1. GPCR/G Protein
  2. GLP Receptor
  3. GZR18

GZR18 is an analog of glucagon-like peptide-1 (GLP-1), which exhibits agonistic activity for GLP-1 receptor, with an EC50 of 0.677 nM. GZR18 ameliorates type 2 diabetes.

For research use only. We do not sell to patients.

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GZR18 Chemical Structure

GZR18 Chemical Structure

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Description

GZR18 is an analog of glucagon-like peptide-1 (GLP-1), which exhibits agonistic activity for GLP-1 receptor, with an EC50 of 0.677 nM. GZR18 ameliorates type 2 diabetes[1].

IC50 & Target

EC50: 0.677 nM (GLP-1 Receptor)

In Vitro

GZR18 (30-90 nM, 0.5-1 h) stimulates glucose-dependent insulin secretion in mouse pancreatic islet β-cells in a dose-dependent manner[1].

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

In Vivo

GZR18 (0-100 nmol/kg, s.c., single dose or 11 dosages) decreases blood glucose levels and body weight dose-depedently, and exhibits glycemic control property in db/db mice model[1].
GZR18 (60 μg/kg, iv or sc, single dose) reveals a pharmacokinetic profil in cynomolgus monkey model[1].

Pharmacokinetic Analysis of GZR18 in cynomolgus monkey[1]

route Dose (μg/kg) T1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (ng·h/mL)) AUC0-inf (ng·h/mL) MRT (h) Vd/F (kg/mL) CL/F (h/g·mL) F (%)
s.c. 60 61.3 14 527 51800 55700 75.2 96.6 1.1 73.3
i.v. 60 61.6 0.167 1640 70700 74800 59.2 59.4 0.803 -

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

Animal Model: Type 2 diabete in db/db mice[1]
Dosage: 0-100 nmol/kg
Administration: s.c., single dose or once every 3 days for 33 days
Result: Lowered blood glucose levels, suppressed food and water intake and improved glucose homeostasis.
Molecular Weight

4141.63

Formula

C189H295N45O59

Sequence

His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys(AEEA-AEEA-gammaGlu-C22 diacid)-Glu-Phe-Ile-Ala-Trp-Leu-Val-Arg-Gly-Arg-Gly

Sequence Shortening

HGEGTFTSDVSSYLEGQAA-K(AEEA-AEEA-gammaGlu-C22 diacid)-EFIAWLVRGRG

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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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.

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Product Name:
GZR18
Cat. No.:
HY-P10269
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