Tirzepatide (sodium salt)

Tirzepatide is an agonist of glucagon-like peptide 1 receptor (GLP-1R) and gastric inhibitory polypeptide (GIP) receptor. It induces cAMP production in HEK293 cells expressing human GLP-1R or human GIP receptor (EC50s = 6.54 and 1.01 nM, respectively). Tirzepatide (100 nM) induces receptor internalization in HEK293 cells expressing human GLP-1R or GIP receptor. In vivo, tirzepatide (10 nmol/kg per day) decreases body weight, food intake, plasma levels of leptin, triglycerides, and free fatty acids (FFAs), hepatic levels of triglycerides, and blood glucose levels in a mouse model of high-fat diet-induced obesity. It prevents A. alternata-induced increases in the numbers of eosinophils and lymphocytes in the bronchoalveolar lavage fluid (BALF) from A. alternata-challenged mice when administered at a dose of 50 nmol/kg every three days. Tirzepatide (50 nmol/kg every three days) inhibits bronchoconstriction induced by the muscarinic receptor agonist methacholine (acetyl-beta-methylcholine, Cay-23092) in a mouse model of diabetes-induced asthma. Formulations containing tirzepatide have been used in the treatment of type 2 diabetes mellitus.Formal Name: L-tyrosyl-2-methylalanyl-L-alpha-glutamylglycyl-L-threonyl-L-phenylalanyl-L-threonyl-L-seryl-L-alpha-aspartyl-L-tyrosyl-L-seryl-L-isoleucyl-2-methylalanyl-L-leucyl-L-alpha-aspartyl-L-lysyl-L-isoleucyl-L-alanyl-L-glutaminyl-N6-[(22S)-22,42-dicarboxy-1,10,19,24-tetraoxo-3,6,12,15-tetraoxa-9,18,23-triazadotetracont-1-yl]-L-lysyl-L-alanyl-L-phenylalanyl-L-valyl-L-glutaminyl-L-tryptophyl-L-leucyl-L-isoleucyl-L-alanylglycylglycyl-L-prolyl-L-seryl-L-serylglycyl-L-alanyl-L-prolyl-L-prolyl-L-prolyl-L-serinamide, sodium salt. Synonyms: LY3298176. Molecular Formula: C225H348N48O68 . XNa. Formula Weight: 4813.5. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: Water: Soluble. SMILES: OC[C@@H](C(N)=O)NC([C@H]1N(C([C@H]2N(C([C@H]3N(C([C@H](C)NC(CNC([C@H](CO)NC([C@H](CO)NC([C@H]4N(C(CNC(CNC([C@H](C)NC([C@H]([C@@H](C)CC)NC([C@H](CC(C)C)NC([C@H](CC5=CNC6=C5C=CC=C6)NC([C@H](CCC(N)=O)NC([C@H](C(C)C)NC([C@H](CC7=CC=CC=C7)NC([C@H](C)NC([C@H](CCCCNC(COCCOCCNC(COCCOCCNC(CC[C@@H](C(O)=O)NC(CCCCCCCCCCCCCCCCCCC(O)=O)=O)=O)=O)=O)NC([C@H](CCC(N)=O)NC([C@H](C)NC([C@H]([C@@H](C)CC)NC([C@H](CCCCN)NC([C@H](CC(O)=O)NC([C@H](CC(C)C)NC(C(C)(C)NC([C@H]([C@@H](C)CC)NC([C@H](CO)NC([C@H](CC8=CC=C(O)C=C8)NC([C@H](CC(O)=O)NC([C@H](CO)NC([C@H]([C@H](O)C)NC([C@H](CC9=CC=CC=C9)NC([C@H]([C@H](O)C)NC(CNC([C@H](CCC(O)=O)NC(C(C)(C)NC([C@H](CC%10=CC=C(O)C=C%10)N)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)CCC4)=O)=O)=O)=O)=O)CCC3)=O)CCC2)=O)CCC1)=O.[Na]. InChi Code: InChI=1S/C225H348N48O68.Na/c1-23-126(10)183(264-198(311)146(64-50-52-88-226)246-202(315)157(109-180(297)298)252-199(312)152(103-124(6)7)261-223(337)225(21,22)269-217(330)185(128(12)25-3)266-209(322)163(120-278)257-200(313)153(107-138-74-78-141(282)79-75-138)250-203(316)158(110-181(299)300)253-207(320)162(119-277)259-216(329)187(134(18)280)267-206(319)155(106-136-60-44-41-45-61-136)254-215(328)186(133(17)279)262-174(289)114-237-193(306)147(83-87-179(295)296)260-222(336)224(19,20)268-192(305)143(227)104-137-72-76-140(281)77-73-137)214(327)242-131(15)190(303)244-148(80-84-168(228)283)196(309)245-145(65-51-53-89-231-175(290)121-340-100-99-339-97-91-233-176(291)122-341-101-98-338-96-90-232-170(285)86-82-150(221(334)335)243-171(286)70-46-38-36-34-32-30-28-26-27-29-31-33-35-37-39-47-71-178(293)294)195(308)240-130(14)191(304)248-154(105-135-58-42-40-43-59-135)205(318)263-182(125(8)9)212(325)247-149(81-85-169(229)284)197(310)251-156(108-139-111-234-144-63-49-48-62-142(139)144)201(314)249-151(102-123(4)5)204(317)265-184(127(11)24-2)213(326)241-129(13)189(302)236-112-172(287)235-115-177(292)270-92-54-66-164(270)210(323)258-161(118-276)208(321)256-160(117-275)194(307)238-113-173(288)239-132(16)218(331)272-94-56-68-166(272)220(333)273-95-57-69-167(273)219(332)271-93-55-67-165(271)211(324)255-159(116-274)188(230)301,/h40-45,48-49,58-63,72-79,111,123-134,143,145-167,182-187,234,274-282H,23-39,46-47,50-57,64-71,80-110,112-122,226-227H2,1-22H3,(H2,228,283)(H2,229,284)(H2,230,301)(H,231,290)(H,232,285)(H,233,291)(H,235,287)(H,236,302)(H,237,306)(H,238,307)(H,239,288)(H,240,308)(H,241,326)(H,242,327)(H,243,286)(H,244,303)(H,245,309)(H,246,315)(H,247,325)(H,248,304)(H,249,314)(H,250,316)(H,251,310)(H,252,312)(H,253,320)(H,254,328)(H,255,324)(H,256,321)(H,257,313)(H,258,323)(H,259,329)(H,260,336)(H,261,337)(H,262,289)(H,263,318)(H,264,311)(H,265,317)(H,266,322)(H,267,319)(H,268,305)(H,269,330)(H,293,294)(H,295,296)(H,297,298)(H,299,300)(H,334,335),/t126-,127-,128-,129-,130-,131-,132-,133+,134+,143-,145-,146-,147-,148-,149-,150-,151-,152-,153-,154-,155-,156-,157-,158-,159-,160-,161-,162-,163-,164-,165-,166-,167-,182-,183-,184-,185-,186-,187-,/m0./s1. InChi Key: LBSFXXWYNMVYDU-ILCOAZDTSA-N.