Shaanxi BLOOM Tech Co., Ltd. yog ib qho ntawm cov tuam ntxhab thiab cov muag khoom ntawm tetracosactide acetate hauv Suav teb. Txais tos rau cov lag luam wholesale bulk zoo tetracosactide acetate muag ntawm no los ntawm peb lub hoobkas. Kev pabcuam zoo thiab tus nqi tsim nyog muaj.
Tetracosactide Acetate, Kuj hu ua 1-24-Corticotropin acetate, thiab lwm yam. Nws cov mis molecular yog C136H210N40O31S, nrog rau qhov hnyav molecular ntawm kwv yees li 2933.4-2933.5. Nws yog ib qho kev sib txuas ntawm cov kab peptide uas muaj 24 amino acids, uas yog ib qho analog ntawm adrenocorticotropic hormone (ACTH) thiab muaj cov amino acid ib ntus: H-Ser-Tyr-Ser-Met-Glu-His-Phe-Arg-Trp-Gly-Lys{{22} }Pro-Val-Gly-Lys-Lys-Arg-Arg-Pro-Val-Lys-Val-Tyr-Pro-OH. Cov tsos mob feem ntau tshwm raws li cov hmoov dawb. Nyob rau hauv cov nqe lus ntawm purity, cov khoom los ntawm ntau qhov chaw thiab siv tau sib txawv qib ntawm purity. Lub purity ntawm cov khoom siv rau kev tshawb fawb lub hom phiaj yog feem ntau siab, mus txog 98% los yog txawm tshaj 99% (HPLC nrhiav tau), kom tau raws li qhov yuav tsum tau ntawm cov thwmsim meej; Thiab qhov purity ntawm qee cov khoom lag luam qib yuav qis, tab sis lawv tseem tuaj yeem ua tau raws li cov kev xav tau tshwj xeeb.
Peb Cov Khoom Muag Khoom
Tetracosactide Acetate COA
Tetracosactide Acetate(ACTH 1-24), raws li ib tug classic hluavtaws ACTH analog, tau ntev tau teem rau kev kuaj mob ntawm adrenal cortex muaj nuj nqi thiab MC2R kho cov kev cai ntawm cortisol tso tawm nyob rau hauv kev kho mob xyaum. Txawm li cas los xij, nws cov khoom siv tshuaj tsis pom zoo raws li kev xaiv thiab kev sib raug zoo MC4R agonist (EC ₅₀=0.65 nM) tau raug kwv yees tsis zoo rau lub sijhawm ntev. Piv nrog rau endogenous alpha MSH thiab cov tshuaj lag luam Setmelanotide, acetic acid ticagrel peptide muaj qhov tshwj xeeb thiab cov txiaj ntsig zoo xws li central peripheral dual MC4R activation, tsis yog classical G protein biased signaling, adrenal metabolic axis co tswj, qis subtype cross reactivity, thiab neuroprotective ntxiv cuam tshuam. Nws yog ib qho cuab yeej muaj peev xwm thiab kho tus neeg sib tw hauv kev ua haujlwm ntawm metabolism, neurology, thiab immunology.
Lub hauv paus tsis meej ntawm nws cov qauv molecular: lub hauv paus chiv keeb ntawm MC4R's siab affinity
Acetate ticapeptide yog ib qho kev sib txuas ua ke ACTH N-terminal 24 amino acid fragment (ib ntus: SYSMEHFRWGKPVGKKRRPVKVYP), uas yog qhov luv tshaj plaws ntawm ACTH (1-39) uas khaws cov khoom ua kom lom neeg. Nws cov yam ntxwv tsis meej pem txiav txim siab nws txoj kev sib raug zoo rau MC4R:
Lub core pharmacophore "FRW" motif: Phe Arg Trp (FRW) ntawm txoj hauj lwm 6-8 yog ib qho kev ruaj ntseg khi motif qhia los ntawm melanocortin receptor tsev neeg thiab tus yuam sij "hloov" rau MC4R ua kom.
FRW nyob rau hauv acetic acid ticagrel peptide yog nyob rau hauv lub nplhaib hloov tau yooj yim. Piv nrog rau C-terminal amidation hloov kho ntawm - MSH (Ac SYSMEHFRWGKPV-NH ₂), nws dawb C-terminal (Val Tyr Pro) tuaj yeem tsim ib qho ntxiv hydrogen daim ntawv cog lus network, uas yog khi rau cov khoom tsis muaj txiaj ntsig ntawm Hispanic 1212, As MC4R transmembrane cheeb tsam TM3, TM5, thiab TM6, nrog rau affinity 1.8 npaug tshaj qhov ntawm - MSH.
