URB597

AASraw ili ndi kaphatikizidwe ndi kapangidwe kameneka kuchokera ku gramu kupita ku dongosolo la URB597 (546141-08-6), pansi pa lamulo la CGMP ndi dongosolo loyendetsa khalidwe labwino.

URB597, omwe amadziwikanso kuti KDS-4103, ndi mankhwala amphamvu komanso osankhidwa kwambiri a fatty-acid amide hydrolase (FAAH), omwe amachititsa kuti tizilombo toyambitsa matenda tizilombo toyambitsa matenda tizilombo toyambitsa matenda tizilombo toyambitsa matenda tizilombo toyambitsa matenda, tizilombo toyambitsa matenda a 50% tizilombo toyambitsa matenda IC50 ya 4.6 nM ndi 0.5 nM mu makoswe a ubongo ndi chiwerengero cha chiwindi cha munthu. URB597 imasonyeza nkhawa, nkhawa, antiinociceptive ndi analgesic zotsatira mu vivo popanda kutulutsa zizindikiro zina zokhudzana ndi mankhwala a khansa.

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Video ya URB597


I.URB597 Makhalidwe Abwino:

Name: URB597
CAS: 546141-08-6
Chiyero: ≥99% (HPLC)
Makhalidwe a Maselo: C20H22N2O3
Kulemera kwa maselo: 338.4
EINECS: 1312995-182-4
Mafanowo: 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; KNSX'-biphenyl] -4103-yl ester ; N-Cyclohexylcarbamic acid 3 '- (aminocarbonyl) [1,1'-biphenyl] -3-yl ester URB 3 KDS 1,1; URB 3,> = 597%; APD4103 (URB597)
Melt Point: 155-157 ° C
Alpha: D + 5 ° (c = 0.437 mu chloroform)
Kusungirako nyengo: 2-8 ° C
Kukhazikika DMSO: sungunuka2mg / mL, bwino (kutentha)
mtundu; White olimba


II. Kugwiritsa ntchito URB597 pozungulira:

1.Name:

URB597

2.Kodi ntchito ya URB597 ndi yotani?

Zowona: Chodetsa nkhaŵa chachikulu chokhudzana ndi kugwiritsidwa ntchito kwa cannabinoid receptor 1 (CB1) agonists mwachindunji ndikuti mankhwalawa amachulukitsa kumwa mowa ndi zoyenera kugwiritsa ntchito mankhwala osokoneza bongo. Monga njira yowonjezera, ntchito ya CB1-receptor-mediated ingathandizidwe mwa kuwonjezera makina a anandamide pogwiritsa ntchito hydrolase mafuta acid amide hydrolase (FAAH) inhibitors. Cholinga: Pogwiritsa ntchito njira ya FAAH yotetezera URB597, ife tafufuza ngati kuyambitsidwa kwa mawu osokoneza bongo kumawonjezera kuledzeretsa, monga momwe zimachitikira ndi CB1 kulandira oponderezedwa. Zida ndi njira: URB597 inayesedwa pa zakumwa zoledzeretsa ku makoswe a Wistar ndipo imaletsa kumwa mowa mwazitsulo zakusankhidwa za Marchigian Sardinian mowa (msP). Mu makoswe a Wistar, zotsatira za URB597 pa nkhawa yoledzeretsa ndi kupsinjika-, yohimbine- ndi kubwezeretsedwa kwa kubwezeretsa mowa kufunafuna zinayesedwanso. Poyerekezera, zotsatira za anti-anti-antagonist anti-CB1 pa ethanol self-administration zinayesedwa. Zotsatira: Pamene tikuyesedwa, intraperitoneal (IP) kayendetsedwe ka URB597 (0.0, 0.3 ndi 1.0 mg / kg) sanawonjezeke mwadzidzidzi kumwa mowa mwauchidakwa mumsambo wa msP kapena kupangitsa kuti chiwerengero cha 1 chikhale chokhazikika komanso kupititsa patsogolo chiŵerengero choledzeretsa mowa mu Wistars osasamala. Mu kuyesa kubwezeretsanso, chigawocho sichinali ndi zotsatirapo zowonongeka, kupsyinjika maganizo ndi kufooka kwa yohimbine. Mosiyana ndi zimenezi, URB597 inathetsa kuthetsa vutoli poyesa kuchotsa pambuyo poyambitsa IP alcohol alcohol (3.0 g / kg). Rimonabant (0.0, 0.3, 1.0 ndi 3.0 mg / kg) yachepetsa kwambiri kutentha kwa ethanol. Zotsatira: Zotsatira zimasonyeza kuti kuyambitsa njira yothetsera matenda a antiandamide pogwiritsa ntchito njira zoletsera za FAAH sikungowonjezera mavuto ozunguza bongo koma imachepetsanso nkhawa zomwe zimakhudzana ndi kuchotsa mowa. Choncho tinganene kuti mankhwala omwe amagwiritsidwa ntchito pogwiritsira ntchito endocannabinoid system modulators monga URB597 angapereke ubwino wofunikira poyerekeza ndi mankhwala ndi otsogolera omwe amalandira CB1.

3.Iyi ikugwira URB597?

Zotsatira za URB 597 zokha komanso kuphatikiza ndi anandamide zinkafufuzidwa mu gulu limodzi la anyani (n = 4) omwe adasankha Δ9-THC (0.1 mg · kg-1 iv) kuchokera ku galimoto, komanso mu gulu lina (n = 5) kulandira chronic Δ9-THC (1 mg · kg-112 h-1 sc) yomwe inachititsa kuti munthu wotsutsana ndi odwala matendawa asagwiritsidwe ntchito (1 mg · kg-1 iv).

