2. GPCR/G Protein
  3. GCGR
  4. LY3324954

LY3324954 is a long-acting, highly selective glucagon receptor (GCGR) agonist. LY3324954 stimulates cAMP production via the hepatic GCGR signaling pathway and induces acute blood glucose elevation, while promoting FGF21 expression in the liver and plasma. LY3324954 reduces body weight and abdominal fat mass, increases energy expenditure, and effectively improves lipid homeostasis, insulin sensitivity, and glucose intolerance. LY3324954 can be used in obesity-related research.

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LY3324954

LY3324954 Chemical Structure

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LY3324954 Related Antibodies

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Description

LY3324954 is a long-acting, highly selective glucagon receptor (GCGR) agonist. LY3324954 stimulates cAMP production via the hepatic GCGR signaling pathway and induces acute blood glucose elevation, while promoting FGF21 expression in the liver and plasma. LY3324954 reduces body weight and abdominal fat mass, increases energy expenditure, and effectively improves lipid homeostasis, insulin sensitivity, and glucose intolerance. LY3324954 can be used in obesity-related research[1][2][3].

In Vitro

LY3324954 (1×10-14 M - 1×10-6 M; 30 min) potently activates human GCGR-expressing HEK293 cells with an EC50 of 5.472×10-10 M, demonstrating greater potency than native glucagon[1].
LY3324954 stimulates glucose output from human iPSC-derived hepatocytes to a comparable extent as native glucagon[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

LY3324954 Related Antibodies
Parmacokinetics
Species Dose Route Tmax Cmax AUC0-inf T1/2 CL/F
Mice[1] 300 nmol/Kg s.c. 6 h 668 nM 11899 nM·h 6.5 h 25 mL/h/kg
Rat[1] 100 nmol/Kg s.c. 8 h 425 nM 11692 nM·h 13 h 8.8 mL/h/kg
Dog[1] 39 nmol/Kg s.c. 14 h 303 nM 28077 nM·h/mL 49 h 1.4 mL/h/kg
Monkey[1] 50 nmol/Kg s.c. 9 h 425 nM 31821 nM·h/mL 44 h 1.6 mL/h/kg
In Vivo

LY3324954 (10 nmol/kg; s.c.; on day 1 and day 4) stimulates transient glucose excursions and progressive insulin secretion in lean C57Bl/6J mice, with enhanced glucose tolerance observed after 7 days of biweekly dosing[1].
LY3324954 (10 nmol/kg; s.c.; single dose) stimulates acute blood glucose elevation via a mechanism dependent on hepatic glucagon receptor signaling in mice[1].
LY3324954 (1-300 nmol/kg; s.c.; every 72 hours; 14 days) induces dose-dependent body weight and fat mass loss in diet-induced obese mice, with improvements in liver and lipid homeostasis observed across all tested doses[1].
LY3324954 (24 nmol/kg; s.c.; every 72 hours; 15 days) induces body weight and fat mass loss in diet-induced obese mice via increased energy expenditure and enhanced lipid oxidation, without reducing total food intake[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57Bl/6J (10-12-week-old male)[1]
Dosage: 10 nmol/kg
Administration: s.c.; on day 1 and day 4
Result: Increased blood glucose at 30 and 60 minutes post-injection on day 1, with glucose returning to baseline by 120 minutes; the area under the curve (AUC) for glucose was significantly higher than vehicle.
On day 4, caused glucose excursion peak at 30 minutes followed by reduced blood glucose at 180 minutes, and the glucose AUC was significantly lower than on day 1.
Stimulated a subtle insulin excursion on day 1, with a robustly increased insulin excursion and AUC on day 4 compared to vehicle.
Induced a trend toward reduced 5-hour fasting blood glucose on day 7, along with enhanced glucose tolerance and a significantly lower glucose AUC during the tolerance test compared to vehicle.
Animal Model: C57Bl/6J (22-24-week-old; diet-induced obesity via high-fat diet for 12 weeks, switched to 39.7% HFD for 4-8 weeks prior to treatment)[1]
Dosage: 1-300 nmol/kg
Administration: s.c.; every 72 hours; 14 days
Result: Induced dose-dependent body weight loss, with significant loss observed at doses ≥10 nmol/kg.
Reduced food intake at 100 and 300 nmol/kg doses, but not at lower doses.
Reduced fat mass and change in fat mass from day 0 to day 14 in a dose-dependent manner, with significant reductions at ≥10 nmol/kg.
Maintained absolute lean mass similar to vehicle across all doses, but caused significant lean mass loss from day 0 to day 14 at 100 and 300 nmol/kg.
Significantly elevated blood glucose at 30 and 100 nmol/kg.
Significantly reduced alanine aminotransferase (ALT) at all doses.
Significantly reduced plasma cholesterol at 30, 100, and 300 nmol/kg.
Significantly reduced liver triglycerides at ≥10 nmol/kg.
Molecular Weight

5139.71

Formula

C238H362N50O76
Sequence

Tyr-Aib-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Lys-Tyr-Leu-Asp-Aib-Lys-Lys-Ala-Lys(EEA-AEEA-γGlu-γGlu-C18 diacid)-Glu-Phe-Val-Glu-Trp-Leu-Leu-Glu-Thr-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2
Sequence Shortening

Y-Aib-QGTFTSDYDKYLD-Aib-KKA-Lys(AEEA-AEEA-γGlu-γGlu-C18 diacid)-EFVEWLLETGPSSGAPPPS-NH2
SMILES

O=C(NC(C)(C)C(N[C@@H](CCC(N)=O)C(NCC(N[C@@H]([C@H](O)C)C(N[C@@H](CC1=CC=CC=C1)C(N[C@@H]([C@H](O)C)C(N[C@@H](CO)C(N[C@@H](CC(O)=O)C(N[C@@H](CC2=CC=C(C=C2)O)C(N[C@@H](CO)C(N[C@@H](CCCCN)C(N[C@@H](CC3=CC=C(C=C3)O)C(N[C@@H](CC(C)C)C(N[C@@H](CC(O)=O)C(NC(C)(C)C(N[C@@H](CCCCN)C(N[C@@H](CCCCN)C(N[C@@H](C)C(N[C@@H](CCCCNC(COCCOCCNC(COCCOCCNC(CC[C@@H](C(O)=O)NC(CC[C@@H](C(O)=O)NC(CCCCCCCCCCCCCCCCC(O)=O)=O)=O)=O)=O)=O)C(N[C@@H](CCC(O)=O)C(N[C@@H](CC4=CC=CC=C4)C(N[C@@H](C(C)C)C(N[C@@H](CCC(O)=O)C(N[C@@H](CC5=CNC6=CC=CC=C56)C(N[C@@H](CC(C)C)C(N[C@@H](CC(C)C)C(N[C@@H](CCC(O)=O)C(N[C@@H]([C@H](O)C)C(NCC(N7[C@@H](CCC7)C(N[C@@H](CO)C(N[C@@H](CO)C(NCC(N[C@@H](C)C(N8[C@@H](CCC8)C(N9[C@@H](CCC9)C(N%10[C@@H](CCC%10)C(N[C@@H](CO)C(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)=O)=O)=O)=O)=O)=O)=O)=O)[C@H](CC%11=CC=C(C=C%11)O)N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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LY3324954 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LY3324954LY 3324954LY-3324954GCGRGlucagon ReceptorGIPRFGF21C57Bl/6J miceglucagon receptordiet-induced obese miceGLP-1Rhuman iPSC-derived hepatocytescAMPHEK293 cellsInhibitorinhibitorinhibit

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