URB597

AASraw o loʻo i ai le tuʻufaʻatasiga ma le gaosiga gafatia mai le gram i le faasologa o le URB597 (546141-08-6), i lalo o le CGMP tulafono faatonutonu ma le siakiina o le lelei o le faʻaogaina o le tino.

URB597, lea e lauiloa foi o le KDS-4103, o se inhibitor sili ona malosi ma filifilia o le fatty-acid amide hydrolase (FAAH), o se enzyme e faʻaaogaina ai le hydrolysis intracellular o le adosocamide endocannabinoid, faatasi ai ma le taua o le ICNNXX 50% inhibition concentration IC50 o 4.6 nM ma 0.5 nM i totonu o le vavae o le rat ma le fatu o le tagata. URB597 o loʻo faʻaalia ai le popole, le faʻamalosi, le faʻamaʻi ma le faʻafefete i aʻafiaga e aunoa ma le faʻailogaina o isi faʻamaoniga e fesootaʻi ma le tuufaatasiga o le cannabinoid.

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Faamatalaga oloa

URB597 vitio


I.URB597 autu Tagata:

igoa: URB597
CAS: 546141-08-6
Mama: ≥99% (HPLC)
Polokalame Molecular: C20H22N2O3
Taumaʻa Masele: 338.4
EINECS: 1312995-182-4
Fa'amatalaga: N-Cyclohexylcarbamic acid 3 '- (aminocarbonyl) [1,1'-biphenyl] -3-yl ester; 3'-CarbaMoyl- [1,1'-biphenyl] -3-yl cyclohexylcarbaMate; 3- (3-CarbaMoylphenyl) phenyl N-cyclohexylcarbaMate CarbaMic acid, N-cyclohexyl-, 3 '- (aMinocarbonyl) [1,1'-biphenyl] -3-yl ester; 4103 N-Cyclohexylcarbamic acid 3' - (aminocarbonyl) [1,1'-biphenyl] -3-yl ester N-Cyclohexylcarbamic acid 3 '- (aminocarbonyl) [1,1'-biphenyl] -3-yl ester URB 597 KDS 4103; URB 597,> = 98%; APD597 (URB597)
Melt Point: 155-157 ° C
Alefa: D + 5 ° (c = 0.437 i le chloroform)
Teu o le Teuina: 2-8 ° C
Solubility DMSO: soluble2mg / mL, manino (mafanafana)
Valivali: Paʻepaʻe papaʻe


II. URB597 faʻaaogaina i le taamilosaga:

1.Name:

URB597

2.O le a le galuega mo URB597?

Rationale: O se popolega ogaoga faʻapitoa i le faʻaaogaina o le faʻamaumauga a le 1 (CB1) faʻamaonia o le cannabinoid, o nei mea faʻaopoopo e faʻaopoopoina le ava malosi ma le faʻaaogaina o fualaau faasaina. I le isi itu, o le CB1-receptor-mediated activity e mafai ona faafaigofieina e ala i le faateleina o le maualuga o le taamilosaga i le faaaogaina o le hydrolase fatty acid amide hydrolase (FAAH) inhibitors. Manulauti: Faʻaaogaina o le initaneti filifilia o le FAA URB597, matou te suʻesuʻeina pe faʻamalosia le gasegase o le cannabinoid e faʻateleina le faʻaleagaina o le ava malosi, e pei o le mea e tupu i le CB1 receptor direct agonists. Meafaigaluega ma auala: URB597 na faʻataʻitaʻiina i luga o le ava malosi-puleaina i laumei Wistar ma luga o le ava malosi fale inu ava malosi filifilia Marchigian Sardinian alcohol-prefering (msP) rat. I Wistar, o aʻafiaga URB597 i luga o le popolega o le ava malosi ma luga o le popolega,, yohimbine- ma le toe faʻafouina o le ava malosi sa iloiloina foi. Mo le faʻatusatusaga, na tofotofoina foi le aʻafiaga o le talitolu o le receptor CB1 rimonabant i le ethanol self-administration. Iʻuga: I lalo o le matou faʻataʻitaʻiga, pulega faʻapitoa o le intraperitoneal (IP) o le URB597 (0.0, 0.3 ma 1.0 mg / kg) poʻo le faateleina o le ava malosi e inu ai i le raukagi MSP poʻo le faʻamaopoopoina le fuainumera 1 ma le alualu i luma o le puleaina o le alcohol self-administration i Wistars. I le toe faʻaleleia o suʻega, e leai ni aʻafiaga o le faʻapipiʻi i luga o le laumei, o le mamafa o le footshock- ma le toe foi mai o le yohimbine. I se isi itu, URB597 faʻamaeʻa atoa le tali popolega na fuaina i le taimi o le tolopoina pe a maeʻa le puleaina IP o le ava malosi (3.0 g / kg). Rimonabant (0.0, 0.3, 1.0 ma le 3.0 mg / kg) na faʻaititia ai le puleaina o le ethanol. Faaiuga: O faʻamatalaga e faʻaalia ai o le faʻamalosia o le endocannabinoid faʻasalaga e ala i le filifiliina o le FAAH e le faateleina ai le faʻaleagaina o le ava malosi ae faʻaitiitia le popole e aʻafia ai le ava. E mafai ona tatou vavalalata o fualaau e faavae i luga o le faʻaogaina o modocamids system modulators e pei ole URB597 e mafai ona ofoina atu tulaga taua pe a faʻatusatusa i togafitiga faʻatasi ma le faʻamalosia CB1 faʻamalosia.

3.Ia faʻaalia URB597?

