A dual GLP-1R and CCK2 receptor agonist
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ZP3022

Item No. 42636

Technical Information
Formal Name
L-histidylglycyl-L-α-glutamylglycyl-L-threonyl-L-phenylalanyl-L-threonyl-L-seryl-L-α-aspartyl-L-leucyl-L-seryl-L-lysyl-L-glutaminyl-L-methionyl-L-α-glutamyl-L-α-glutamyl-L-α-glutamyl-L-alanyl-L-valyl-L-arginyl-L-leucyl-L-phenylalanyl-L-isoleucyl-L-α-glutamyl-L-tryptophyl-L-leucyl-L-lysyl-L-asparaginyl-2- [2-(2-aminoethoxy)ethoxy] acetyl-2-[2- (2-aminoethoxy)ethoxy] acetyl-L-tyrosylglycyl-L-tryptophyl-L-leucyl-L-α-aspartyl-L-phenylalaninamide
CAS Number
1345835-12-2
Molecular Formula
C199H294N48O61S
Formula Weight
Purity
≥95%
Formulation
A solid
DMSO: Soluble: ≥10 mg/mlPBS (pH 7.2): Slightly soluble: 0.1-1 mg/ml
SMILES
O=C(COCCOCCNC(COCCOCCNC([C@H](CC(N)=O)NC([C@H](CCCCN)NC([C@H](CC(C)C)NC([C@H](CC1=CNC2=C1C=CC=C2)NC([C@H](CCC(O)=O)NC([C@H]([C@@H](C)CC)NC([C@H](CC3=CC=CC=C3)NC([C@H](CC(C)C)NC([C@H](CCCNC(N)=N)NC([C@H](C(C)C)NC([C@H](C)NC([C@H](CCC(O)=O)NC([C@H](CCC(O)=O)NC([C@H](CCC(O)=O)NC([C@H](CCSC)NC([C@H](CCC(N)=O)NC([C@H](CCCCN)NC([C@H](CO)NC([C@H](CC(C)C)NC([C@H](CC(O)=O)NC([C@H](CO)NC([C@H]([C@H](O)C)NC([C@H](CC4=CC=CC=C4)NC([C@H]([C@H](O)C)NC(CNC([C@H](CCC(O)=O)NC(CNC([C@H](CC5=CNC=N5)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)N[C@H](C(NCC(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N)=O)CC6=CC=CC=C6)=O)CC(O)=O)=O)CC(C)C)=O)CC7=CNC8=C7C=CC=C8)=O)=O)CC9=CC=C(C=C9)O
InChi Code
InChI=1S/C199H294N48O61S/c1-17-108(12)165(196(302)230-133(58-64-161(268)269)181(287)237-144(87-117-93-213-124-45-30-28-43-121(117)124)188(294)234-136(78-103(2)3)183(289)222-126(47-32-34-67-201)176(282)238-145(89-151(204)254)172(278)210-70-72-306-73-75-307-100-155(258)209-69-71-305-74-76-308-101-156(259)221-140(85-115-49-51-119(252)52-50-115)173(279)216-96-153(256)220-143(86-116-92-212-123-44-29-27-42-120(116)123)187(293)233-138(80-105(6)7)185(291)239-146(90-162(270)271)189(295)231-135(168(205)274)82-112-36-21-18-22-37-112)246-191(297)141(83-113-38-23-19-24-39-113)236-184(290)137(79-104(4)5)232-177(283)127(48-35-68-211-199(206)207)229-195(301)164(107(10)11)245-169(275)109(13)218-174(280)130(55-61-158(262)263)225-179(285)131(56-62-159(264)265)226-180(286)132(57-63-160(266)267)227-182(288)134(65-77-309-16)228-178(284)129(53-59-150(203)253)224-175(281)125(46-31-33-66-200)223-193(299)148(98-248)242-186(292)139(81-106(8)9)235-190(296)147(91-163(272)273)240-194(300)149(99-249)243-198(304)167(111(15)251)247-192(298)142(84-114-40-25-20-26-41-114)241-197(303)166(110(14)250)244-154(257)97-215-171(277)128(54-60-157(260)261)219-152(255)95-214-170(276)122(202)88-118-94-208-102-217-118/h18-30,36-45,49-52,92-94,102-111,122,125-149,164-167,212-213,248-252H,17,31-35,46-48,53-91,95-101,200-202H2,1-16H3,(H2,203,253)(H2,204,254)(H2,205,274)(H,208,217)(H,209,258)(H,210,278)(H,214,276)(H,215,277)(H,216,279)(H,218,280)(H,219,255)(H,220,256)(H,221,259)(H,222,289)(H,223,299)(H,224,281)(H,225,285)(H,226,286)(H,227,288)(H,228,284)(H,229,301)(H,230,302)(H,231,295)(H,232,283)(H,233,293)(H,234,294)(H,235,296)(H,236,290)(H,237,287)(H,238,282)(H,239,291)(H,240,300)(H,241,303)(H,242,292)(H,243,304)(H,244,257)(H,245,275)(H,246,297)(H,247,298)(H,260,261)(H,262,263)(H,264,265)(H,266,267)(H,268,269)(H,270,271)(H,272,273)(H4,206,207,211)/t108-,109-,110+,111+,122-,125-,126-,127-,128-,129-,130-,131-,132-,133-,134-,135-,136-,137-,138-,139-,140-,141-,142-,143-,144-,145-,146-,147-,148-,149-,164-,165-,166-,167
InChi Key
NNIQIOUWVDDUSE-GGXPHKMXSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    ZP3022 is a dual agonist of the glucagon-like peptide 1 receptor (GLP-1R) and cholecystokinin 2 (CCK2) receptor.1 It selectively increases cAMP accumulation or ERK phosphorylation in HEK293 cells expressing GLP-1R or the CCK2 receptor over ERK phosphorylation in HEK293 cells expressing the CCK1 receptor (EC50s = 0.02, 10.3, and >1,000 nM, respectively, for the human receptors). ZP3022 (40 nM) increases the proliferation of rat neonatal β-cells in vitro.2 It also increases glucose-induced insulin secretion (GSIS) in rat pancreatic islets when used at concentrations of 10 and 100 nM and reduces body weight in rats when administered at a dose of 40 nmol/kg twice per day. ZP3022 (100 nmol/kg per day) increases β-cell mass and total pancreatic mass and improves glucose tolerance in db/db mice.1 It also reduces food intake but not body weight in db/db mice.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Fosgerau, K., Jessen, L., Lind Tolborg, J., et alThe novel GLP-1-gastrin dual agonist, ZP3022, increases β-cell mass and prevents diabetes in db/db mice. Diabetes Obes. Metab. 15(1), 62-71 (2013).

    2. Skarbaliene, J., Rigbolt, K.T., Fosgerau, K., et alIn-vitro and in-vivo studies supporting the therapeutic potential of ZP3022 in diabetes. Eur. J. Pharmacol. 815, 181-189 (2017).