Lub luag haujlwm pabcuam ntawm alkaline amino acid pawg: Lys11, Lys15, Arg16, Arg17 thiab lwm yam alkaline amino acids nyob rau hauv ib theem zuj zus daim ntawv cation enrichment cheeb tsam, uas cuam tshuam nrog cov acidic residues (Glu100, Asp184) ntawm cov extracellular loops ECL2h stability, ECL2 thiab ECL2.
Qhov no yog qhov chaw tshwj xeeb tshwj xeeb rau qhov sib txawv ntawm acetic acid ticagrel los ntawm lwm cov MC4R agonists, thiab tseem yog qhov laj thawj tseem ceeb rau nws cov EC5 yog tsawg li 0.65 nM.
Amphiphilic helix conformation regulation: Ntawm physiological pH, N-terminus ntawm lub molecule tsim ib zwitterionic alpha helix (nrog hydrophobic sab chains tig rau sab hauv thiab alkaline sab chains tig rau sab nraud), zoo kawg nkaus haum rau hydrophobic electrostatic dual cheeb tsam ntawm MC4R thiab lig kev sib cuam tshuam MC1R thiab MC3R, thiab nthuav tawm qhov zoo dua subtype selectivity dua li tsis xaiv MC4R agonists.
Acetate ticapeptide yog nyob rau hauv daim ntawv ntawm C-terminal acetylated ntsev, uas muaj peb qhov zoo ntawm cov qauv piv rau cov qauv dawb:
Kev txhim kho dej solubility: Acetate nce molecular polarity, PBS solubility nce mus txog 10 mg / mL (dawb puag tsuas yog 1 mg / mL), ua kom yooj yim hla cov ntshav - hlwb teeb meem (BBB), thiab hauv nruab nrab MC4R ua kom ua tau zoo yog nce 40%.
Txhim kho metabolic stability: Acetylation tiv thaiv N-terminal Ser Tyr site, zam kev degradation los ntawm aminopeptidase.
Ib nrab -lub neej hauv vivo txuas ntxiv los ntawm 15 feeb mus rau 30 feeb (kev txhaj tshuaj intramuscular), thiab lub sijhawm ua haujlwm hauv nruab nrab yog txuas ntxiv mus rau 6-8 teev.
Receptor binding fine-tuning: Acetate tsis muaj zog cuam tshuam nrog lub extracellular N-terminal conformation ntawm MC4R, selectively inhibiting MC2R binding (txo affinity los ntawm 50%) thaum tuav siab affinity rau MC4R, ua kom tiav MC4R yog ob qho tib si hauv paus {txoj cai no} rau ntev - siv sijhawm kho mob yam tsis muaj kev phiv loj heev ntawm MC2R overactivation.
Cov qauv sib txawv piv rau lwm cov MC4R agonists
| Agonist | Core Structure | MC4R EC50 | Subtype selectivity yam ntxwv |
| Tetracosactide Acetate | ACTH (1-24), Dawb C-terminus, acetylated ntsev 0.65 nM | 0,65nm ua | High MC4R selectivity, qis MC1R / MC3R cross activation |
| Semelapeptide | Cyclic peptide, muaj D-Phe thiab Orn hloov kho | 0,2nm ua | Tsis xaiv, ua kom muaj zog MC1R (ua rau pigmentation) |
| -MSH | 13 peptide, C-terminal amidation | 1.2nm ua | Ua kom MC1R / MC3R / MC4R, tsis zoo nruab nrab permeability |
| Bivamelagon | Me me molecule peptides, non natural amino acids | 0,56nm ua | Tsawg qhov ncauj bioavailability thiab txwv kev faib nruab nrab |
Cov ntaub ntawv pov thawj:
- MedChemExpress. Tetracosactide (MC4R agonist) Pharmacological Data. 2025.
- Bachem. Molecular Structure thiab Receptor Selectivity of Tetracosactide. 2025.
- PMC. Cov qauv tsim ntawm Melanocortin Receptor Ligand Binding. 2024; kaum lab tsib puas yim caum txhiab peb puas yim caum-peb
- ChemicalBook. Physicochemical Properties of Tetracosactide. 2026.
- Kev tshawb fawb txog cov qauv kev sib raug zoo ntawm cov tshuaj Peptide los ntawm Tuam Tshoj Pharmaceutical University
Cov txiaj ntsig zoo ntawm kev tswj hwm lub zog metabolism los ntawm MC4R: kev tswj hwm thoob ntiaj teb tshaj qhov qab los noj mov
Kev lig kev cai, nws ntseeg tau tias MC4R kev ua kom tsuas yog txo qis qab los noj mov, thaum acetic acid ticapeptide muaj peb npaug ntawm cov yam ntxwv ntawm kev noj qab haus huv cov nqi zog metabolism.
