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URB597

URB597, eyaziwa nangokuthi i-KDS-4103, inhibitor enamandla kakhulu kwaye ekhethiweyo ye-fatty-acid amide hydrolase (FAAH), i-enzyme eyenza i-intracellular hydrolysis ye-endocannabinoid i-anamamide, enexabiso le-50% inhibition concentration I-IC50 ye-4.6 nM ne-0.5 nM kwiimbumba zeengqondo zomlingo kunye ne-microsomes yesibindi somntu ngokulandelanayo. I-URB597 ibonisa i-anxiolytic, i-anti-depressant, i-antinociceptive kunye ne-analgesic imiphumo kwi-vivo ngaphandle kokukhupha ezinye iimpawu ezinxulumene nama-asnabinoid-like compounds.

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Ingcaciso yeMveliso

 

Ividiyo ye-URB597

 

 


 

I.URB597 Abalinganiswa basisiseko:

 

igama: URB597
CAS: 546141-08-6
Ukucoceka: ≥99% (HPLC)
I-molecular Formula: C20H22N2O3
Isisindo somzimba: 338.4
EINECS: 1312995-182-4
Iintetho: I-N-Cyclohexylcarbamic acid 3 '- (aminocarbonyl) [1,1'-biphenyl] -3-yl ester; 3'-CarbaMoyl- [XNUM''-biphenyl] -1,1-yl cyclohexylcarbaMate; 3- (3-carbaMoylphenyl) phenyl N-cyclohexylcarbaMate I-CarbaMic acid, i-N-cyclohexyl-, i-3 '- (aMinocarbonyl) [3'-biphenyl] -1,1-yl ester; i-KDS 3 N-Cyclohexylcarbamic acid 4103' - (aminocarbonyl) [3'-biphenyl] -1,1-yl ester I-N-Cyclohexylcarbamic acid 3 '- (aminocarbonyl) [3'-biphenyl] -1,1-yl ester URB 3 KDS 597; URB 4103,> = 597%; APD98 (URB597)
Melt Point: 155-157 ° C
Alpha: D + 5 ° (c = 0.437 kwi-chloroform)
Isitoreji sokugcina: 2-8 ° C
I-DMSO enamandla i-soluble2mg / mL, icacile (ifudumele)
umbala: OMhlophe

 


 

II. Ukusetyenziswa kwe-URB597 kumjikelezo:

 

1.Name:

URB597

 

2.Kuphi umsebenzi we-URB597?

Isisombululo: Inkxalabo enkulu yeklinikhi yokusetyenziswa kwe-cannabinoid receptor i-1 (CB1) i-agonists ngokuthe ngqo kukuba ezi zixhobo zandisa ukusela utywala kunye nokuziphatha kakubi kweziyobisi. Njengendlela enye, imisebenzi ye-CB1-receptor-mediated ingenziwa lula ngokunyusa amanqanaba e-anandamide ngokusetyenziswa kwe-hydrolase fatty acid amide hydrolase (FAAH) inhibitors. Injongo: Ukusebenzisa i-FAAH inhibitor ye-URB597 ekhethiweyo, siphucule ukuba ukusetyenziswa kwetoni ye-cannabinoid engapheliyo kwandisa uxanduva lokusetyenziswa kakubi kotywala, njengoko kwenzekayo kunye ne-CB1 receptor ngqo kwi-agonists. Izinto kunye neendlela: I-URB597 yavavanywa ekulawuleni utywala kwiiliti ze-Wistar kunye nokuphuza utshwala kotywala ekukhethiweyo kwiMarchigian Sardinian-choice (msP). Kwiiriti zeWistar, iimiphumo ze-URB597 ngokuxhalabisa utywala kunye noxinzelelo-, i-yohimbine- kunye ne-cue-induced incarnation of the alcohol alcohol Ukuthelekisa, umphumo we-CB1 ummkeli ophikisanayo kunye ne-ethanol ukulawulwa kwe-self-administration kwavanywa kwakhona. Iziphumo: Ngaphantsi kwimeko yethu yokulinga, ukuphathwa kwe-intraperitoneal (IP) ye-URB597 (0.0, 0.3 kunye ne-1.0 mg / kg) ayikwenyanga ngokuzenzekelayo ukusetyenziswa kotywala kotywala kwi-rp i-rats okanye ukulungelelanisa umlinganiselo ochanekileyo we-1 kunye nomlinganiselo wokuqhubela utywala ulawulo lwezolawulo kwii-Wistars ezingafunekiyo. Kwiimvavanyo zokubuyiselwa, i-compound ayizange ibe nempembelelo kwi-cue-, i-foothock stress-and stimulated-back stimulation. Ngakolunye uhlangothi, i-URB597 yatshitshisa ngokupheleleyo impendulo yokuxhalaxwa kwimiba yokuxhatshazwa emva kokuhoxiswa emva kolawulo lwe-IP olunxilisayo (3.0 g / kg). I-Rimonabant (0.0, 0.3, 1.0 kunye ne-3.0 mg / kg) yanciphisa kakhulu i-ethanol yokulawula. Izigqibo: Iziphumo zibonisa ukuba ukusebenza kwenkqubo ye-anandamide yokugcina i-endocannabinoid ngokuchithwa okukhethiweyo kwe-FAAH ayinyuli umngcipheko wokusetyenziswa kakubi kotywala kodwa kunciphisa ukuxhalabisa okunxulumene nokuhoxiswa kotywala. Ngaloo ndlela singacinga ukuba amayeza asekelwe ekusebenziseni i-modocannabinoid system modulators ezifana ne-URB597 inokunika iingenelo ezibalulekileyo xa kuthelekiswa nophatho kunye nabasebenzi basebenzayo be-CB1.

