2. GPCR/G Protein Neuronal Signaling Metabolic Enzyme/Protease
  3. GPR119 Dipeptidyl Peptidase
  4. HBK001

HBK001 is an orally active and selective dual GPR119 agonist and DPP-IV inhibitor. HBK001 triggers cAMP production, PKA activation, CREB phosphorylation, glucose-stimulated insulin secretion, plasma incretin elevation, β-cell proliferation, and β-cell function gene up-regulation. HBK001 reduces blood glucose, ameliorates hyperglycemia, improves glucose tolerance, and enhances islet morphology. HBK001 can be used for the research of type 2 diabetes mellitus.

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HBK001

HBK001 Chemical Structure

CAS No. : 1942922-78-2

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HBK001 Related Antibodies

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DPP-1 DPP-2 DPP-4 DPP-8 DPP-9

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Description

HBK001 is an orally active and selective dual GPR119 agonist and DPP-IV inhibitor. HBK001 triggers cAMP production, PKA activation, CREB phosphorylation, glucose-stimulated insulin secretion, plasma incretin elevation, β-cell proliferation, and β-cell function gene up-regulation. HBK001 reduces blood glucose, ameliorates hyperglycemia, improves glucose tolerance, and enhances islet morphology. HBK001 can be used for the research of type 2 diabetes mellitus[1][2].

IC50 & Target[1]

DPP-4

40 nM (IC50)

In Vitro

HBK001 potently inhibits DPP-IV with an IC50 of 0.04 μM[1].
HBK001 (10 μM) exhibits no inhibitory activity against DPP-8/9 at 10 μM, demonstrating high selectivity for DPP-IV[1].
HBK001 acts as a GPR119 agonist in HEK293 cells with an EC50 of 1.40 μM and 58% relative activity at 1 μM[1].
HBK001 (30 min) shows low stability in mouse and rat hepatocytes, but favorable stability in human hepatocytes with 101.2% substrate remaining after 30 min incubation[1].
HBK001 (serial dilutions; 48 h) displays low cytotoxicity against Vero cells with an IC50 of 46.6 μg/mL[1].
HBK001 (3.28 nM-10 μM; 24 h) activates GPR119 in transfected HEK293 cells with an EC50 of 0.03 μM[2].
HBK001 (10 μM; 24 h) does not activate GPR40, GLP1R, or GIPR at 10 μM in transfected HEK293 cells, demonstrating selective activation of GPR119 over related GPCRs[2].
HBK001 (1-10 μM) enhances glucose-stimulated insulin secretion in ICR mouse primary islets in vitro in a concentration-dependent manner at 16.7 mM glucose[2].
HBK001 (10 μM) enhances glucose-stimulated insulin secretion in human primary islets from healthy donors[2].
HBK001 (0.1-10 μM) increases intracellular cAMP production in NIT-1 mouse pancreatic β-cells in vitro in a concentration-dependent manner[2].
HBK001 (10 μM) activates transactivation of mouse Ins1 and Ins2 gene promoters in GPR119-transfected HEK293 cells at 10 μM[2].
HBK001 (10 μM; 24 h) upregulates expression of β-cell function-related genes (Nkx6.1, Nkx2.2, Ins1, Ins2) in ICR mouse primary islets[2].
HBK001 (10 μM) enhances glucose-stimulated insulin secretion in KKAy mouse primary islets via an adenylate cyclase-dependent pathway[2].

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

HBK001 Related Antibodies

Real Time qPCR[2]

Cell Line: ICR mouse primary islets
Concentration: 10 μM
Incubation Time: 24 h
Result: Upregulated expression of β-cell function-related genes (Nkx6.1, Nkx2.2, Ins1, Ins2)
Parmacokinetics
Species Dose Route T1/2 Cmax AUC0-t AUC0-∞ MRT0-∞ Tmax F
Mice[1] 20 mg/kg p.o. 1.06 h 213 ng/mL 308 ng·h/mL 318 ng·h/mL 1.22 h 0.42 h 12.2 %
Mice[1] 2 mg/kg i.v. 1.64 h 850 ng/mL 257 ng·h/mL 261 ng·h/mL 0.76 h / /
Rat[1] 30 mg/kg p.o. 1.11 h 192 ng/mL 468 ng·h/mL 502 ng·h/mL 2.11 h 1.17 h 31.8 %
In Vivo

