Description
VU0152100 is a potent and selective allosteric potentiator of M4 mAChR with an EC50 of 380 ± 93 nM. VU0152099 is a potent, selective and brain-penetrant mAChR M4 positive allosteric modulator with an EC50 of 0.4 µM for rat M4 receptor. VU0152099 is inactive for other mAChR subtypes or other GPCRs. VU0152099 has no agonist activity but potentiated responses of M4 to acetylcholine.
Product information
CAS Number: 612514-42-8
Molecular Weight: 355.41
Formula: C18H17N3O3S
Chemical Name: 3-amino-N-[(2H-1, 3-benzodioxol-5-yl)methyl]-4, 6-dimethylthieno[2, 3-b]pyridine-2-carboxamide
Smiles: CC1C=C(C)N=C2SC(=C(N)C=12)C(=O)NCC1C=CC2OCOC=2C=1
InChiKey: AZOGCTMOKNTHIU-UHFFFAOYSA-N
InChi: InChI=1S/C18H17N3O3S/c1-9-5-10(2)21-18-14(9)15(19)16(25-18)17(22)20-7-11-3-4-12-13(6-11)24-8-23-12/h3-6H,7-8,19H2,1-2H3,(H,20,22)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: To be determined
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:
VU0152099 (30 µM) induces a dose-dependent leftward shift of the acetylcholine (ACh) concentration response curve (CRC) with maximal shifts of 30-fold observed with 30 µM. VU0152099 dose-dependently potentiates the response to an EC20 concentration of ACh with EC50 values of 1.2 µM, and increases the maximal response to ACh to approximately 130%. VU0152099 is a potent positive allosteric modulator that enhance the response of the M4 receptor to the endogenous agonist ACh.
In Vivo:
VU0152099 (56.6 mg/kg; i.p.; once) reverses Amphetamine-induced hyperlocomotion in rats
References:
- Brady AE, et al. Centrally active allosteric potentiators of the M4 muscarinic acetylcholine receptor reverse amphetamine-induced hyperlocomotor activity in rats. J Pharmacol Exp Ther. 2008 Dec;327(3):941-53.
Products are for research use only. Not for human use.
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