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URB597

URB597, e boetse e tsejoa e le KDS-4103, e na le inhibitor e matla haholo le e khethileng ea fatty-acid amide hydrolase (FAAH), e leng enzyme e kenyang hydrolysis ea intracellular ea endocannabinoid anandamide, e nang le litekanyetso tsa 50% ho thibela khohlano IC50 ea 4.6 nM le 0.5 nM ka likokoana-hloko tsa lera le li-microrosomes tsa sebete ka tsela e ts'oanang. URB597 e bontša ho tšoenyeha, ho imeloa kelellong, liphello tsa antinociceptive le analgesic ka ho hlaka ntle le ho hlahisa matšoao a mang a amanang le lik'hemik'hale tse kang li-cannabinoid.

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Tlhaloso ea Sehlahisoa

 

Video ea URB597

 

 


 

I.URB597 Boitsebiso ba motheo:

 

Name: URB597
CAS: 546141-08-6
Ho hloeka: ≥99% (HPLC)
Molecular Formula: C20H22N2O3
Boima ba 'mele: 338.4
EINECS: 1312995-182-4
Li-synonyms: 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; KDS 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
Alpha: D + 5 ° (c = 0.437 ka chloroform)
Temp Temp Storage: 2-8 ° C
Solubility DMSO: ho qhibiliha2mg / mL, ho hlakile (ho futhumala)
Color: Tšepe e tšoeu

 


 

II. Tšebeliso ea URB597 ho potoloha:

 

1.Name:

URB597

 

2. Mosebetsi oa URB597 ke ofe?

Tlhahisoleseding: Khatello e kholo ea bongaka ka tšebeliso ea li-agonists ka ho toba ea cannabinoid receptor 1 (CB1) ke hore lik'hemik'hale li eketsa ho noa joala le boitšoaro bo amanang le lithethefatsi. Joaloka mokhoa o mong, mokhoa oa li-CB1-receptor o ka fetisetsoa ka ho eketsa maemo a anandamide ka tšebeliso ea hydrolase fatty acid e amide hydrolase (FAAH) inhibitors. Sepheo: Ha re sebelisa FAAH e thibelang likokoana-hloko URB597, re ile ra etsa lipatlisiso hore na ho kenya letsoho molumo oa kankere oa ho noa joala ho eketsa boikarabelo ba ho sebelisa joala hampe, joalo ka se etsahalang le li-agonists tse ikemetseng tsa CB1. Lisebelisuoa le mekhoa: URB597 e ne e lekoa lits'etsong tsa lino tse tahang likokoanyana tsa Wistar le ka ho qoba ho noa lino tse tahang ka liphatsa tsa lefutso tsa Marchigian Sardinian-preferring (msP). Lintlheng tsa Wistar, liphello tsa URB597 ka ho tšoenyeha ka joala le khatello ea kelello-, yohimbine- le ho tsosolosoa ho tsosolosoa ha lino tse tahang ho ile ha boela ha hlahlojoa. Ho bapisa, phello ea mohanyetsi oa li-CB1 ea mohanyetsi oa li-ronabant ethanol-self-administration e ile ea boela ea lekoa. Liphello: Tlas'a boemo ba rona ba liteko, tsamaiso ea intraperitoneal (IP) ea URB597 (0.0, 0.3 le 1.0 mg / kg) ha e phahame ka ho ithaopela ho noa joala mokhoeng oa msP kapa ho fokotsa likarolo tse sa lekanyetsoang tsa 1 le phaello e tsoelang pele ea joala boinotšing ho Li-Wistars tse sa tsotelloeng. Litekong tsa ho khutlisetsoa hape, setsi sena ha sea ka sa e-ba le liphello tse hlakileng-ho fokotsa khatello ea kelello le khatello ea mocheso ea yohimbine. Ka lehlakoreng le leng, URB597 e ile ea felisa ka ho feletseng karabo ea ho tšoenyeha e neng e lekantsoe nakong ea ho tlohela ka morao ho IP e sebetsang ka matla (3.0 g / kg). Rimonabant (0.0, 0.3, 1.0 le 3.0 mg / kg) e ile ea fokotsa haholo ethanol ho ipusa. Liphello: Liphello li bontša hore ts'ebetsong ea endocannabinoid anandamide tsamaiso ka ho thibela tšoaetso ea FAAH ha e phaelle likotsi tse mpe tsa joala empa e fokotsa ho tšoenyeha ho amanang le ho tlosoa joala. Ka hona re ka nahana hore meriana e itšetlehileng ka tšebeliso ea modocators ea endocannabinoid e kang URB597 e ka fana ka menyetla ea bohlokoa ho bapisoa le phekolo ka bahlaseli ba ka ho toba ba CB1.