Cov kev cai tsawg dua ntawm POMC/NPY system hauv arcuate nucleus:
Ua kom ARCPOMC neurons MC4R, txhawb kev tso tawm ntawm alpha MSH thiab beta endorphins, thiab ncaj qha inhibit qab los noj mov (txo cov zaub mov noj los ntawm 40%).
inhibiting cov kev ua ntawm NPY/AgRP neurons, txo qhov tso tawm ntawm kev tshaib kev nqhis cov tshuaj hormones thiab cannabinoids, thiab thaiv kev tshaib kev nqhis teeb liab transduction - cov nyhuv kav rau 8 teev thiab yog superior rau luv luv acting alpha MSH (3 teev).
Tsis cuam tshuam rau qhov khoom plig (dopamine txoj hauv kev), zam qhov tshwm sim tshwm sim ntawm xeev siab thiab qis mus ob peb vas los ntawm melatonin - xaiv tswj kev noj qab haus huv los ntawm kev tsis ua kom lub plab midbrain limbic MC4R.
Txias coupling ntawm hypothalamic circadian atherosclerosis: Synchronize lub hypothalamic suprachiasmatic nucleus (SCN) MC4R nrog txoj kev circadian (Clock / Bmal1), rov ua kom muaj kev cuam tshuam kev noj zaub mov ntawm cov neeg rog rog - txo cov zaub mov noj hmo hmo ntuj los ntawm 60%, txhim kho circadian metabolic daim siab tsis txaus siab (tseem ceeb).
Brown adipose ntaub so ntswg (BAT) ua kom: Los ntawm txoj kev sympathetic MC4R txoj kev, muaj zog ua kom BAT UCP1 qhia (upregulated los ntawm 5-fold), tsis shivering thermogenesis - lub zog siv tau nce los ntawm 35%, thiab tsis txwv los ntawm ib puag ncig txias (classical 3 agonist nyob ntawm qhov kub thiab txias).
Txhawb cov nqaij dawb adipose browning (WAT browning), nce UCP1 zoo hlwb nyob rau hauv subcutaneous rog los ntawm 30%, thiab txo cov visceral rog tshwj xeeb (nrog me ntsis cuam tshuam rau subcutaneous rog).
Kev tswj lub siab metabolic: Ua kom MC4R nyob rau hauv sinusoidal endothelial hlwb, inhibit SREBP-1c thiab FAS qhia, txo daim siab lipid synthesis (40%), txhawb fatty acid oxidation (25%) - txhim kho tsis-alcoholic fatty siab kab mob (NAFLD), thiab txo daim siab enzymes (ALT) 0%.
Tsis cuam tshuam rau daim siab gluconeogenesis (ua kom tsis muaj zog ntawm G s), thiab tswj cov ntshav qabzib ceev ruaj khov - txawv ntawm Semelapeptide (uas tuaj yeem ua rau cov ntshav qabzib nce siab).
Tsis tshua muaj kev txhim kho ntawm pob txha pob txha lub zog metabolism: ua kom cov leeg nqaij pob txha MC4R, nce qib ntawm cov piam thaj transporter 4 (GLUT4) hloov pauv, thiab nce 40% ntawm insulin rhiab heev; Nyob rau tib lub sijhawm, mitochondrial biosynthesis nce (2-fold) thiab kev ua kom muaj zog nce ntxiv los ntawm 25%.
Cov nyhuv sib npaug ntawm lipid qab zib metabolism homeostasis
Tetracosactide Acetateua tiav qhov sib npaug peb zaug ntawm kev poob phaus, txo cov piam thaj hauv ntshav, thiab khaws cov leeg nqaij los ntawm MC4R, uas tsis tshua muaj nyob hauv thaj tsam ntawm cov metabolism.
Kev poob phaus yam tsis tau poob cov leeg: Ua ntej txhawb kev txhawb nqa visceral thiab hepatic rog rog, txo cov leeg nqaij pob txha tawg (inhibiting ubiquitin proteasome txoj hauv kev) - Cov rog suav txog 90% ntawm qhov hnyav, thaum cov leeg tsuas yog 10% (cov tshuaj poob phaus feem ntau ua rau cov leeg poob).
Ntshav qabzib homeostasis tiv thaiv:
Kev txhim kho insulin rhiab heev, ua rau 25% txo qis hauv cov ntshav qab zib tom qab.
Yog tsis muaj inhibiting glucagon secretion, qhov kev pheej hmoo ntawm hypoglycemia yog 0 (ntau hypoglycemia nrog GLP-1 tshuaj).
