Amunine, Kuj hu ua CRF (Ovine) Trifluoroacetate, nws yog ib daim ntawv trifluoroacetate ntawm corticotropin releasing factor (CRF) muab rho tawm los ntawm yaj thiab synthesized. Nws feem ntau tshwm dawb, uas yog xim xim hauv nws lub xeev ntshiab. Qee qhov xwm txheej, vim qhov sib txawv ntawm cov txheej txheem kev npaj lossis kev cia khoom, cov xim yuav txawv me ntsis, tab sis feem ntau tseem nyob hauv thaj tsam ntawm dawb mus rau dawb. Cov tshuaj no feem ntau yog nyob rau hauv daim ntawv hmoov, ua rau nws yooj yim rau khaws thiab siv. Tsis tas li ntawd, nws kuj tseem tuaj yeem muaj nyob hauv daim ntawv khov- cov hmoov qhuav, uas pab tswj nws txoj kev ruaj khov thiab kev ua haujlwm. Nws lub ntsiab physiological muaj nuj nqi yog los txhawb kev tso tawm ntawm adrenocorticotropic hormone (ACTH) los ntawm lub caj pas anterior pituitary. ACTH txuas ntxiv ua haujlwm ntawm adrenal cortex, txhawb kev sib txuas thiab tso tawm ntawm glucocorticoids xws li cortisol. Cov txheej txheem no yog ib qho tseem ceeb ntawm cov hypothalamic pituitary adrenal axis (HPA axis), uas yog ib qho tseem ceeb rau kev tswj lub cev kev ntxhov siab, lub zog metabolism, thiab kev tiv thaiv kab mob.
Peb Cov Khoom Muag Khoom
Amunine COA
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| Certificate of Analysis | ||
| Compound npe | CRF (Ovine) Trifluoroacetate | |
| Qib | Pharmaceutical qib | |
| CAS Nr. | 79804-71-0 | |
| Ntau | 15g | |
| Ntim txheem | PE hnab + Al foil hnab | |
| Chaw tsim tshuaj paus | Shaanxi BLOOM TECH Co., Ltd | |
| Ntau No. | 202501090026 | |
| MFG | Peb 9, 2025 | |
| EXP | Peb 8, 2028 | |
| Qauv |
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| Yam khoom | Enterprise txheem | Kev txheeb xyuas qhov tshwm sim |
| Qhov tshwm sim | Dawb los yog yuav luag dawb hmoov | Ua raws |
| Cov ntsiab lus dej | Tsawg dua lossis sib npaug li 5.0% | 0.39% |
| Poob rau ziab | Tsawg dua lossis sib npaug li 1.0% | 0.26% |
| Hnyav Hlau | Pb Tsawg dua lossis sib npaug li 0.5ppm | N.D. |
| Tsawg dua lossis sib npaug li 0.5ppm | N.D. | |
| Hg Tsawg dua lossis sib npaug li 0.5ppm | N.D. | |
| Cd Tsawg dua lossis sib npaug li 0.5ppm | N.D. | |
| Purity (HPLC) | Ntau dua lossis sib npaug li 99.0% | 99.99% |
| Ib leeg impurity | <0.8% | 0.53% |
| Tag nrho microbial suav | Tsawg dua lossis sib npaug li 750cfu / g | 99 |
| E. Coli | Tsawg dua lossis sib npaug li 2MPN / g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (los ntawm GC) | Tsawg dua lossis sib npaug li 5000ppm | 400ppm ua |
| Cia | Khaws rau hauv qhov chaw kaw, tsaus, thiab qhuav hauv qab -20 degree | |
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| Tshuaj Formula | C205H339N59O63S |