 

3.Iyasebenza kwi-URB597?

Iimpembelelo ze-URB 597 yedwa kunye kunye ne-anandamide zaphandwa kwelinye iqela leenkwenkwezi (n = 4) ezahlula i-Δ9-THC (0.1 mg · kg-1 iv) kwizithuthi, nakwelinye iqela (n = 5) elifumana engapheliyo Δ9-THC (1 mg · kg-112 h-1 sc) eyahlula umchasane ongenakunozinyo (1 mg · kg-1 iv).

 

4.Iminye imiyalelo:

I-URB 597 ikhulise imiphumo yokuziphatha ye-anandamide kodwa ayikho enye i-CB1 agonists. Nangona kunjalo, i-URB 597 ayizange ikhulise ngokukodwa ukucinywa kwe-Δ9-THC ukukhishwa kwe-anandamide. Ngokuqokeleleneyo, le nkcukacha zibonisa ukuba i-anandamide engapheliyo ebuchosheni bobuchopho ayifani ngokukhawuleza nemiphumo yokuziphatha ye-anandamide ephathekayo.

I-Potential ne-selective acety acid i-amide hydrolase (FAAH) inhibitor (ixabiso le-IC50 yi-3 kunye ne-5 nM kwisibindi somntu kunye nobuchopho besilathisi, ngokulandelanayo). Imiboniso ayikho into ebalulekileyo yokuvimbela izinto ezahlukeneyo, iimon i-ion kunye ne-enzyme, kuquka i-receptor yabantu abangenawo umbane kunye ne-rat monoacylglycerol lipase. Ubonisa umsebenzi we-antiallodynic kunye ne-antihyperalgesic kwimodeli evuthayo. I-In vitro, i-KDS-4103 inqanda umsebenzi we-FAAH ngamanqanaba emimiselo engavumelekanga (IC (50)) ye-5 nM kwiimbumbulu zengqondo kunye ne-3 nM kwi-microsomes yesibindi somntu. Ku-vivo, i-KDS-4103 inqanda ubuchopho besilathisi se-FAAH emva kokulawulwa kwe-intraperitoneal (ip) kunye ne-dose inhibitory dose (ID (50)) ye-0.15 mg / kg. I-compound ayihambelani kakhulu kunye nezinye iithagethi ezinxulumene ne-cannabinoid, kuquka i-receptors ye-cannabinoid kunye ne-anandamide zothutho, okanye nepaneli ebanzi yama-receptors, iziteshi ze-ion, abathumeli kunye ne-enzymes. Ngolawulo lwe-ip kwiisundu kunye neenkondlo ze-KDS-4103 zibangela izinto ezibalulekileyo, ezinjenge-anxiolytic, ezinjenge-anti-depressant-like and analgesic effects, eziye zithintelwa unyango kunye nabaxhamli be-CB1. Ngokwahlukileyo, kwii-doses ezivimbela kakhulu umsebenzi we-FAAH kwaye ziphakamisa amanqanaba e-anandamide engqondweni, i-KDS-4103 ayiyikukhupha imiphumo ye-cannabinoid (njenge-catalepsy, hypothermia, hyperphagia), ayiyi kubangela indawo, iziphumo ezichasayo zesithako esisebenzayo senkunkuma, i-Delta9-tetrahydrocannabinol (i-Delta9-THC). Ezi ziphumo zibonisa ukuba izenzo ze-KDS-4103 ngokuphucula