| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
hu mGluR7 7 nM (EC50)
mGluR7 (metabotropic glutamate receptor 7). |
|---|---|
| ln Vitro |
CVN636 is a potent allosteric agonist of mGluR7 with EC50 values of 7 nM for the human receptor and 2 nM for the mouse receptor. This high potency, combined with its selectivity and oral bioavailability, makes it a valuable tool for in vivo studies of mGluR7 function.
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| ln Vivo |
In msP rats, CVN636 (0.3–3 mg/kg; po) decreases ethanol self-administration[1].
As a CNS-penetrant and orally active compound, CVN636 is suitable for in vivo studies to explore the therapeutic potential of mGluR7 activation. Its effects on synaptic transmission and neuronal excitability can be evaluated in various behavioral and disease models to understand the role of mGluR7 in conditions such as anxiety, depression, and pain. |
| Enzyme Assay |
In vitro receptor binding and functional assays are used to characterize CVN636's interaction with mGluR7. These assays involve the use of cells expressing human or mouse mGluR7 receptors. The compound's binding affinity and its ability to allosterically activate the receptor are assessed using radioligand binding and functional readouts such as calcium mobilization or cAMP modulation.
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| Cell Assay |
Cells expressing human or mouse mGluR7 are treated with CVN636, and receptor activation is measured by assessing downstream signaling pathways. The EC50 for the agonistic effect is determined from the concentration-response curve. The selectivity of CVN636 for mGluR7 over other mGluR subtypes is also evaluated in these assays.
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| Animal Protocol |
Animal/Disease Models: msP rat[1]
Doses: 0.3, 1, and 3 mg/kg Route of Administration: oral administration Experimental Results: decreased alcohol self-administration in a dose-dependent. In vivo studies are conducted in rodent models to evaluate the behavioral and pharmacological effects of mGluR7 activation. CVN636 is typically administered orally or via intraperitoneal injection due to its oral bioavailability. Its effects on anxiety-like behavior, depressive-like behavior, pain sensitivity, and cognitive function are assessed to determine its therapeutic potential. |
| ADME/Pharmacokinetics |
No detailed pharmacokinetic data are publicly available for CVN636. However, its classification as an orally bioavailable and CNS-penetrant compound suggests favorable ADME properties. Standard PK studies would be conducted to determine its half-life, bioavailability, and brain exposure levels.
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| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available. As a potent mGluR7 agonist, its safety profile would need to be evaluated in standard preclinical toxicology studies. Potential side effects could be related to its mechanism of action, affecting neurotransmitter release and synaptic transmission in the CNS.
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| References | |
| Additional Infomation |
CVN636 is a recently developed, highly potent, and selective mGluR7 allosteric agonist with promising drug-like properties, including oral bioavailability and CNS penetration. Its discovery represents a significant advance in the development of mGluR7-targeted therapeutics. It is currently a research tool and is not approved for clinical use. Its in vivo efficacy in disease models is an active area of investigation.
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| Molecular Formula |
C19H20FNO4S
|
|---|---|
| Molecular Weight |
377.429807662964
|
| Exact Mass |
377.109
|
| CAS # |
2226732-62-1
|
| PubChem CID |
134521670
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| Appearance |
White to off-white solid powder
|
| LogP |
3.1
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
26
|
| Complexity |
597
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
C[C@@H](C1=CC=C(C=C1)F)C(=O)N[C@H]2COC3=CC=CC=C3[C@@H]2S(=O)(=O)C
|
| InChi Key |
DKLUNKKXISSMIY-IWEFOYFVSA-N
|
| InChi Code |
InChI=1S/C19H20FNO4S/c1-12(13-7-9-14(20)10-8-13)19(22)21-16-11-25-17-6-4-3-5-15(17)18(16)26(2,23)24/h3-10,12,16,18H,11H2,1-2H3,(H,21,22)/t12-,16-,18-/m0/s1
|
| Chemical Name |
(2S)-2-(4-fluorophenyl)-N-[(3S,4S)-4-methylsulfonyl-3,4-dihydro-2H-chromen-3-yl]propanamide
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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 (~265.0 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.62 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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 (6.62 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6495 mL | 13.2475 mL | 26.4950 mL | |
| 5 mM | 0.5299 mL | 2.6495 mL | 5.2990 mL | |
| 10 mM | 0.2649 mL | 1.3247 mL | 2.6495 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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