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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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CAS. Nr.: 1942922-78-2
Formel: C₃₀H₃₈N₁₀O₃
Molecular Weight:586.69

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

HBK001 Chemical Structure

CAS. Nr.: 1942922-78-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

DPP-4

40 nM (IC₅₀)

Alle Dipeptidyl Peptidase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Vero	IC₅₀	46.6 μg/mL Compound: 21h; HBK001	Cytotoxicity against African green monkey Vero cells incubated for 48 hrs by MTT assay Cytotoxicity against African green monkey Vero cells incubated for 48 hrs by MTT assay	[PMID: 31926470]

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.

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	T_1/2	C_max	AUC_0-t	AUC_0-∞	MRT_0-∞	T_max	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.

Chemical Information

CAS. Nr. 1942922-78-2
Molecular Weight 586.69
Formel C₃₀H₃₈N₁₀O₃
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Li G, et al. The optimization of xanthine derivatives leading to HBK001 hydrochloride as a potent dual ligand targeting DPP-IV and GPR119. Eur J Med Chem. 2020;188:112017. [Content Brief]

[2]. Huan Y, et al. The dual DPP4 inhibitor and GPR119 agonist HBK001 regulates glycemic control and beta cell function ex and in vivo. Sci Rep. 2017;7(1):4351. Published 2017 Jun 28. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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