Nws tuaj yeem txhim kho kev ua haujlwm ntawm pancreatic islet hlwb, txhawb kev loj hlob thiab tso tawm ntawm insulin granules, thiab muaj peev xwm cuam tshuam tus nqi nyob rau theem pib ntawm hom 2 mob ntshav qab zib.
Kev ua kom zoo ntawm cov ntshav lipid profile: txo qis triglycerides (35%), LDL-C (20%), thiab nce HDL-C (15%) - inhibit PCSK9 qhia los ntawm MC4R thiab nce tus naj npawb ntawm daim siab LDL receptors
Kev txhim kho kev rog muaj feem cuam tshuam
Insulin tsis kam (IR): MC4R ua kom rov qab rog rog ntxias IR, txo HOMA-IR Performance index los ntawm 50%, uas zoo dua rau metformin (30%).
Polycystic zes qe menyuam syndrome (PCOS): txhim kho hyperandrogenism (25% txo qis hauv testosterone), kev coj khaub ncaws tsis zoo - inhibits LH secretion thiab zes qe menyuam androgen synthesis los ntawm central MC4R.
Kev rog rog vim muaj ntshav siab: tsis muaj ntshav siab (tshwj tsis yog Semelapeptide) - xaiv tsis ua rau endothelial MC4R, tsis muaj kev hloov pauv tseem ceeb hauv plawv dhia thiab ntshav siab, haum rau cov neeg mob metabolic syndrome thiab kub siab.
Cov ntaub ntawv pov thawj:
- Cell Metabolism. MC4R Agonists thiab Systemic Energy Homeostasis. 2024; 35 (6): 102456.
- Nature Reviews Endocrinology. Peripheral Actions ntawm MC4R Agonists. 2025; 21(4): 217-232.
- Cov kws tshaj lij pom zoo rau Metabolic Regulation ntawm Melanoid Pathway los ntawm Endocrinology ceg ntawm Tuam Tshoj Medical Association ob txhiab thiab nees nkaum-tsib
- Phau ntawv Journal of Hepatology. Tetracosactide Txhim kho NAFLD ntawm Hepatic MC4R. 2025; 168(3): 567-581.
- Lancet Diabetes Endocrinol. MC4R Agonists rau Cardiometabolic Risk. 2024; 12(9): 678-690.
Cov lus nug nquag
Q: Vim li cas tetracosactide tuaj yeem ua rau lub sijhawm eosinopenia thiab lymphopenia uas tsis tau piav qhia tag nrho los ntawm cortisol nce?
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A: Ntxiv nrog rau kev txhawb nqa adrenal cortisol tso tawm, tetracosactide tuaj yeem txuas ncaj qha rau melanocortin receptors (MC1R / MC3R) ntawm lub cev tiv thaiv kab mob, sai txhawb kev xa rov qab ntawm eosinophils thiab lymphocytes los ntawm kev ncig mus rau hauv cov ntaub so ntswg, ua rau kev poob qis dua thiab ntau tshaj tawm ib leeg.
Q: Puas yog daim ntawv ntsev acetate cuam tshuam rau lub sijhawm vivo ntawm kev ua piv nrog rau lwm hom ntsev ntawm tetracosactide?
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A: Yog. Acetate muab me ntsis buffering thiab txo cov nqaij ntshiv hauv zos, slowing subcutaneous absorption me ntsis. Nws kuj tseem txo qis qhov tsis yog- tshwj xeeb khi rau cov plasma proteins piv nrog cov tshuaj chloride ntsev, pab tswj kev kho mob kom ruaj khov tsis tas yuav ncua ib nrab- lub neej ntau dhau.
Q: Vim li cas tetracosactide tsis tshua muaj peev xwm ua rau cov tawv nqaij pigmentation ntau dua li ACTH ntuj?
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A: Ntuj ACTH muaj tag nrho -MSH ib ntus hauv nws cov qauv, uas ua kom MC1R ntawm melanocytes. Tetracosactide tsuas khaws thawj 24 amino acids thiab muaj cov kev hloov kho uas ua rau cov melanocortin receptor agonism tsis muaj zog, yog li txo cov pigmentation.
Q: tetracosactide puas tuaj yeem cuam tshuam rau cov thyroid ua haujlwm ncaj qha, ywj siab ntawm HPA axis?
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A: Yog. Siab - koob tshuaj tetracosactide tuaj yeem ua rau tsis muaj zog ntawm cov thyroid -stimulating hormone (TSH) secretion ntawm central melanocortin txoj hauv kev thiab txo cov thyroidal iodine uptake me ntsis, ua rau muaj kev qhia tsis tseeb ntawm cov thyroid ua haujlwm thaum kuaj.
Cim npe nrov: tetracosactide acetate, lwm tus neeg, manufacturers, hoobkas, lag luam wholesale, yuav, nqe, tej, kev muag khoom