| Size | Price | Stock | Qty |
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| 1mg |
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| 10mg | |||
| Other Sizes |
| Targets |
SUVN-D4010 is a selective 5-HT4 receptor partial agonist. The 5-HT4 receptor is a G protein-coupled receptor that is involved in cognitive function, learning, and memory. Partial agonism at this receptor enhances cholinergic and glutamatergic neurotransmission, which is beneficial for cognitive function in Alzheimer's disease.
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| ln Vitro |
SUVN-D4010 is a potent and selective 5-HT4 receptor partial agonist with an EC50 of 44 nM. It increases levels of soluble amyloid precursor protein α (sAPPα). sAPPα has neuroprotective and cognitive-enhancing properties. The compound's partial agonist activity at the 5-HT4 receptor modulates neurotransmitter release and synaptic plasticity, contributing to its cognitive-enhancing effects.
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| ln Vivo |
In the Object Recognition Test (ORT), usmarapride (SUVN-D4010) (1-3 mg/kg; oral; male Wistar rats, 10–12 weeks old) freebase attenuates long-term memory deficits [1]. The amnesia caused by scopolamine is significantly reversed by usmarapride (1, 3, and 10 mg/kg; oral) free base [1]. At a dose of 3.0 mg/kg, usmarapride free base had statistically significant effects on both the recognition index and the exploration time [1]. In rats, the free base usmarapride (SUVN-D4010) showed good oral exposure, good absorption, and good cerebral exposure [1].
SUVN-D4010 is orally active and brain penetrant. In vivo studies have demonstrated its ability to improve cognitive function in animal models of Alzheimer's disease and other dementias. The compound increases sAPPα levels in the brain, which is associated with cognitive improvement. Specific animal model data and dosing regimens are not extensively detailed. |
| Enzyme Assay |
The binding affinity of SUVN-D4010 to the 5-HT4 receptor can be assessed using radioligand binding assays with membrane preparations from cells expressing recombinant human 5-HT4 receptors. Competition binding experiments are performed with increasing concentrations of SUVN-D4010 against a fixed concentration of a high-affinity radioligand (e.g., [³H]GR113808). Non-specific binding is determined in the presence of an excess of a reference compound (e.g., serotonin or a specific 5-HT4 antagonist).
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| Cell Assay |
The functional activity of SUVN-D4010 at the 5-HT4 receptor is evaluated in vitro using cell lines (e.g., CHO or HEK293 cells) expressing recombinant 5-HT4 receptors. Cells are treated with increasing concentrations of SUVN-D4010, and the stimulation of cAMP accumulation is measured using a cAMP ELISA or homogeneous time-resolved fluorescence (HTRF) assay. The EC50 for cAMP production is determined. Partial agonism is confirmed by comparing the maximal response to that of a full agonist (e.g., serotonin).
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| Animal Protocol |
SUVN-D4010 is administered orally to animal models of cognitive dysfunction. In rodent models (e.g., scopolamine-induced amnesia or aged rats), the compound is given at various doses via oral gavage. Cognitive function is assessed using behavioral tests such as the Morris water maze, novel object recognition, or passive avoidance tests. Brain concentrations of sAPPα and other biomarkers are measured to confirm target engagement.
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| ADME/Pharmacokinetics |
SUVN-D4010 is orally bioactive and brain penetrant (BBB permeable). It has an EC50 of 44 nM at the 5-HT4 receptor. The compound is a partial agonist. Specific pharmacokinetic parameters such as half-life, bioavailability, and plasma protein binding are not extensively detailed in standard reference sources, but the compound is described as orally active and brain penetrant.
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| Toxicity/Toxicokinetics |
The toxicity profile of SUVN-D4010 is not extensively documented in standard reference sources. As a 5-HT4 receptor partial agonist, potential adverse effects may include gastrointestinal effects (e.g., nausea, diarrhea) due to the role of 5-HT4 receptors in gastrointestinal motility. Specific LD50 values and organ-specific toxicity data are not readily available.
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| References |
[1]. Nirogi R, et al. Discovery and Preclinical Characterization of Usmarapride (SUVN-D4010): A Potent, Selective 5-HT4 Receptor Partial Agonist for the Treatment of Cognitive Deficits Associated with Alzheimer's Disease. J Med Chem. 2021;64(15):10641-10665.
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| Additional Infomation |
SUVN-D4010 (CAS# 1428862-32-1) is also known as Usmarapride. It is a potent, selective, brain penetrant, and orally active 5-HT4 receptor partial agonist. The compound has been developed for the treatment of cognitive dysfunction associated with Alzheimer's disease and other dementias. It increases sAPPα levels.
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| Molecular Formula |
383.4960
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|---|---|
| Molecular Weight |
383.4873
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| Exact Mass |
383.232
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| CAS # |
1428862-32-1
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| Related CAS # |
Usmarapride;1428862-33-2
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| PubChem CID |
71508291
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
541.9±60.0 °C at 760 mmHg
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| Flash Point |
281.5±32.9 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.636
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| LogP |
1.78
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
28
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| Complexity |
485
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1C(C2C3C=CC=CC=3N(C(C)C)N=2)=NN=C1C1CCN(CCCOC)CC1
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| InChi Key |
DWTFBJGTRBMHPG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H29N5O2/c1-15(2)26-18-8-5-4-7-17(18)19(24-26)21-23-22-20(28-21)16-9-12-25(13-10-16)11-6-14-27-3/h4-5,7-8,15-16H,6,9-14H2,1-3H3
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| Chemical Name |
2-[1-(3-methoxypropyl)piperidin-4-yl]-5-(1-propan-2-ylindazol-3-yl)-1,3,4-oxadiazole
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| Synonyms |
SUVN D4010; SUVN-D 4010; SUVN-D4010
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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 : ≥ 100 mg/mL (~260.76 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.52 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.52 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6076 mL | 13.0381 mL | 26.0763 mL | |
| 5 mM | 0.5215 mL | 2.6076 mL | 5.2153 mL | |
| 10 mM | 0.2608 mL | 1.3038 mL | 2.6076 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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