Cat. No.: HY-12528

DBPR108

Name: DBPR108
Brand: MedChemExpress
SKU: HY-12528
Price: 128.00 USD
Availability: InStock
Rating: 5 (1 reviews)

1 Cited Publications

고객리뷰

Based on 1 publication(s) in Google Scholar

DBPR108 is an orally active, selective dipeptidyl peptidase-4 (DPP-4) inhibitor with an IC₅₀ of 15 nM. DBPR108 reduces glycated hemoglobin, fasting plasma glucose and postprandial plasma glucose levels, increases serum active GLP-1 and insulin levels, and improves glucose tolerance. DBPR108 can be used in research related to type 2 diabetes.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity : 99.93%
CAS No.: 1186426-66-3
화학식: C₁₆H₂₅FN₄O₂
분자량:324.39

보관:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

DBPR108 Chemical Structure

CAS No.: 1186426-66-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
용액&용해도
- In Vitro
- In Vivo
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[1]^[2]

DPP-4

15 nM (IC₅₀)

GLP-1

All Dipeptidyl Peptidase Isoforms :

In Vitro

DBPR108 potently and selectively inhibits DPP-4 with an IC₅₀ of 15 nM, and exhibits no significant inhibitory activity against DPP-8, DPP-9 or fibroblast activation protein (IC₅₀ >50 μM)^[1].
The IC₅₀ values of DBPR108 against DPP-4 in human, rodent, canine and monkey plasma range from 4.1 to 20.4 nM^[2].

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

Parmacokinetics

Species	Dose	Route	C_max	T_max	AUC_0-∞	T_1/2
Rat^[2]	5 mg/kg	p.o.	108 ng/mL	1.8 h	410 ng·h/mL	3.8 h

In Vivo

DBPR108 (0.1-30 mg/kg; p.o.; single dose) dose-dependently inhibits plasma DPP-4 activity (ED₅₀ = 0.9 mg/kg), increases active GLP-1 levels, and enhances insulin secretion in glucose-challenged SD rats^[2].
DBPR108 (0.01-10 mg/kg; p.o.; single dose) dose-dependently inhibits plasma DPP-4 activity (ED₅₀ = 1.9 mg/kg) in diabetic db/db mice^[2].
DBPR108 (0.01-3 mg/kg; p.o.; single dose) dose-dependently inhibits plasma DPP-4 activity (ED₅₀ = 0.1 mg/kg) in healthy beagle dogs^[2].
DBPR108 (0.1-10 mg/kg; p.o.; single dose) dose-dependently improves oral glucose tolerance (ED₅₀ = 0.144 mg/kg) in healthy C57BL/6JNarl mice^[2].
DBPR108 (0.01-10 mg/kg; p.o.; single dose) dose-dependently improves oral glucose tolerance (ED₅₀ = 0.033 mg/kg) in DIO mice, with additive efficacy when combined with Metformin (HY-B0627)^[2].

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

Animal Model:

Sprague Dawley (male, 250-300 g, glucose ingestion challenged)^[2]
Dosage:

0.1 mg/kg; 0.5 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration:

p.o.; single dose
Result:

Dose-dependently inhibited plasma DPP-4 activity, with an ED₅₀ of 0.9 mg/kg.
Significantly increased plasma active GLP-1 levels at 5 minutes post-glucose challenge, with a greater ΔAUC than vehicle control at 10 mg/kg dose.
Significantly increased plasma insulin levels at 10 minutes post-glucose challenge, with a prolonged elevation until 15 minutes and a greater ΔAUC than vehicle control at 10 mg/kg dose.

Animal Model:

BKS.Cg-m+/+Lepr^db/J (db/db) (adult)^[2]
Dosage:

0.01 mg/kg; 0.1 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration:

p.o.; single dose
Result:

Dose-dependently inhibited plasma DPP-4 activity.
Achieved an ED₅₀ of 1.9 mg/kg for DPP-4 inhibition.

Animal Model:

Beagle (male, 9-10 months old)^[2]
Dosage:

0.01 mg/kg; 0.05 mg/kg; 0.1 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg
Administration:

p.o.; single dose
Result:

Dose-dependently inhibited plasma DPP-4 activity at all tested doses.
Achieved an ED₅₀ of 0.1 mg/kg for DPP-4 inhibition.

Animal Model:

C57BL/6JNarl (both sexes, adult)^[2]
Dosage:

0.1 mg/kg; 0.5 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration:

p.o.; single dose
Result:

Dose-dependently suppressed glucose-induced blood glucose elevation.
Achieved an ED₅₀ of 0.144 mg/kg for improved glucose tolerance.

Animal Model:

C57BL/6JNarl (both sexes, fed high-fat diet for 6 months)^[2]
Dosage:

0.01 mg/kg; 0.1 mg/kg; 0.5 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
0.1 mg/kg (in combination with 50, 100 mg/kg Metformin)
Administration:

p.o.; single dose
Result:

Dose-dependently suppressed glucose-induced blood glucose elevation.
Achieved an ED50 of 0.033 mg/kg for improved glucose tolerance.
Produced additive improvements in glucose tolerance when combined with 0.1 mg/kg DBPR108 plus 50 or 100 mg/kg metformin.
Completely suppressed glucose-induced blood glucose elevation when combined with 0.1 mg/kg DBPR108 plus 100 mg/kg metformin.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1186426-66-3
Appearance Solid
분자량 324.39
화학식 C₁₆H₂₅FN₄O₂
Color White to off-white
SMILES

N#C[C@H]1N(C(CNC(C)(C)CC(N2CCCC2)=O)=O)C[C@@H](F)C1
선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Journal Impact Factor

bioRxiv

2026 May 13.

용액&용해도

In Vitro:

DMSO : ≥ 25 mg/mL (77.07 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.0827 mL

15.4135 mL

30.8271 mL

5 mM

0.6165 mL

3.0827 mL

6.1654 mL

10 mM

0.3083 mL

1.5414 mL

3.0827 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (7.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (7.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (7.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (287 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Wang W, et al. Prusogliptin (DBPR108) monotherapy in treatment-naïve patients with type 2 diabetes: A randomized, double-blind, active and placebo-controlled, phase 3 study. Diabetes, obesity & metabolism. 2024 Apr;26(4):1321-1332.

[2]. Yeh KC, et al. DBPR108, a novel dipeptidyl peptidase-4 inhibitor with antihyperglycemic activity. Life sciences. 2021 Aug 01;278:119574.

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.0827 mL	15.4135 mL	30.8271 mL	77.0677 mL
	5 mM	0.6165 mL	3.0827 mL	6.1654 mL	15.4135 mL
	10 mM	0.3083 mL	1.5414 mL	3.0827 mL	7.7068 mL
	15 mM	0.2055 mL	1.0276 mL	2.0551 mL	5.1378 mL
	20 mM	0.1541 mL	0.7707 mL	1.5414 mL	3.8534 mL
	25 mM	0.1233 mL	0.6165 mL	1.2331 mL	3.0827 mL
	30 mM	0.1028 mL	0.5138 mL	1.0276 mL	2.5689 mL
	40 mM	0.0771 mL	0.3853 mL	0.7707 mL	1.9267 mL
	50 mM	0.0617 mL	0.3083 mL	0.6165 mL	1.5414 mL
	60 mM	0.0514 mL	0.2569 mL	0.5138 mL	1.2845 mL

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DBPR108

Publications Citing Use of MedChemExpress (MCE) DBPR108

All Dipeptidyl Peptidase Isoforms