Description
VU10010 is a potent, highly selective and allosteric M4 mAChR potentiator with an EC50 of 400 nM. VU10010 binds to an allosteric site on M4 mAChR and increases affinity for acetylcholine and coupling to G proteins. VU10010 increases carbachol-induced depression of transmission at excitatory but not inhibitory synapses in the hippocampus.
Product information
CAS Number: 633283-39-3
Molecular Weight: 345.85
Formula: C17H16ClN3OS
Chemical Name: 3-amino-N-[(4-chlorophenyl)methyl]-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamide
Smiles: CC1C=C(C)N=C2SC(=C(N)C=12)C(=O)NCC1C=CC(Cl)=CC=1
InChiKey: FPRULFHDSFKYBV-UHFFFAOYSA-N
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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
VU10010 potentiates the M4 response to acetylcholine 47-fold while having no activity at other mAChR subtypes (rM1, rM2, rM3 or rM5). VU10010 causes an increase in affinity for ACh and M4-mediated [35S]GTPγS binding. VU10010 (10 μM) has no agonist, antagonist or allosteric potentiator activity at P2Y1R or mGluR5. The EC50 values are 33 and 0.7 nM for ACh in the absence and presence of VU10010, respectively.
Products are for research use only. Not for human use.
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