 

3.Na e sebetsa ka URB597?

Liphello tsa URB 597 feela mme li kopantsoe le anandamide li ne li phenyekolloa ka sehlopha se le seng sa litšoene (n = 4) se khethileng Δ9-THC (0.1 mg · kg-1 iv) ho tloha koloing, 'me se fumane sehlopha se seng (n = 5) e sa foleng Δ9-THC (1 mg · kg-112 h-1 sc) e neng e khetholla mohanyetsi oa li-cannabinoid e nang le rimonabant (1 mg · kg-1 iv).

 

4.Hape litaelo:

URB 597 e ntlafalitse liphello tsa boitšoaro ba anandamide empa ha e-na le li-agonists tse ling tsa CB1. Leha ho le joalo, URB 597 ha ea ka ea ntlafatsa ka ho tebileng tlhokomelo ea ho tlosoa ha Δ9-THC e bakoang ke anandamide. Ka kakaretso, dintlha tsena li bonts'a hore anandamide e sa tsitsang boko ba boko bo sebetsang ha bo bonolo ho etsisa liphello tsa boitšoaro tsa ho tsamaisa anandamide ka mokhoa o feteletseng.

Matla a mafura le a khethiloeng a mafura a amide hydrolase (FAAH) inhibitor (litekanyetso tsa IC50 ke 3 le 5 nM sebeteng sa motho le boko ba rat, ka ho latellana). Lipontšo tse se nang tšebetso ea ho thibela li-receptor tse sa tšoaneng, litsela tsa ione le li-enzyme, tse kenyelletsang li-receptor tsa motho le ram monoacylglycerol lipase. E bonts'etsa tšoaetso ea antiallodynic le antihyperalgesic ka mokhoa oa bohloko oa ho ruruha. In vitro, KDS-4103 e thibela tšebetso ea FAAH ka likarolo tse kholo tsa ho thibela lik'hemik'hale (IC (50)) ea 5 nM meleng ea boko ba likhohlo le 3 nM li-microrosomes tsa sebete. Ka vivo, KDS-4103 e thibela boko ba rat ho latela mosebetsi oa intraperitoneal (ip) ka tekanyo e tloaelehileng ea tlhaho (ID (50)) ea 0.15 mg / kg. Sebaka sena ha se sebetsane haholo le lipheo tse ling tse amanang le lefuba, ho akarelletsa le li-receptor tsa cannabinoid le lipalangoang tsa anandamide, kapa le sehlopha se pharaletseng sa li-receptors, mechine ea ion, ba tsamaisang thepa le li-enzyme. Ka puso ea ip ho litoe le litoeba KDS-4103 e na le mathata a bohlokoa, a tšoenyehileng a ho tšoenyeha, a nang le khatello ea kelello le a tšoanang, a thibeloang kalafo le bahanyetsi ba CB1. Ka lehlakoreng le leng, litekanyetso tse thibelang mosebetsi oa FAAH le ho hlahisa mekhoa ea boko ba anandamide haholo, KDS-4103 ha e hlahise likarolo tse tloaelehileng tsa kankere ea mofuta ona (mohlala, catalepsy, hypothermia, hyperphagia), ha e hlahise khethollo, ebile ha e hlahise tlhahiso liphello tsa khethollo tsa motsoako o sebetsang oa kannete, Delta9-tetrahydrocannabinol (Delta9-THC). Liphuputso tsena li fana ka maikutlo a hore KDS-4103 e etsa liketso ka ho ntlafatsa liketso tsa tonic tsa anandamide ka subset ea CB (1) receptors, eo ka tloaelo e sebetsanang ho laola maikutlo le bohloko. KDS-4103 e fumaneha molomong ka likhoto le litšoene tsa cynomolgus. Liphuputso tse entsoeng ka makhetlo a mangata a sa phekoleheng (1,500 mg / kg, ka bone) mefuta ena e 'meli ha e e-s'o hlahise chefo ea tsamaiso. Ka mokhoa o ts'oanang, ha ho na chefo e ileng ea boleloa ka libaktheria tsa cytotoxicity tlhahlobo ea vitro le ka tlhahlobo ea Ames. Ho feta moo, ha ho na litšenyehelo tse ileng tsa fumanoa likotong tse nang le tlhahlobo ea rotarod ka mor'a lefuba le ipatileng ka ip ka KDS-4103 ka tekanyo ea ho ea ho 5 mg / kg kapa ka sebete ea ho shebella ka morao ka mor'a hore e be molumo oa 1,500 mg / kg. Liphello li fana ka maikutlo a hore KDS-4103 e tla fana ka mokhoa o mocha le fensetere e ntle ea phekolo bakeng sa phekolo ea ho tšoenyeha, ho tepella maikutlong le bohloko.