| Exact Mass | 4667.49 |
| Molecular Luj | 4670.38 |
| M/Z | 4669.49 (100.0%),4668.49 (90.6%),4670.50 (73.1%),4667.49 (40.9%),4671.50 (39.5%),4670.49 (21.8%),4669.49 (19.8%),4672.50 (16.2%),4671.50 (12.9%),4670.49 (11.7%),4671.49 (11.3%),4668.48 (8.9%),4672.50 (5.7%),4669.49 (5.3%),4671.49 (4.6%),4671.49 (4.5%),4673.50 (4.3%),4670.48 (4.1%),4673.51 (3.9%),4672.50 (3.6%),4672.50 (3.1%),4672.50 (2.9%),4672.49 (2.3%),4669.48 (1.8%),4673.49 (1.8%),4671.49 (1.6%),4670.48 (1.3%) |
| Elemental Analysis | C,53.69; H,6.87; N,19.50; O,17.59; S,2.35 |
Amunine(CRF (Ovine)Trifluoroacetate) yog ib qho tseem ceeb ntawm kev tswj hwm molecule ntawm hypothalamic pituitary adrenal axis (HPA axis) hauv cov tsiaj, ua lub luag haujlwm tseem ceeb hauv kev ntxhov siab, kev tswj kev xav, thiab kev sib npaug ntawm metabolic. CRF (Ovine) Trifluoroacetate, raws li CRF analogue muab los ntawm yaj, tau dhau los ua cov cuab yeej tseem ceeb rau kev kawm txog kev ua haujlwm ntawm lub cev ntawm CRF thiab kev tsim tshuaj vim nws qhov tshwj xeeb thiab ruaj khov.
Molecular hauv paus thiab tshuaj hloov kho ntawm CRF (Ovine)
Keeb kwm thiab cov yam ntxwv ntawm natural CRF
CRF tau pib cais tawm thiab ntxuav tawm ntawm cov yaj hypothalamus los ntawm Vale thiab lwm tus kws tshawb fawb hauv xyoo 1981. Nws cov amino acid ib ntus yog:
H-Ser-Gln-Glu-Pro-Pro-Ile-Ser-Leu-Asp-Leu-Thr{{ 11}}Ph-His-Leu-Leu-Arg-Glu-Val-Leu-Glu-Met{21 }}Thr-Lys-Ala-Asp-Gln-Leu-Ala-Gln-Gln-Ala- Nws-Ser-Asn-Arg-Lys-Leu-Leu-Asp-Ile-Ala-NH2
Cov kab ke no muaj 41 amino acids nrog qhov hnyav molecular ntawm kwv yees li 4.7 kDa, nrog serine (Ser) ntawm N-terminus thiab alanine (Ala) amidation modification ntawm C-terminus. Cov amino acid homology ntawm yaj CRF thiab tib neeg CRF yog 95%, tsuas yog qhov sib txawv ntawm txoj haujlwm 7, 10, 13, 16, 21, 23, 26, 28, 31, 34, thiab 38, tab sis cov haujlwm tseem ceeb heev.
Cov tshuaj tseem ceeb ntawm kev hloov kho Trifluoroacetate
CRF (Ovine) Trifluoroacetate (CAS naj npawb: 79804-71-0) yog cov ntsev ntsev tsim los ntawm kev sib txuas cov carboxyl kawg ntawm CRF nrog trifluoroacetic acid (TFA). Qhov zoo ntawm TFA hloov kho muaj xws li:
Txhim kho kev solubility: Cov pab pawg muaj zog acidic (- COCF ∝) ntawm TFA tuaj yeem ua kom cov kuab tshuaj peptides nyob rau hauv cov kuab tshuaj organic, ua kom yooj yim rau kev sim ua haujlwm.
Cov qauv peptide ruaj khov: TFA txo qis peptide aggregation thiab degradation los ntawm kev tsim cov ntsev txuas hniav, ua kom ntev ib nrab - lub neej.
Tswj kev ua haujlwm lom neeg: Hloov kho CRF tseem tuaj yeem khi rau CRF receptor (CRFR), khaws cov yam ntxwv ua haujlwm ntawm ntuj molecules.