O aʻafiaga o le URB 597 naʻo ia ma faatasi ai ma le anandamide na suʻesuʻeina i se tasi vaega o manuki (n = 4) na faʻamaonia ai le Δ9-THC (0.1 mg · kg-1 iv) mai le taavale, ma i le isi vaega (n = 5) chronic Δ9-THC (1 mg · kg-112 h-1 sc) lea na faʻamaonia ai le timononabant cannabinoid (1 mg · kg-1 iv).

4.Further instructions:

URB 597 na faʻamalosia le faʻalauiloaina o amioga o le anandamide ae le o isi CB1 agonists. Peitai, URB 597 e leʻi faʻaleleia atili le atinaʻeina o le toesea o le Δ9-THC na faʻaosoina e le anandamide. I le tuufaatasiga uma, o nei faamatalaga e taʻu mai ai o le oona i le mafaufau o le mafaufau e le faigofie ona faʻataʻitaʻiina amioga faʻaleagaina o le mea na tupu i se mea faʻatalanoa.

Malosiaga ma le filifilia o le gaʻo masima acid amide hydrolase (FAAH) inhibitor (IC50 taugata o 3 ma 5 nM i le mafaufau o le ate ma le rat, i le faasologa). E leʻo iai ni mea faʻalavelave e tetee atu ai i le tele o faʻaleleia, o laina elemene ma enzymes, e aʻafia ai ma tagata resitala o le cannabinoid ma le rat monoacylglycerol lipase. Faʻaalia le faʻaaogaina o antiallodynic ma antihyperalgesic i se faʻataʻitaʻiga tiga o le tino. I vitro, KDS-4103 faʻalavelaveina ai le gaoioiga FAAH i faʻataʻitaʻiga faʻasaina (IC (50)) o le 5 nM i fusi masile ma le 3 nM i totonu ole fatu ole fatu. I totonu o vivo, KDS-4103 e faʻasaina ai le rat brain brain FAAH i le maea ai o le intraperitoneal (ip) pulega faʻatasi ai ma se vailaʻau faʻasaina (ID (50)) o le 0.15 mg / kg. E le tele fesoʻotaʻiga le tuufaatasiga ma isi sini e fesoʻotaʻi ma le cannabinoid, e aofia ai le faʻaaogaina o le cannabinoid ma le fagafaʻalele, pe faʻatasi ai ma se lautele lautele o le faʻaleleia, o laina eletise, o loʻo faʻapipiʻi ma enzymes. E ala i le pulega i rato ma muse KDS-4103 e faʻaalia ai le taua, faʻalavelave popole-pei, faʻamaʻi-pei-pei ma faʻafitiga o aʻafiaga, lea e puipuia mai togafitiga faʻatasi ma CB1 taligata. I le eseesega, i vailaau e matua taofia ai le gaoioiga a le FAAH ma siitia tele ai le maualuga o le faiʻai, o le KDS-4103 e le faʻavevelaina aafiaga faʻaleagaina o le cannabinoid (eg, catalepsy, hypmiamia, hyperphagia), e le maua ai le faʻasalalauga o aʻafiaga faʻapitoa o le gaosiga gaosi o le cannabis, Delta9-tetrahydrocannabinol (Delta9-THC). O nei suʻesuʻega ua faʻamaonia mai ai o le KDS-4103 o loʻo galue e ala i le faʻaleleia o le tonic actions of anandamide i luga o se vaega o faʻamaumauga CB (1), lea e ono masani ona punouai i le pulea o lagona ma tiga. O le KDS-4103 o loʻo maua i le faʻalaulei i kusi ma ckey male. O suʻesuʻega faʻasolosolo faʻasolosolo masani (1,500 mg / kg, per os) i nei ituaiga meaola e lua e le o faʻaalia ai le faʻamaʻi. E faʻapea foʻi, e leai se mea na tupu na iloa i suʻesuʻega o cytotoxicity siama i vitro ma i le suega a Ames. E le gata i lea, e leai ni paʻu na matauina i tamaʻi i luga ole suega o rotarod ina ua maeʻa togafitiga faʻamaʻi ma le KDS-4103 i doses e oo atu i le 5 mg / kg poʻo i totonu o se siama mataʻituina o le tino pe a uma ona tuʻuina atu i le 1,500 mg / kg. O iʻuga e taʻu mai ai o KDS-4103 o le a ofoina atu se auala faʻataʻitaʻi ma se faamalama faʻaleleia lelei mo togafitiga o popolega, atuatuvale ma tiga.

5. URB597:

Min poloaiga 10grams.
O le suʻesuʻega i le aofaʻi masani (I totonu ole 1kg) e mafai ona lafo i 12 itula pe a uma ona totogi.
Mo le faasologa sili (I totonu 1kg) e mafai ona auina atu ile 3 workingdays pe a uma le totogiina.

6. URB597 Recipes:

Faʻatalanoaina o matou Tagata Faʻatau (CSR) mo auiliiliga, mo lau faʻamatalaga.

7. URB597 Marketing:

Ia saunia i le lumanai.


III. URB597 HNMR

O matou o Aprepating powder powder, Aprepitant powder for sale, Lafo Faʻatau (170729-80-3) hplc≥98% | AASraw R & D Reagents


IV. Faʻafefea ona faʻatau URB597 mai AASraw?

1.E faʻafesoʻotaʻi mai i matou i la matou imelisuʻesuʻega, poʻo le skypesui o le au faipisinisi (CSR).
2.E tuʻu mai ia i matou le tele o au fesili ma lau tuatusi.
3.Our CSR o le a tuʻuina atu ia te oe le upusii, taimi o totogi, numera o le suʻega, auala e tuʻuina atu ai ma le aso atofaina e taunuu ai (ETA).
4.Payment na faia ma o oloa o le a auina atu i itula 12 (Mo le faʻasalalauga i totonu ole 10kg).
5.Goods na maua ma tuuina mai ni faʻamatalaga.


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