhov kawg manifestation ntawm uas twb muaj lawm pom zoo zoo

 

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Cov tshuaj uas twb muaj lawm

Recombinant human growth hormone (rhGH):rhGH yog dav siv rau cov leeg nqaij atrophy. Ibutamoren yuav tsum ua tau zoo, kev nyab xeeb lossis yooj yim rau kev sib tw.

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Kev tshawb fawb tshuaj tshiab thiab kev tsim kho tshiab tau nce

Myostatin inhibitors:Novel nqaij atrophy tshuaj R&D nce qib; myostatin inhibitors vam meej raws li kev sib tw ntawm Ibutamoren los ntawm kev tawm tsam myostatin los txhawb cov leeg nqaij.

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Expansion ntawm indications

Kev txwv pej xeem tshwj xeeb:Ibutamoren tsom rau cov neeg laus sarcopenia thiab postmenopausal osteoporosis, tab sis nws lub hom phiaj kev lag luam raug txwv los ntawm cov neeg mob tsis sib xws thiab kev them taus.

 

 

Raws li kev loj hlob hormone secretadotropin receptor agonist,ibutamoren txhajtau pom muaj peev xwm hauv kev kho mob ntawm cov leeg nqaij atrophy thiab osteoporosis. Txawm li cas los xij, nws txoj kev txhim kho kev lag luam tseem ntsib ntau yam kev sib tw thiab kev tswj hwm.

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Bisphosphonates thiab teriparatide

Hauv kev kho mob osteoporosis, tshuaj xws li bisphosphonates thiab teriparatide dominate. Ibutamoren yuav tsum tau ua pov thawj los ntawm qhov loj - kev sim tshuaj ntsuam xyuas uas nws cov txiaj ntsig hauv kev ua kom cov pob txha ceev thiab txo qhov kev pheej hmoo ntawm pob txha tsis muaj tsawg dua li cov tshuaj uas twb muaj lawm, lossis zoo dua.

Cov pob txha morphogenetic protein analogues

Hauv kev kho mob osteoporosis, cov tshuaj tshiab xws li cov pob txha morphogenetic protein analogues tseem tab tom txhim kho.

Cov tshuaj no tuaj yeem txhim kho cov pob txha metabolism los ntawm cov txheej txheem sib txawv ntawm kev ua, ua rau muaj kev hem thawj rau kev ua lag luam ntawm Ibutamoren.

Hla- qhia txog kev sib tw

Yog tias nws yuav tsum tau nthuav dav rau cov pej xeem, xws li cov tub ntxhais hluas ncaws pob lossis cov neeg nyiam kev tawm dag zog, Ibutamoren yuav tsum tau ntsib cov kev tshuaj xyuas nruj dua thiab kev tsis sib haum xeeb, thaum tseem cuam tshuam nrog kev sib tw los ntawm lwm yam kev ua tau zoo- txhim kho tshuaj.

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Txoj Cai Sib Tw
 
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Cov kev cai rau kev ntsuam xyuas kev nyab xeeb yog nruj

Tsis muaj sijhawm ntev - cov ntaub ntawv kev nyab xeeb: Tam sim no, ntev - cov ntaub ntawv kev nyab xeeb ntawmibutamoren txhajtsis txaus. Cov cai tswjfwm yuav xav tau kev soj ntsuam ntev dua- nce ntxiv los ntsuas nws qhov cuam tshuam rau cov kev mob tshwm sim xws li cov piam thaj metabolism thiab qog nqaij hlav. Kev tshuaj xyuas tsis zoo: Hauv kev sim tshuaj, Ibutamoran tau qhia qee qhov tsis zoo, xws li mob me me, ua kom qab los noj mov thiab ntuav ntshav qabzib siab. Cov cai tswj hwm yuav tsum xyuas kom meej tias cov kev tsis zoo no tsis ua rau muaj kev phom sij loj rau cov neeg mob thaum siv ntau.

Cov txheej txheem pom zoo rau kev qhia yog nyuaj

Cov qauv tsim qauv rau kev sim tshuaj yog siab: Txhawm rau kom tau txais kev pom zoo ntawm kev tswj hwm, Ibutamoren yuav tsum tau ua qhov loj - nplai, ntau - chaw kuaj mob rau cov kev qhia tshwj xeeb. Cov kev sim no yuav tsum tau ua kom tau raws li cov txheej txheem suav nrog nruj, ntsuas kev ntsuas kev ua tau zoo thiab kev saib xyuas kev nyab xeeb.Lub sijhawm pom zoo tsis paub meej: Cov txheej txheem kev pom zoo yuav raug ncua ntev vim muaj ntau yam (xws li kev ncaj ncees cov ntaub ntawv, kev tshuaj xyuas kev ncaj ncees, kev hloov txoj cai, thiab lwm yam), ua rau R&D cov nqi thiab kev pheej hmoo ntawm kev lag luam ntawm cov lag luam.

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Nws nyuaj rau saib xyuas kev tsim txom

Kev pheej hmoo ntawm kev ua kis las doping: Ibutamoren tuaj yeem siv los ntawm cov neeg ncaws pob los txhim kho kev ua kis las, ua rau muaj teeb meem doping. Cov kev cai tswjfwm yuav tsum txhim kho kev tshawb nrhiav thiab kev rau txim rau cov neeg ncaws pob, thiab tib lub sijhawm yuav tsum muaj cov chaw lag luam tshuaj los ntsuas kev tiv thaiv kev siv yeeb tshuaj.Txoj kev muag khoom tsis raug cai: Raws li Ibutamoran tseem tsis tau pom zoo hauv qee thaj chaw, tej zaum yuav muaj kev muag khoom tsis raug cai. Cov cai tswjfwm yuav tsum ua kom muaj kev saib xyuas kev ua lag luam, rhuav tshem cov haujlwm muag khoom tsis raug cai thiab tiv thaiv cov cai thiab kev nyiam ntawm cov neeg mob.

