Cat. No.: HY-172811

DA-302168S

Name: DA-302168S
Brand: MedChemExpress
SKU: HY-172811
Price: 555.00 USD
Availability: InStock
Rating: 5 (1 reviews)

고객리뷰

Based on 1 Customer Validation

DA-302168S is an orally active and selective agonist targeting the GLP-1R, with EC₅₀ value of 1.32 nM. DA-302168S reduces blood glucose levels and suppresses appetite, demonstrates minimal safety risks including low hERG channel inhibition and no significant off-target toxicity, and mitigates drug-drug interaction risk. DA-302168S can be used for the research of type 2 diabetes and obesity.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity : 98.01%
CAS No.: 2969158-02-7
화학식: C₃₃H₂₄ClF₂N₃O₅
분자량:616.01

보관:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

DA-302168S Chemical Structure

CAS No.: 2969158-02-7

사이즈

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수량

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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
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
- Clinical Trial
Chemical Information
용액&용해도
- In Vitro
- In Vivo
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[1]

GLP-1

1.32 nM (EC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC50	1.32 nM	GLP-1R agonist activity in HEK293 cells expressing human GLP-1R measured by luciferase assay. GLP-1R agonist activity in HEK293 cells expressing human GLP-1R measured by luciferase assay.	40257122
HEK293	EC50	0.0293 nM	GLP-1R agonist activity in HEK293 cells expressing human GLP-1R measured by cAMP accumulation assay. GLP-1R agonist activity in HEK293 cells expressing human GLP-1R measured by cAMP accumulation assay.	40257122
HEK293	EC50	0.0124 nM	GLP-1R agonist activity in HEK293 cells expressing Cynomolgus monkey GLP-1R measured by cAMP accumulation assay. GLP-1R agonist activity in HEK293 cells expressing Cynomolgus monkey GLP-1R measured by cAMP accumulation assay.	40257122
HEK293	EC50	117.7 nM	Weak partial agonist activity for β-arrestin recruitment measured in vitro. Weak partial agonist activity for β-arrestin recruitment measured in vitro.	40257122

In Vitro

DA-302168S (compound 29) potently activates human GLP-1R in HEK293 cells with an EC₅₀ of 1.32 nM^[1].
DA-302168S shows superior metabolic stability in human liver microsomes with a T_1/2 of 131 min, supporting potential for reduced dosing frequency^[1].
DA-302168S has minimal CYP isoform inhibition activity in human liver microsomes, with an IC₅₀ of 28.31 μM for CYP2C8 and IC₅₀ > 30 μM for all other tested isoforms^[1].
DA-302168S potently activates human and Cynomolgus monkey GLP-1R in HEK293 cells with EC₅₀ values of 0.0293 nM and 0.0124 nM, respectively, but has negligible activity on rodent and dog GLP-1R^[1].
DA-302168S exhibits high selectivity for human GLP-1R over other class B GPCRs, with only minor activity on human GIPR at the highest tested concentration and no activity on GLP-2R or GCGR^[1].

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

Parmacokinetics

Species	Dose	Route	AUC_last	T_1/2	C_max	T_max	F
Rat^[1]	1 mg/kg	i.v.	1481 ng/mL·h	/	/	/	/
Rat^[1]	10 mg/kg	p.o.	2958 ng/mL·h	/	347 ng/mL	3.50 h	20.1 %
Cynomolgus Monkey^[1]	0.5 mg/kg	i.v.	1766 ng/mL·h	12.7 h	/	/	/
Cynomolgus Monkey^[1]	5 mg/kg	p.o.	2441 ng/mL·h	10.4 h	327 ng/mL	2.5 h	13.9 %

In Vivo

DA-302168S (0.025-1 mg/kg; p.o.; single dose) exhibits dose-dependent hypoglycemic activity in hGLP-1R transgenic mice^[1].
DA-302168S (3-10 mg/kg; p.o.; single dose) exhibits dose-dependent hypoglycemic activity and stimulates insulin secretion in Cynomolgus monkeys^[1].
DA-302168S (1-10 mg/kg; p.o.; single dose) dose-dependently reduces food intake in hGLP-1R transgenic mice^[1].

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

Animal Model:

hGLP-1R transgenic mice^[1]
Dosage:

0.025, 0.05, 0.1, 0.3, 1 mg/kg
Administration:

p.o.; single dose
Result:

Reduced blood glucose levels in a dose-dependent manner.
Exhibited hypoglycemic effect.
Promoted insulin secretion in hGLP-1R transgenic mice.

Animal Model:

hGLP-1R transgenic mice^[1]
Dosage:

1, 3, 10 mg/kg
Administration:

p.o.; single dose
Result:

Reduced food intake in a dose-dependent manner.
Achieved a significantly greater reduction in food intake at 3 mg/kg.

Animal Model:

Cynomolgus monkeys^[1]
Dosage:

3, 10 mg/kg
Administration:

p.o.; single dose
Result:

Reduced blood glucose levels in a dose-dependent manner.
Significantly promoted insulin secretion at 3 mg/kg.

Clinical Trial

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

Chemical Information

CAS No. 2969158-02-7
Appearance Solid
분자량 616.01
화학식 C₃₃H₂₄ClF₂N₃O₅
Color White to off-white
SMILES

O=C(C1=CC2=C(N=C(N2C[C@@H]3CCO3)CC4=CC=C(C=C4F)C5=NC(OCC6=CC=C(C7=C6OC=C7)Cl)=C(C=C5)F)C=C1)O
선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

용액&용해도

In Vitro:

DMSO : 100 mg/mL (162.34 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

1.6234 mL

8.1168 mL

16.2335 mL

5 mM

0.3247 mL

1.6234 mL

3.2467 mL

10 mM

0.1623 mL

0.8117 mL

1.6234 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.06 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 (275 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Dong G, et al. Discovery and Evaluation of DA-302168S as an Efficacious Oral Small-Molecule Glucagon-Like Peptide-1 Receptor Agonist. Journal of medicinal chemistry. 2025 May 08;68(9):9555-9583. [Content Brief]

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.6234 mL	8.1168 mL	16.2335 mL	40.5838 mL
	5 mM	0.3247 mL	1.6234 mL	3.2467 mL	8.1168 mL
	10 mM	0.1623 mL	0.8117 mL	1.6234 mL	4.0584 mL
	15 mM	0.1082 mL	0.5411 mL	1.0822 mL	2.7056 mL
	20 mM	0.0812 mL	0.4058 mL	0.8117 mL	2.0292 mL
	25 mM	0.0649 mL	0.3247 mL	0.6493 mL	1.6234 mL
	30 mM	0.0541 mL	0.2706 mL	0.5411 mL	1.3528 mL
	40 mM	0.0406 mL	0.2029 mL	0.4058 mL	1.0146 mL
	50 mM	0.0325 mL	0.1623 mL	0.3247 mL	0.8117 mL
	60 mM	0.0271 mL	0.1353 mL	0.2706 mL	0.6764 mL
	80 mM	0.0203 mL	0.1015 mL	0.2029 mL	0.5073 mL
	100 mM	0.0162 mL	0.0812 mL	0.1623 mL	0.4058 mL

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DA-302168S