Synthesis Method thiab Kev Tswj Xyuas Zoo
CRF (Ovine) Trifluoroacetate feem ntau yog npaj los ntawm cov khoom siv -theem peptide synthesis (SPPS), qhov twg cov amino acid sab chains tiv thaiv los ntawm Fmoc los yog Boc tiv thaiv pawg, maj mam ua ke los ua ib tug linear polypeptide saw, thiab thaum kawg txiav los ntawm TFA resin thiab purified. Cov qauv tswj kev ua tau zoo muaj xws li:
Purity: Kev ua haujlwm siab ua kua chromatography (HPLC) kuaj pom qhov purity ntau dua lossis sib npaug li 98%.
Kev txheeb xyuas qhov hnyav Molecular: Mass spectrometry (MS) lees paub tias qhov hnyav molecular yog raws li tus nqi theoretical.
Kev ntsuam xyuas kev ua haujlwm lom neeg: Txheeb xyuas nws lub peev xwm los txhawb kev tso tawm ntawm adrenocorticotropic hormone (ACTH) los ntawm kev sim hauv vitro cell (xws li AtT-20 pituitary qog hlwb).
Classification thiab teeb liab transduction mechanism ntawm CRF receptors
Cov qauv thiab kev faib tawm ntawm CRF receptors
CRF receptor belongs rau B-class G protein coupled receptor (GPCR) tsev neeg, uas suav nrog ob hom subtypes: CRF ₁ R thiab CRF ₂ R
CRF ₁ R: Dav faib rau hauv nruab nrab lub paj hlwb (xws li cerebral cortex, hippocampus, amygdala) thiab cov ntaub so ntswg peripheral (xws li pituitary caj pas, qog adrenal, placenta).
CRF ₂ R: feem ntau yog qhia nyob rau hauv paraventricular nucleus ntawm lub hypothalamus, locus coeruleus, qaum qaum, thiab peripheral cov ntaub so ntswg xws li lub plawv, hlab ntsha, thiab gastrointestinal ib ntsuj av.
Homology ntawm cov amino acid sequences ntawm ob receptors nce mus txog 70%, tab sis muaj qhov sib txawv ntawm ligand khi tshwj xeeb: CRF ₁ R muaj kev sib raug zoo rau CRF dua li CRF ₂ R, uas nyhav rau khi rau Urocortin (UCN) tsev neeg ligands.
G protein ua ke txoj kev taw qhia
Tom qab khi rau cov receptor, CRF txhawb nqa adenylate cyclase (AC) kev ua haujlwm los ntawm kev ua kom G s protein, ua rau muaj kev nce qib ntawm intracellular adenosine monophosphate (cAMP), uas nyob rau hauv lem activates protein kinase A (PKA) thiab downstream signaling molecules xws li CREB. Tsis tas li ntawd, CRF tuaj yeem qhib tau phospholipase C (PLC) los ntawm G q protein, ua rau calcium ion (Ca ² ⁺) mobilization thiab protein kinase C (PKC) activation.
Cov teeb liab tseem ceeb nodes yog
CAMP PKA txoj hauv kev: tswj ACTH secretion, qabzib metabolism, thiab cov noob qhia.
Ca ² ⁺ - PKC txoj hauv kev: koom nrog kev tswj hwm ntawm neuronal excitability thiab synaptic plasticity.
MAPK txoj hauv kev: kho kom haum xeeb ntev - cov lus teb hloov kho (xws li kev muaj sia nyob ntawm lub hlwb) los ntawm ERK1/2 phosphorylation.
Mechanisms ntawm receptor desensitization thiab endocytosis
Lub sij hawm ntev raug rau CRF tuaj yeem ua rau receptor desensitization, manifested li txo G protein coupling efficiency thiab receptor phosphorylation. Lub desensitization ntawm CRF ₁ R feem ntau yog nyob ntawm - ntes hauv nruab nrab endocytosis, thaum lub sij hawm endocytosis efficiency ntawm CRF ₂ R yog qhov tsawg, uas tej zaum yuav muaj feem xyuam rau qhov sib txawv ntawm receptor subcellular localization. Tom qab endocytosis, receptors tuaj yeem rov ua dua mus rau lub cell membrane los yog nkag mus rau lysosomes rau degradation, uas yog qhov tseem ceeb rau kev tswj hwm receptor functional homeostasis.