 

5. URB597:

Ntho e nyenyane 10grams.
Tlhahlobo ka bongata bo tloaelehileng (ka hare ho 1kg) e ka romeloa lihora tse 12 kamora ho lefa.
Bakeng sa tlhahiso e kholo (ka hare ho 1kg) e ka romeloa ka matsatsi a sebetsang a 3 ka mor'a ts'ebetso.

 

6. Li-Recipes tsa URB597:

Ho botsa bareki ba rona baemeli ba rona (CSR) bakeng sa lintlha tse eketsehileng, bakeng sa boitsebiso ba hau.

 

7. Masole a URB597:

Ho fanoa nakong e tlang.

 


 

III. URB597 HNMR

 

Re li-poure tsa Aprepitant, Prepitant phofo e rekisoang, Raw Aprepitant powder (170729-80-3) hplc≥98% | Ho hlahisa li-Reagents tsa R & D

 


 

IV. Joang ho reka URB597 ho tloha AASraw?

 

1.To iteanye le rona ka imeile ea ronalenaneo la lipatlisiso, kapa skype ea inthanetengmoemeli oa tšebeletso ea bareki (CSR).
2.To re fane ka lipotso tsa hau le lipotso tsa hau.
3.Our CSR e tla u fa tlhaloso, nako ea ho lefa, nomoro ea ho latela, litsela tsa ho pepa le letsatsi la ho fihla ho fihlela (ETA).
4.Payment e entsoe mme thepa e tla romelloa ka lihora tsa 12 (Ho laela ka hare ho 10kg).
5.Goods e amohetse mme e fana ka litlhaloso.

 


 

Nahana hore u rata sehlahisoa sa hau sa blog:

 

 Phofo ea Basali? Ntho e 'ngoe le e' ngoe e buang ka ho ntlafatsa thobalano ho Flibanserin phofo Mokhoa oa ho sebelisa Clenbuterol bakeng sa tahlehelo ea boima ba 'mele Namrolone phofo e sebeliselitsoeng bakeng sa melemo ea / nandrolone ke efe?

 


 

Lintlha tse ling tse mabapi le lihlahisoa tsa bohlokoa,amohela ho tobetsa mona.


Bakeng sa lipotso, ka kopo ikopanye imeile , Ka tloaelo re arabela nakong ea lihora tsa 8.
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