DA-302168S
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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 98.01%
- CAS No.: 2969158-02-7
- Formule: C33H24ClF2N3O5
- Masse moléculaire:616.01
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
GLP-1 1.32 nM (EC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
1.32 nM
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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.
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40257122 |
| HEK293 | EC50 |
0.0293 nM
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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.
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40257122 |
| HEK293 | EC50 |
0.0124 nM
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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.
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40257122 |
| HEK293 | EC50 |
117.7 nM
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Weak partial agonist activity for β-arrestin recruitment measured in vitro.
Weak partial agonist activity for β-arrestin recruitment measured in vitro.
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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 T1/2 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
In Vivo
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.
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Animal Model:hGLP-1R transgenic mice[1]
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Dosage:0.025, 0.05, 0.1, 0.3, 1 mg/kg
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Administration:p.o.; single dose
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Result:Reduced blood glucose levels in a dose-dependent manner.
Exhibited hypoglycemic effect.
Promoted insulin secretion in hGLP-1R transgenic mice.
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Animal Model:hGLP-1R transgenic mice[1]
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Dosage:1, 3, 10 mg/kg
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Administration:p.o.; single dose
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Result:Reduced food intake in a dose-dependent manner.
Achieved a significantly greater reduction in food intake at 3 mg/kg.
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Animal Model:Cynomolgus monkeys[1]
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Dosage:3, 10 mg/kg
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Administration:p.o.; single dose
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Result:Reduced blood glucose levels in a dose-dependent manner.
Significantly promoted insulin secretion at 3 mg/kg.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2969158-02-7
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Appearance Solid
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Masse moléculaire 616.01
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Formule C33H24ClF2N3O5
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Color White to off-white
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (275 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
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.
| 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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