Kev lag luam kws tshuaj
Raws li kev kuaj mob reagent los ntsuas pituitary muaj nuj nqi
Amunineyog tus txheej txheem kub diagnostic reagent rau kev soj ntsuam pituitary adrenal axis muaj nuj nqi. Nws mechanism ntawm kev txiav txim yog raws li nram no:
Txhawb nqa ACTH secretion: Tom qab txhaj tshuaj ntawm CRF (Ovine), CRF ₁ R hauv lub caj pas pituitary tuaj yeem ua kom nrawm nrawm, txhawb kev sib txuas thiab tso tawm ntawm ACTH.
Indirectly txhawb cortisol secretion: ACTH nkag mus rau hauv cov hlab ntsha thiab ua rau adrenal cortex, inducing cortisol secretion. Los ntawm kev txheeb xyuas cov kev hloov pauv hauv plasma ACTH thiab cortisol qib, kev ua haujlwm ntawm cov qog pituitary thiab adrenal tuaj yeem raug soj ntsuam tuaj yeem siv rau kev kuaj mob sib txawv ntawm Cushing's syndrome. Cov neeg mob Cushing's syndrome muaj ACTH nyob ntawm cortisol secretion, tab sis qhov ua rau tuaj yeem yog pituitary adenoma (Cushing's disease) lossis ectopic ACTH syndrome. CRF (Ovine) stimulation test tuaj yeem paub qhov txawv ntawm ACTH thiab cortisol los ntawm kev soj ntsuam lawv cov qauv lus teb.
Pituitary Cushing's tus kab mob yog tus cwj pwm los ntawm kev txhim kho cov lus teb ntawm lub qog pituitary rau CRF (Ovine), nrog rau qib siab ntawm ACTH thiab cortisol. Ectopic ACTH syndrome yog hais txog kev tso tawm ntawm ACTH los ntawm kev ua haujlwm tsis zoo ntawm pituitary adenomas lossis ectopic hlav, uas tsis teb rau CRF (Ovine). Cov neeg mob uas muaj cov qog adrenal tsis txaus (xws li cov kab mob pituitary) tau txo qis ACTH secretion, ua rau txo qis cov lus teb cortisol.
Cov cuab yeej sib txuas hauv kev tsim tshuaj
CRF system ua lub luag haujlwm tseem ceeb hauv kev xav tsis zoo xws li kev ntxhov siab thiab kev nyuaj siab, thiab CRF ₁ R antagonists tau dhau los ua lub ntsiab lus kub hauv kev txhim kho cov tshuaj tiv thaiv kev ntxhov siab / kev nyuaj siab. CRF (Ovine) Trifluoroacetate yog siv los ua cov cuab yeej sib txuas rau receptor binding thwmsim los tshuaj xyuas cov affinity siab CRF ₁ R antagonists thiab ntsuas lawv cov peev xwm sib tw. Cov kev sim ua haujlwm tau ua los ua pov thawj cov nyhuv inhibitory ntawm antagonists ntawm ACTH secretion induced los ntawm CRF (Ovine) nyob rau hauv ib lub cell qauv. Tsiaj cov qauv kev tshawb fawb siv kev ntxhov siab xws li kev coj tus cwj pwm coj los ntawm CRF (Ovine), xws li kev ntsuam xyuas qhov siab, los ntsuam xyuas cov kev ntxhov siab los ntawm cov antagonists.
Cov tshuaj sawv cev:
Verucerfont: Phase II kev sim tshuaj tau ua tiav thiab pom tias muaj txiaj ntsig zoo hauv kev kho mob kev ntxhov siab dav dav (GAD).
Pexacerfont: Siv los kho kev nyuaj siab los ntawm inhibiting CRF ₁ R kom txo cov kev ntxhov siab.
Kev loj hlob ntawm CRF2 R agonists
CRF2R plays lub luag haujlwm tseem ceeb hauv kev tiv thaiv kab mob plawv thiab kev hloov pauv kev ntxhov siab, thaumAmunine yog siv rau:
Receptor selectivity research: Distinguishing lub functional sib txawv ntawm CRF 1 R thiab CRF2 R coj tus tsim ntawm selective agonists.
