Ecnoglutide

Ecnoglutide is a cAMP-biased peptide glucagon-like peptide 1 receptor (GLP-1R) agonist. It selectively induces cAMP accumulation over beta-arrestin recruitment (EC50s = 0.018 and 1,300 nM, respectively) without inducing GLP-1R receptor internalization (EC50 = >10,000 nM) in cell-based assays using human GLP-1R. In vivo, ecnoglutide (0.15 mg/kg) reduces fasting and post-prandial blood glucose levels in db/db mice. It also reduces body weight and food intake in db/db mice when administered at a dose of 0.05 mg/kg.Formal Name: L-histidyl-L-valyl-L-alpha-glutamylglycyl-L-threonyl-L-phenylalanyl-L-threonyl-L-seryl-L-alpha-aspartyl-L-valyl-L-seryl-L-seryl-L-tyrosyl-L-leucyl-L-alpha-glutamyl-L-alpha-glutamyl-L-glutaminyl-L-alanyl-L-alanyl-L-arginyl-L-alpha-glutamyl-L-phenylalanyl-L-isoleucyl-N6-[N-(17-carboxy-1-oxoheptadecyl)-L-gamma-glutamyl-2-[2-(2-aminoethoxy)ethoxy]acetyl-2-[2-(2-aminoethoxy)ethoxy]acetyl]-L-lysyl-L-tryptophyl-L-leucyl-L-valyl-L-arginylglycyl-L-arginyl-glycine. CAS Number: 2459531-73-6. Synonyms: XW003. Molecular Formula: C194H304N48O61. Formula Weight: 4284.8. Purity: >98%. Formulation: (Request formulation change), A solid. Peptide Sequence: HVEGTFTSDVSSYLEEQAAREFIK-(AEEA-AEEA-{gamma-Glu}-C18 diacid)-WLVRGRG (AEEA = 2-(2-(2-aminoethoxy)ethoxy)acetic acid). Solubility: DMSO: Sparingly soluble: 1-10 mg/ml. SMILES: O=C([C@@H](N)CC1=CNC=N1)N[C@H](C(N[C@H](C(NCC(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(NCC(N[C@H](C(NCC(O)=O)=O)CCCNC(N)=N)=O)=O)CCCNC(N)=N)=O)C(C)C)=O)CC(C)C)=O)CC2=CNC3=C2C=CC=C3)=O)CCCCNC(COCCOCCNC(COCCOCCNC(CC[C@H](NC(CCCCCCCCCCCCCCCCC(O)=O)=O)C(O)=O)=O)=O)=O)=O)[C@H](CC)C)=O)CC4=CC=CC=C4)=O)CCC(O)=O)=O)CCCNC(N)=N)=O)C)=O)C)=O)CCC(N)=O)=O)CCC(O)=O)=O)CCC(O)=O)=O)CC(C)C)=O)CC5=CC=C(C=C5)O)=O)CO)=O)CO)=O)C(C)C)=O)CC(O)=O)=O)CO)=O)[C@@H](C)O)=O)CC6=CC=CC=C6)=O)[C@@H](C)O)=O)=O)CCC(O)=O)=O)C(C)C. InChi Code: InChI=1S/C194H304N48O61/c1-17-109(12)160(188(295)225-125(51-40-41-73-204-148(254)101-302-83-82-301-80-78-206-149(255)102-303-84-81-300-79-77-205-144(250)68-62-132(191(298)299)218-145(251)55-36-28-26-24-22-20-18-19-21-23-25-27-29-37-56-150(256)257)171(278)231-138(90-117-93-210-122-50-39-38-49-120(117)122)177(284)228-134(86-105(4)5)178(285)239-158(107(8)9)186(293)224-124(53-43-75-208-193(199)200)167(274)211-95-146(252)217-123(52-42-74-207-192(197)198)166(273)213-97-156(268)269)241-179(286)136(87-114-45-32-30-33-46-114)229-174(281)131(66-72-154(264)265)221-170(277)126(54-44-76-209-194(201)202)219-164(271)111(14)215-163(270)110(13)216-169(276)128(61-67-143(196)249)220-172(279)129(64-70-152(260)261)222-173(280)130(65-71-153(262)263)223-175(282)133(85-104(2)3)227-176(283)135(89-116-57-59-119(248)60-58-116)230-182(289)140(98-243)234-184(291)142(100-245)235-187(294)159(108(10)11)240-181(288)139(92-155(266)267)232-183(290)141(99-244)236-190(297)162(113(16)247)242-180(287)137(88-115-47-34-31-35-48-115)233-189(296)161(112(15)246)237-147(253)96-212-168(275)127(63-69-151(258)259)226-185(292)157(106(6)7)238-165(272)121(195)91-118-94-203-103-214-118/h30-35,38-39,45-50,57-60,93-94,103-113,121,123-142,157-162,210,243-248H,17-29,36-37,40-44,51-56,61-92,95-102,195H2,1-16H3,(H2,196,249)(H,203,214)(H,204,254)(H,205,250)(H,206,255)(H,211,274)(H,212,275)(H,213,273)(H,215,270)(H,216,276)(H,217,252)(H,218,251)(H,219,271)(H,220,279)(H,221,277)(H,222,280)(H,223,282)(H,224,293)(H,225,295)(H,226,292)(H,227,283)(H,228,284)(H,229,281)(H,230,289)(H,231,278)(H,232,290)(H,233,296)(H,234,291)(H,235,294)(H,236,297)(H,237,253)(H,238,272)(H,239,285)(H,240,288)(H,241,286)(H,242,287)(H,256,257)(H,258,259)(H,260,261)(H,262,263)(H,264,265)(H,266,267)(H,268,269)(H,298,299)(H4,197,198,207)(H4,199,200,208)(H4,201,202,209)/t109-,110-,111-,112+,113+,121-,123-,124-,125-,126-,127-,128-,129-,130-,131-,132-,133-,134-,135-,136-,137-,138-,139-,140-,141-,142-,157-,158-,159-,160-,161-,162-/m0/s1. InChi Key: DJMLKAVQDZZBNC-NYHUXPQOSA-N.