HBK001 (30 mg/kg; p.o.; single dose) exhibits in vivo glucose-lowering activity in euglycemic ICR mice at a single oral dose of 30 mg/kg[1].
HBK001 (5-30 mg/kg; p.o.; single dose) selectively inhibits serum DPP4 activity, increases glucose-stimulated incretin release, and reduces glucose excursion in euglycemic ICR mice, with a glucose-lowering plateau at 30 mg/kg[2].
HBK001 (30 mg/kg; p.o.; daily; 6 weeks) ameliorates hyperglycemia, improves glucose tolerance, enhances insulin secretion, normalizes islet morphology, and up-regulates β-cell function-related genes in spontaneous diabetic KKAy mice via GPR119-dependent signaling, despite only inhibiting ~50% of serum DPP4 activity[2].
HBK001 (30 mg/kg; p.o.; daily; 5 weeks) ameliorates hyperglycemia and improves glucose tolerance in spontaneous diabetic db/db mice[2].

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

Animal Model: ICR mice (male, 26-27 g)[1]
Dosage: 30 mg/kg
Administration: p.o.; single dose
Result: Reduced blood glucose levels after oral glucose loading.
Showed higher area under the oral glucose tolerance test curve (AUCOGTT) than HBK001 hydrochloride (22) group at equivalent molar dose.
Animal Model: ICR mice (male)[2]
Dosage: 5 mg/kg; 10 mg/kg; 20 mg/kg; 30 mg/kg
Administration: p.o.; single dose
Result: Achieved approximately 50% serum DPP4 inhibition compared to baseline for about 4 hours at 30 mg/kg.
Increased glucose-induced total GLP-1 levels by 41.0% and glucose-induced GIP levels by 40.2% compared to vehicle at 30 mg/kg.
Significantly reduced blood glucose levels 30 minutes after oral glucose loading at doses of 5, 10, 20, and 30 mg/kg, with the area under the curve (AUC) decreased by 17.1%, 21.8%, 24.2%, and 22.8%, respectively, compared to vehicle.
Animal Model: KKAy mice (female, spontaneous diabetic, fasting blood glucose >180 mg/dl)[2]
Dosage: 30 mg/kg
Administration: p.o.; daily; 6 weeks
Result: Significantly decreased fasting blood glucose levels over 6 weeks.
Reduced OGTT AUC by 26.5% compared to vehicle.
Inhibited ~50% of serum DPP4 activity.
Increased first-phase insulin secretion by 4.7-fold compared to vehicle.
Increased glucose infusion rate (GIR) during hyperglycemic clamp.
Increased β-cell area percentage by 17.9% compared to vehicle.
Increased pancreatic CREB phosphorylation.
Up-regulated β-cell function-related genes including NeuroD, Nkx6.1, Nkx2.2, MafA, Ins1, and Ins2 compared to vehicle.
Animal Model: db/db (BKS.Cg-m+/+ Leprdb/J) mice (female, spontaneous diabetic, fasting blood glucose >180 mg/dl)[2]
Dosage: 30 mg/kg
Administration: p.o.; daily; 5 weeks
Result: Significantly decreased fasting blood glucose levels over 5 weeks.
Reduced OGTT AUC by 13.0% compared to vehicle, with effects comparable to linagliptin.
Molecular Weight

586.69

Formula

C30H38N10O3
CAS No.
SMILES

CC#CCN1C2=C(N(C(N(C2=O)CCCN3CCN(C4=NC(C5=CC=CC=C5)=NO4)CC3)=O)C)N=C1N6C[C@@H](CCC6)N
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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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HBK001 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:

HBK0011942922-78-2HBK 001HBK-001GPR119Dipeptidyl PeptidaseG Protein-Coupled Receptor 119DPPhERGGPR40GLP1RDPP8DPP-IVtype 2 diabetes mellitusGIPRhuman DPP-IVhuman GPR119Inhibitorinhibitorinhibit

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