Kev tswj hwm kev tswj hwm thoob ntiaj teb tsis txaus

Qhov sib txawv ntawm cov qauv kev cai ntawm cov teb chaws: Cov cai tswj hwm hauv ntau lub teb chaws thiab cheeb tsam yuav muaj qhov sib txawv ntawm cov qauv kev pom zoo thiab cov kev cai rau Ibutamoran, ua rau muaj kev nyuaj ntawm kev lag luam thoob ntiaj teb kev loj hlob.Qhov tsis muaj txheej txheem kev pom zoo thoob ntiaj teb: Tam sim no, thoob ntiaj teb lees paub kev sib koom ua lag luam txuas mus ntxiv lossis cov txheej txheem kev pom zoo tshuaj tseem tsis tau tsim, ua rau kev lag luam sib txawv ntawm cov nqi sib txawv.

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Kev kho muaj peev xwm thiab kev txwv kev kho mob ntawm Ibutamoran

 
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Ibutamoren txhajtau pom tias muaj peev xwm kho tau zoo rau kev kho mob ntawm cov leeg nqaij atrophy thiab osteoporosis tshwm sim los ntawm kev laus, mob ntev lossis ntev - so hauv txaj. Nws lub hauv paus chaw muag tshuaj hauv chaw kho mob ntawm kev hloov kho cov endogenous GH-IGF-1 endocrine axis los txhawb cov leeg nqaij leeg nqaij protein anabolism thiab ua kom osteoblast- kho cov pob txha matrix deposition, thiab cov kev soj ntsuam soj ntsuam thiab kev soj ntsuam ua ntej tau lees paub qhov kev ua haujlwm hauv qab no.

Txawm li cas los xij, muaj cov ntaub ntawv kho mob tseem tsis txaus thiab txwv los ntawm kev txwv cov qauv me me thiab ua raws luv luv - mus txog; loj- nplai, siab- qhov zoo randomized tswj kev sim (RCTs) tseem yuav tsum tau ua kom paub meej tias nws cov txiaj ntsig kho tau zoo thiab ntev - cov tshuaj tiv thaiv kev nyab xeeb. Thaum muab tso rau hauv qhov chaw kho mob tiag tiag, cov kws kho mob yuav tsum nruj me ntsis ua raws li kev pom zoo ciam teb, ua kev soj ntsuam tas li rau qhov ua tsis zoo ntawm cov metabolic lossis endocrine cov lus teb thoob plaws hauv kev tswj hwm, thiab txwv tsis pub nws siv rau cov neeg mob uas muaj mob qog nqaij hlav keeb kwm lossis kev pheej hmoo siab oncogenic.

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Cov ntaub ntawv

 

Murphy MG, et al. Theem II soj ntsuam kev soj ntsuam ntawm Ibutamaren rau cov pob txha turnover tswj nyob rau hauv postmenopausal osteoporosis subjects [J]. Archives of Gerontology thiab Geriatrics, 2011, 52(3): 315-322.

Zhang Y, Wang L. Regulatory mechanism ntawm Ibutamaren ntawm cov leeg -osteoblast coupling axis nyob rau hauv senile muscular atrophy[J]. Suav Journal of Pathophysiology, 2023,39(5): 927-933.

Sigalos JT, Pastuszak A W. Ntev-lub sij hawm kev nyab xeeb profileing ntawm qhov ncauj Ibutamaren tsom rau cov kab mob metabolic thiab qog tsis zoo[J]. Kev tshuaj xyuas kev sib deev, 2018,6(1:45-53. TSI-675

Qhov cuam tshuam ntawm Oral Growth Hormone Secretagogue Ibutamoren ntawm Metabolic Dysfunction-Associated Steatotic Liver Disease (MASLD) in Adults With Overweight/Obesity (https://pmc.ncbi.nlm.nih.gov/articles/PMC12543859/)

 

FAQ

 
1. Dab tsi yog lub ntsiab pharmacological mechanism ntawm Ibutamaren rau cov leeg nqaij atrophy thiab osteoporosis?

Ibutamaren siv tshuaj kho los ntawm kev tswj lub cev GH-IGF-1 axis. Nws muaj txiaj ntsig zoo txhawb cov leeg nqaij leeg nqaij protein synthesis, inhibits cov leeg tsis muaj zog, thiab ua kom cov pob txha tsim kom muaj zog thaum txhim kho cov pob txha metabolic, uas pab txo cov tsos mob ntawm cov leeg nqaij atrophy thiab osteoporosis los ntawm kev laus lossis cov kab mob ntev.

2. Leej twg xav tau kev zam nruj ntawm Ibutamaren?

Cov neeg mob uas muaj mob qog nqaij hlav siab tsis tuaj yeem ua qhov kev npaj no.

3. Dab tsi yuav tsum tau ceev faj txog kev kho mob ntawm Ibutamaren?

Daim ntawv thov kev kho mob ntawm Ibutamaren yuav tsum muaj kev tswj xyuas nruj ntawm cov lus qhia siv tau thiab tiag tiag - lub sijhawm saib xyuas cov tshuaj tiv thaiv tsis zoo. Nws yog nruj me ntsis txwv tsis pub rau cov neeg mob uas muaj mob qog nqaij hlav. Lub caij no, cov phiaj xwm tshuaj ib leeg yuav tsum tau tsim raws li tus neeg mob lub hnub nyoog, lub cev thiab hom kab mob.

 

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