Cov qauv kab mob plawv: Hauv cov qauv myocardial infarction, CRF ₂ R agonists (xws li UCN2) tuaj yeem txo myocardial cell apoptosis thiab txhim kho lub plawv ua haujlwm.
Cov lus nug nquag
Vim li cas CRF tshwj xeeb yog los ntawm " yaj" es tsis yog tib neeg lossis nas qhov chaw?
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Vim nws cov yam ntxwv pharmacological. Piv nrog rau tib neeg lossis nas CRF, yaj CRF (oCRF) muaj kev sib txuas zoo dua rau CRF receptor hom 1 thiab ib nrab ntev dua -lub neej hauv vivo, ua kom muaj zog thiab ruaj khov ACTH tso tawm cov lus teb, ua rau nws yog tus qauv thiab ntau dua cov cuab yeej peptide rau kev tshawb fawb thiab kev kuaj mob.
Lub ntsiab lus 'trifluoroacetate' txhais li cas? Puas yog daim ntawv ntsev ntau hauv cov tshuaj?
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Qhov no yog ib qho txiaj ntsig zoo hauv kev ua kom huv thiab kev npaj ntawm cov tshuaj peptide. Trifluoroacetic acid yog ib qho acidic mobile theem tivthaiv siv nyob rau hauv lub purification ntawm peptides los ntawm siab -kev ua tau zoo kua chromatography, uas yuav nyob twj ywm nyob rau hauv cov khoom kawg thiab daim ntawv ntsev. Nws tsis yog cov khoom xyaw nquag thiab cov kab mob feem ntau tso cai rau hauv kev npaj lom neeg.
Nws pab qhia txog kev sib txuas ncaj qha ntawm "kev ntxhov siab" thiab "kev ntxhov siab" tus cwj pwm hauv kev tshawb fawb?
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Kev txhaj tshuaj oCRF ncaj qha mus rau thaj chaw tshwj xeeb ntawm cov tsiaj lub hlwb (xws li amygdala) tuaj yeem hla cov kab mob endocrine thiab ncaj qha mus rau hauv nruab nrab CRF neurons, yog li ua rau muaj kev ntxhov siab xws li kev coj cwj pwm (xws li kev ceeb toom thiab txo tus cwj pwm tshawb nrhiav). Qhov no muab cov pov thawj ncaj qha rau cov neural circuits uas ua rau muaj kev ntxhov siab los ntawm kev ntxhov siab.
Dhau li ntawm stimulating lub caj pas pituitary, dab tsi yog nws lub luag haujlwm tsawg dua hauv kev tiv thaiv kab mob?
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Lub cev tiv thaiv kab mob, xws li T hlwb thiab macrophages, kuj qhia CRF receptors. OCRF tuaj yeem tswj hwm kev ua haujlwm ntawm lub cev tiv thaiv kab mob, xws li inhibiting kev tso tawm ntawm cov kab mob inflammatory los ntawm macrophages thiab cuam tshuam rau lymphocyte proliferation. Nws yog ib qho tseem ceeb txuas molecule nyob rau hauv lub neuroendocrine tiv thaiv network.
Vim li cas nws yog ib qho cuab yeej zoo tshaj plaws rau kev kawm txog cov kev tawm tswv yim tsis zoo ntawm hypothalamic pituitary adrenal axis?
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Los ntawm kev tswj hwm cov tshuaj exogenous thiab tus qauv ntawm oCRF, HPA axis tuaj yeem raug sib tw, thiab kev tso tawm kinetics thiab ncov qhov tseem ceeb ntawm ACTH thiab cortisol tuaj yeem saib xyuas. Qhov no tuaj yeem ua rau muaj kev cuam tshuam txog kev ua haujlwm ntawm lub qog pituitary rau CRH thiab kev tawm tswv yim tsis zoo ntawm cortisol, siv los ntsuas qhov kev ncaj ncees ntawm HPA axis muaj nuj nqi.
Cim npe nrov: Tuam Tshoj amunine manufacturers, lwm tus neeg