4.Inanso malangizo:

URB 597 inalimbikitsa zotsatira za khalidwe la anandamide koma osati ena a CB1 agonists. Komabe, URB 597 sinasinthe kwambiri kuchepetsa kuchepa kwa Δ9-THC kuchotsedwa ndi anandamide. Zonsezi, deta imeneyi imasonyeza kuti anandamide osagwira ntchito mu ubongo wamaphunziro amatha kusonyeza mosavuta zotsatira za makhalidwe omwe amachititsa kuti anandamide apitirize kutero.

Mafuta abwino komanso osankhidwa a asidi amadzi hydrolase (FAAH) inhibitor (IC50 chikhalidwe ndi 3 ndi 5 nM mu chiwindi cha munthu ndi ubongo wa ubongo). Zisonyezero sizinali zolepheretsa kugwira ntchito zosiyanasiyana, mapulogalamu a ion ndi mavitamini, kuphatikizapo mapuloteni a anthu omwe amatha kulandira mankhwalawa ndi rat monoacylglycerol lipase. Amasonyeza antiallodynic ndi antihyperalgesic ntchito mu chitsanzo chopweteka kwambiri. In vitro, KDS-4103 imaletsa ntchito ya FAAH ndi njira zochepetsetsa (IC (50)) za 5 nM mu ubongo wa ubongo ndi 3 nM mu microsomes ya chiwindi. Mu vivo, KDS-4103 imaletsa ubongo wa abambo a FAAH pambuyo pa intraperitoneal (ip) maulamuliro omwe ali ndi chiwerengero chodziletsa (ID (50) ya 0.15 mg / kg. Kachilombo kamene sikakhudzana kwambiri ndi zofuna zina zokhudzana ndi matenda a khansa, kuphatikizapo zizindikiro za cannabinoid ndi transport ya anandamide, kapena ndi malo ambirimbiri othandizira, njira za ion, otumiza katundu ndi mavitamini. Ndi ip ip management kwa makoswe ndi mbewa KDS-4103 imakhala yofunika kwambiri, nkhawa, monga kupweteka kwapadera monga momwe amachitira, omwe amaletsedwa ndi mankhwala omwe amatsutsana ndi CB1. Mosiyana ndi, mankhwala omwe amalepheretsa kwambiri ntchito ya FAAH ndipo amaletsa kwambiri ubongo wa anandamide, KDS-4103 siimatulutsa zotsatira zofanana ndi zomwe zimachitika (monga, catalepsy, hypothermia, hyperphagia), sizimapanga mphamvu zotsatira zowonongeka za mankhwala opangira mankhwala, Delta9-tetrahydrocannabinol (Delta9-THC). Zotsatirazi zikusonyeza kuti KDS-4103 amachita mwa kuwonjezera zochita za anandamide pamagulu a CB (1) receptors, omwe kawirikawiri amawongolera kuthetsa ululu ndi ululu. KDS-4103 imapezeka pamlomo pa makoswe ndi nyani za cynomolgus. Maphunziro a mlingo wafupipafupi (1,500 mg / kg, per os) mwa mitundu iwiriyi sanawonetsere poizoni. Mofananamo, palibe poizoni omwe amadziwika mu mabakiteriya cytotoxicity ayero mu vitro komanso mu test Ames. Kuwonjezera apo, palibe vuto lililonse lomwe linawonedwa mu makoswe pamayeso oyendetsa katemera pambuyo pa mankhwala opatsirana pogwiritsa ntchito KDS-4103 pa mlingo wa 5 mg / kg kapena mu battery yoyang'anitsitsa potsatira mlingo wa 1,500 mg / kg. Zotsatirazo zikusonyeza kuti KDS-4103 idzapereka njira yatsopano ndiwindo lothandizira kuti athetse nkhawa, kuvutika maganizo ndi kupweteka.

5. URB597:

10grams yayamba.
Funso labwino kwambiri (mkati mwa 1kg) lingatumizedwe mu maola a 12 mutatha kulipira.
Kuti mukhale wamkulu (mkati mwa 1kg) mukhoza kutumizidwa mu tsiku la ntchito 3 mutatha kulipira.

6. Maphikidwe a URB597:

Kuti mufunse Wotumikira Wathu Woimira Wathu (CSR) kuti mudziwe zambiri, kuti muwone.

7. Makampani a URB597:

Kuti aperekedwe m'tsogolomu.


III. URB597 HNMR

Ndife aprepitant ufa wophimba, ufa wa Aprepitant wogulitsidwa, ufa wochuluka wa Aprepitant (170729-80-3) hplc =98% | Ikani ma Reagents a R & D


IV. Kodi mungagule bwanji URB597 ku AASraw?

1.Kutiwuza ife ndi imelo yathukafukufuku, kapena skype pa intanetiwoimira makasitomala (CSR).
2.Zotipatseni ife afunsidwa zambiri ndi adiresi yanu.
3.Our CSR idzakupatsani inu ndondomeko, nthawi yobwezera, nambala yotsatira, njira yobweretsera ndi tsiku lofika kufika (ETA).
4.Payment yachitidwa ndipo katunduyo adzatumizidwa mu maola a 12 (Kukonzekera mkati mwa 10kg).
5.Goods inalandira ndi kupereka ndemanga.


Tangoganizirani zomwe mumakonda kwambiri blog:

Mmene mungagwiritsire ntchito Clenbuterol kuti muwonongeke Kodi ufa wa nandrolone umagwiritsidwa ntchito bwanji / nandrolone phindu?


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