Glepaglutide (acetate)

Glepaglutide is a peptide agonist of the glucagon-like peptide 2 receptor (GLP-2R). It selectively induces cAMP accumulation in HEK293 cells expressing GLP-2R over those expressing GLP-1R (EC50s = 0.24 and 8.7 nM, respectively, for the human receptors). Glepaglutide (10 mg/kg per day for 26 weeks) increases mucosal hyperplasia thickness in the duodenum, jejunum, and ileum, as well as increases small intestinal wet weight and length, an effect that lasts six weeks post-administration, in rats. It also increases small intestinal mass and length, as well as reduces ileal levels of alpha-1-acid glycoprotein (AGP 1) and myeloperoxidase (MPO), in a rat model of inflammatory bowel disease (IBD) induced by indomethacin (Cay-70270) when administered at a dose of 400 nmol/kg twice per day.Synonyms: ZP1848. Molecular Formula: C197H325N53O55 . XC2H4O2. Formula Weight: 4316.1. Purity: >95%. Formulation: (Request formulation change), A solid. Peptide Sequence: HGEGTFSSELATILDALAARDFIAWLIATKITDKKKKKK-NH2. Solubility: PBS (pH 7.2): Slightly Soluble: 0.1-1 mg/ml. SMILES: [H]N[C@H](C(NCC(N[C@@H](CCC(O)=O)C(NCC(N[C@]([C@@H](C)O)([H])C(N[C@H](C(N[C@@H](CO)C(N[C@@H](CO)C(N[C@@H](CCC(O)=O)C(N[C@@H](CC(C)C)C(N[C@H](C(N[C@]([C@@H](C)O)([H])C(N[C@]([C@H](CC)C)([H])C(N[C@@H](CC(C)C)C(N[C@H](C(N[C@H](C(N[C@@H](CC(C)C)C(N[C@H](C(N[C@H](C(N[C@@H](CCCNC(N)=N)C(N[C@H](C(N[C@H](C(N[C@]([C@H](CC)C)([H])C(N[C@H](C(N[C@H](C(N[C@@H](CC(C)C)C(N[C@]([C@H](CC)C)([H])C(N[C@H](C(N[C@]([C@@H](C)O)([H])C(N[C@@H](CCCCN)C(N[C@]([C@H](CC)C)([H])C(N[C@]([C@@H](C)O)([H])C(N[C@H](C(N[C@@H](CCCCN)C(N[C@@H](CCCCN)C(N[C@@H](CCCCN)C(N[C@@H](CCCCN)C(N[C@@H](CCCCN)C(N[C@@H](CCCCN)C(N)=O)=O)=O)=O)=O)=O)=O)CC(O)=O)=O)=O)=O)=O)=O)C)=O)=O)=O)CC1=CNC2=C1C=CC=C2)=O)C)=O)=O)CC3=CC=CC=C3)=O)CC(O)=O)=O)=O)C)=O)C)=O)=O)C)=O)CC(O)=O)=O)=O)=O)=O)C)=O)=O)=O)=O)=O)CC4=CC=CC=C4)=O)=O)=O)=O)=O)CC5=CN=CN5.CC(O)=O. InChi Code: InChI=1S/C197H325N53O55.C2H4O2/c1-27-102(13)152(190(299)220-111(22)166(275)248-157(113(24)254)194(303)230-129(66-45-52-78-204)176(285)244-155(105(16)30-4)192(301)250-158(114(25)255)195(304)240-142(90-151(267)268)183(292)228-128(65-44-51-77-203)173(282)227-127(64-43-50-76-202)172(281)226-126(63-42-49-75-201)171(280)225-125(62-41-48-74-200)170(279)224-124(61-40-47-73-199)169(278)222-123(160(206)269)60-39-46-72-198)245-185(294)136(83-101(11)12)234-182(291)139(86-118-91-211-122-59-38-37-58-120(118)122)232-164(273)109(20)219-189(298)153(103(14)28-2)246-186(295)138(85-117-56-35-32-36-57-117)235-184(293)141(89-150(265)266)236-174(283)130(67-53-79-210-197(207)208)223-162(271)107(18)215-161(270)106(17)216-177(286)133(80-98(5)6)231-163(272)108(19)217-179(288)140(88-149(263)264)237-180(289)135(82-100(9)10)238-191(300)154(104(15)29-3)247-196(305)159(115(26)256)249-165(274)110(21)218-178(287)134(81-99(7)8)233-175(284)132(69-71-148(261)262)229-187(296)143(95-251)242-188(297)144(96-252)241-181(290)137(84-116-54-33-31-34-55-116)239-193(302)156(112(23)253)243-146(258)94-213-168(277)131(68-70-147(259)260)221-145(257)93-212-167(276)121(205)87-119-92-209-97-214-119,1-2(3)4/h31-38,54-59,91-92,97-115,121,123-144,152-159,211,251-256H,27-30,39-53,60-90,93-96,198-205H2,1-26H3,(H2,206,269)(H,209,214)(H,212,276)(H,213,277)(H,215,270)(H,216,286)(H,217,288)(H,218,287)(H,219,298)(H,220,299)(H,221,257)(H,222,278)(H,223,271)(H,224,279)(H,225,280)(H,226,281)(H,227,282)(H,228,292)(H,229,296)(H,230,303)(H,231,272)(H,232,273)(H,233,284)(H,234,291)(H,235,293)(H,236,283)(H,237,289)(H,238,300)(H,239,302)(H,240,304)(H,241,290)(H,242,297)(H,243,258)(H,244,285)(H,245,294)(H,246,295)(H,247,305)(H,248,275)(H,249,274)(H,250,301)(H,259,260)(H,261,262)(H,263,264)(H,265,266)(H,267,268)(H4,207,208,210),1H3,(H,3,4)/t102-,103-,104-,105-,106-,107-,108-,109-,110-,111-,112+,113+,114+,115+,121-,123-,124-,125-,126-,127-,128-,129-,130-,131-,132-,133-,134-,135-,136-,137-,138-,139-,140-,141-,142-,143-,144-,152-,153-,154-,155-,156-,157-,158-,159-,/m0./s1. InChi Key: OTEFGBFHVADIFU-JHLBKGQUSA-N.