izenzo zethoni ze-anandamide kwi-subset ye-CB (1) i-receptors, enokuqhelekileyo ibe neengxaki zokulawula iimvakalelo nentlungu. I-KDS-4103 ifumaneka ngomlomo kwiinki kunye neenkomo ze-cynomolgus. Izifundo eziphindaphindiweyo zezilwanyana (1,500 mg / kg, nge-os) kwezi zimbini zezilwanyana aziboniswanga ngendlela enobuqhetseba. Ngokufanayo, akukho netyhefu yaqatshelwa kwii-bacterial cytotoxicity tests in vitro nakuvavanyo lwe-Ames. Ukongezelela, akukho ziphulo eziye zaphawulwa kwiinqongi kwi-test ye-rotarod emva kokunyanga kwe-ip ye-ip kunye ne-KDS-4103 kumayeza ukuya kwi-5 mg / kg okanye kwibhethri yokuqwalasela esebenzayo emva kwemiyalelo yomlomo ukuya kwi-1,500 mg / kg. Iziphumo zibonisa ukuba i-KDS-4103 iya kunika indlela enomdla ngefestile efanelekileyo yokunyanga, ukuxinezeleka kunye nentlungu.

 

5. URB597:

I-10grams encinci.
Uphando malunga nobukhulu obuqhelekileyo (ngaphakathi kwe-1kg) lungathunyelwa kwiiyure ze-12 emva kokuhlawula.
Ukwenza umlinganiselo omkhulu (ngaphakathi kwe-1kg) ungathunyelwa kwimihla yokusebenza ye-3 emva kokuhlawula.

 

6. URB597 Recipes:

Ukubuza ummeli wethu ummeli (Representative Representative) (CSR) ngeenkcukacha, ngokubhekiselele kuyo.

 

7. Ukuthengiswa kweRB597:

Ukubonelelwa kwikamva elizayo.

 


 

III. I-URB597 HNMR

 

Siyi-Aprepitant powder supplie, i-Aprepitant powder yokuthengisa, i-Raw Aprepitant powder (170729-80-3) hplc =98% | Ukurhoxisa iR & D Reagents

 


 

IV. Indlela yokuthenga i-URB597 kwi-AASraw?

 

1.Qhagamshelana nathi nge-imeyile yethuinkqubo yophando, okanye i-skype ye-intanethiummeli wenkonzo yamakhasimende (CSR).
2.Ukusibonelela ngobuninzi bakho kunye neadesi.
I-3.I-CSR yethu iya kukunika isingeniso, ixesha lokuhlawula, inombolo yokulandelela, iindlela zokuhambisa kunye nomhla wokufika oqikelelwayo (i-ETA).
I-4.Inkokhelo eyenziwe kwaye iimpahla ziya kuthunyelwa kwiiyure ze-12 (Ukuze ulandelwe ngaphakathi kwe-10kg).
5.Goods zifunyenwe kwaye zinike izimvo.

 


 

Cinga ibhlogi yakho yomkhiqizo oyintandokazi:

 

 Viagra? Yonke into malunga noTywala yaseFlibanserin Indlela yokusebenzisa i-Clenbuterol yokulahleka kwesisindo Yintoni i-nandrolone powder esetyenziselwa i-nandrolone inzuzo?

 


 

Ingcaciso engakumbi ngemveliso echaphazelekayo,wamkele ukucofa apha.


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