| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
GLP1R[1]
The primary pharmacological target of DD202-114 is the glucagon-like peptide-1 receptor (GLP-1R), a G protein-coupled receptor (GPCR). Activation of GLP-1R stimulates the production of cyclic AMP (cAMP), leading to insulin secretion, reduced glucagon secretion, slowed gastric emptying, and enhanced satiety. This mechanism positions GLP-1R agonists as key therapeutics for metabolic diseases. |
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| ln Vitro |
DD202-114 is highly potent in vitro, with an EC₅0 of 0.03 nM in a cAMP accumulation assay using HEK293 cells expressing human GLP-1R. The compound demonstrates full agonistic efficacy in promoting cAMP accumulation and exhibits improved drug-like properties compared to the clinical candidate Danuglipron. No significant off-target activity or cytotoxicity has been reported in standard cell viability assays at pharmacologically relevant concentrations.
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| ln Vivo |
In hGLP-1R knock-in mice, DD202-114 displays a sustained pharmacological effect following oral administration. The compound effectively reduces blood glucose levels in oral glucose tolerance tests and decreases cumulative food intake over time. These in vivo findings are consistent with the anticipated GLP-1R-mediated pharmacodynamic profile, supporting its advancement for preclinical research in T2DM and obesity.
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| Enzyme Assay |
The in vitro cell‑free receptor binding or functional activity of DD202-114 is assessed using a cAMP accumulation assay with a membrane preparation or whole cells. For non‑cellular assessment, membranes from GLP-1R‑overexpressing HEK293 cells are incubated with varying concentrations of DD202-114 (0.01 pM-1 uM) in reaction buffer containing GTPgammaS and forskolin. The amount of cAMP generated is quantified by HTRF (homogeneous time‑resolved fluorescence) or competitive ELISA, and EC₅0 values are calculated by non‑linear regression.
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| Cell Assay |
For in vitro cellular assays, HEK293 cells stably expressing human GLP-1R are seeded in 96‑well plates (20,000 cells/well) and cultured overnight. Cells are treated with DD202‑114 at concentrations ranging from 0.001 nM to 1 uM for 30 min at 37degC. cAMP accumulation is detected using a homogeneous time‑resolved fluorescence (HTRF) kit following the manufacturer's protocol. The EC₅0 is determined by fitting a four‑parameter logistic curve to the normalized data using GraphPad Prism.
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| Animal Protocol |
Standard in vivo animal experiments for GLP‑1R agonists such as DD202‑114 utilize hGLP‑1R knock‑in mice. Mice are fasted overnight (16 h) then administered DD202‑114 (0.1-3 mg/kg, p.o.) or vehicle 30 min before an oral glucose challenge (2 g/kg). Blood glucose is measured via tail vein at multiple time points (0, 15, 30, 60, 120 min). For food intake studies, mice are individually housed and treated once daily with DD202‑114 (p.o.) for 7 days, with cumulative food consumption measured daily.
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| ADME/Pharmacokinetics |
DD202‑114 has a molecular weight of 586.65 g/mol and a formula of C33H3₅FN4O₅. It is soluble in DMSO at approximately 125 mg/mL (~213.07 mM) with ultrasonication. For in vivo use, the compound can be formulated as a suspension in 0.5% methylcellulose or using standard injection formulations such as DMSO:PEG300:Tween 80:saline (10:40:5:45) for oral administration. The powder is stable at -20degC for 3 years and at 4degC for 2 years.
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| Toxicity/Toxicokinetics |
Available safety data for DD202‑114 indicates that it is not a hazardous substance under standard laboratory conditions. The compound is intended for research use only and not for human consumption. No overt toxicity has been reported in animal studies at the active doses described in the literature. Standard laboratory safety precautions, including the use of gloves, lab coats, and eye protection, should be followed during handling.
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| References | |
| Additional Infomation |
DD202‑114 (CAS: 2886728‑09‑0) was first described in 2024 by Zhang et al. in the Journal of Medicinal Chemistry (J Med Chem. 2024;67(17):14820‑14839). It was identified using an AIDD/CADD method and selected as a preclinical candidate (PCC). The compound is also referred to as Conveglipron, HDM1002, and compound 14. DD202‑114 is strictly for research use only and has not yet entered human clinical trials or received regulatory approval for therapeutic use.
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| Molecular Formula |
C33H35FN4O5
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|---|---|
| Molecular Weight |
586.65
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| Exact Mass |
586.259
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| CAS # |
2886728-09-0
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| PubChem CID |
166540968
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
1
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
43
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| Complexity |
935
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1CO[C@@H]1CN2C3=C(C=CC(=C3)C(=O)O)N=C2CN4CCC(CC4)C5=NC(=CC=C5)OCC6=C(C=C(C=C6)C7COC7)F
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| InChi Key |
SFKAXUUDIGSMBK-SANMLTNESA-N
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| InChi Code |
InChI=1S/C33H35FN4O5/c34-27-14-22(25-18-41-19-25)4-5-24(27)20-43-32-3-1-2-28(36-32)21-8-11-37(12-9-21)17-31-35-29-7-6-23(33(39)40)15-30(29)38(31)16-26-10-13-42-26/h1-7,14-15,21,25-26H,8-13,16-20H2,(H,39,40)/t26-/m0/s1
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| Chemical Name |
2-[[4-[6-[[2-fluoro-4-(oxetan-3-yl)phenyl]methoxy]-2-pyridinyl]piperidin-1-yl]methyl]-3-[[(2S)-oxetan-2-yl]methyl]benzimidazole-5-carboxylic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~213.1 mM; with ultrasonication)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7046 mL | 8.5230 mL | 17.0459 mL | |
| 5 mM | 0.3409 mL | 1.7046 mL | 3.4092 mL | |
| 10 mM | 0.1705 mL | 0.8523 mL | 1.7046 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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