VU 10010CAS# 633283-39-3 |
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Quality Control & MSDS
3D structure
Package In Stock
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| Cas No. | 633283-39-3 | SDF | Download SDF |
| PubChem ID | 714286 | Appearance | Powder |
| Formula | C17H16ClN3OS | M.Wt | 345.85 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble in DMSO > 10 mM | ||
| Chemical Name | 3-amino-N-[(4-chlorophenyl)methyl]-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamide | ||
| SMILES | CC1=CC(=NC2=C1C(=C(S2)C(=O)NCC3=CC=C(C=C3)Cl)N)C | ||
| Standard InChIKey | FPRULFHDSFKYBV-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C17H16ClN3OS/c1-9-7-10(2)21-17-13(9)14(19)15(23-17)16(22)20-8-11-3-5-12(18)6-4-11/h3-7H,8,19H2,1-2H3,(H,20,22) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Selective allosteric potentiator of M4 acetylcholine receptors (EC50 values are 33 and 0.7 nM for ACh in the absence and presence of VU10010 respectively). Binds to an allosteric site on the receptor increasing affinity for ACh and coupling to G-proteins. |
VU 10010 Dilution Calculator
VU 10010 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.8914 mL | 14.4571 mL | 28.9143 mL | 57.8285 mL | 72.2857 mL |
| 5 mM | 0.5783 mL | 2.8914 mL | 5.7829 mL | 11.5657 mL | 14.4571 mL |
| 10 mM | 0.2891 mL | 1.4457 mL | 2.8914 mL | 5.7829 mL | 7.2286 mL |
| 50 mM | 0.0578 mL | 0.2891 mL | 0.5783 mL | 1.1566 mL | 1.4457 mL |
| 100 mM | 0.0289 mL | 0.1446 mL | 0.2891 mL | 0.5783 mL | 0.7229 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Presynaptic M3 muscarinic cholinoceptors mediate inhibition of excitatory synaptic transmission in area CA1 of rat hippocampus.[Pubmed:26505913]
Brain Res. 2015 Dec 10;1629:260-9.
Acetylcholine can modulate hippocampal network function through activation of both nicotinic and muscarinic acetylcholine receptors (mAChRs). All five mAChR subtypes have been identified in the hippocampus. Besides by their involvement in excitability of hippocampal cells, synaptic plasticity and memory, a large body of research has demonstrated the involvement of presynaptic mAChRs in the inhibition of glutamatergic transmission in the hippocampus. Over the years, however, pharmacological and molecular genetic studies have yielded quite contradictory results regarding the mAChR subtype(s) involved. In this study, multi-electrode array technology was used for the pharmacological elucidation of the subtype of mAChR mediating the depression of excitatory synaptic transmission at the SC-CA1 synapse. Using selective antagonists (VU0255035, MT7, tripinamide, MT3) and allosteric potentiators (VU 10010, VU 0238429) the involvement of M1, M2, M4, and M5 subtypes was ruled out thereby implying a major modulatory role for M3 receptors in the inhibition of excitatory synaptic transmission in area CA1 of rat hippocampus.
Functional activation of G-proteins coupled with muscarinic acetylcholine receptors in rat brain membranes.[Pubmed:24849282]
J Pharmacol Sci. 2014;125(2):157-68. Epub 2014 May 20.
The functional activation of Gi/o proteins coupled to muscarinic acetylcholine receptors (mAChRs) was investigated with the conventional guanosine-5'-O-(3-[(35)S]thio) triphosphate ([(35)S]GTPgammaS) binding assay in rat brain membranes. The most efficacious stimulation elicited by acetylcholine or carbachol (CCh) was obtained in striatal membranes. The pharmacological properties of mAChR-mediated [(35)S]GTPgammaS binding determined with a series of muscarinic agonists and antagonists were almost identical among the three brain regions investigated, i.e., cerebral cortex, hippocampus, and striatum, except for the apparent partial agonist effects of (alphaR)-alpha-cyclopentyl-alpha-hydroxy-N-[1-(4-methyl-3-pentenyl)-4-piperidinyl ]benzeneacetamide fumarate (J 104129) observed only in the hippocampus, but not in the other two regions. Among the muscarinic toxins investigated, only MT3 attenuated CCh-stimulated [(35)S] GTPgammaS binding. The highly selective allosteric potentiator at the M4 mAChR subtype, 3-amino-N-[(4-chlorophenyl)methyl]-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamid e (VU 10010), shifted the concentration-response curve for CCh leftwards as well as upwards. On the other hand, neither thiochrome nor brucine N-oxide was effective. The increases induced by CCh and 5-HT were essentially additive, though not completely, indicating that the mAChRs and 5-HT1A receptors were coupled independently to distinct pools of Gi/o proteins. Collectively, all of the data suggest that functional activation of Gi/o proteins coupled to mAChRs, especially the M4 subtype, is detectable by means of CCh-stimulated [(35)S]GTPgammaS binding assay in rat discrete brain regions.
