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409351-28-6 (VU0152100)

1

Identification

VU0152100 VU0152100
Name VU0152100
Formula C18H19N3O2S
MW 341.43
CAS No. 409351-28-6
EINECS
Smiles CC1=C2C(SC(C(NCC3=CC=C(OC)C=C3)=O)=C2N)=NC(C)=C1
Synonyms VU152100;VU 0152100;VU-0152100; 3-amino-N-(4-methoxybenzyl)-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamide
InChI InChI=1S/C18H19N3O2S/c1-10-8-11(2)21-18-14(10)15(19)16(24-18)17(22)20-9-12-4-6-13(23-3)7-5-12/h4-8H,9,19H2,1-3H3,(H,20,22)
2

Introduction

VU0152100 is a potent and selective allosteric potentiator of M4 mAChR with an EC50 of 380 ± 93 nM. IC50 Value: 380 ± 93 nM (EC50) [1] Target: M4 mAChR in vitro: VU0152100 was selective for M4 relative to M1, M2, M3, and M5.

Background Information

Positive allosteric modulator of muscarinic choline receptor M4. Potentiates activation by acetylcholine, but posesses no intrinsic agonist activity alone. ......by AbMole BioScience
VU0152100 is a selective and positive allosteric modulators of M4 receptor. It has shown a potent positive allosteric modulators that increase the response of the M4 receptor to the endogenous agonist ACh in in vitro study. And it has been revealed to enh ......by BOC Sciences
VU0152100 is a highly selective M4 positive allosteric modulator (PAM) that exerts central effects after systemic administration. VU0152100 dose-dependently reverses amphetamine-induced hyperlocomotion in rats and wild-type mice, but not in M4 KO mice. VU0152100 also blocks amphetamine-induced disruption of the acquisition of contextual fear conditioning and prepulse inhibition of the acoustic startle reflex. ......by MedKoo Biosciences, Inc.
VU0152100 (VU152100) is a potent, selective positive allosteric modulator of M4 mAChR with EC50 of 0.38 uM for rat M4; potentiates the M4-mediated calcium response calcium response with maximal shifts of 70-fold with 10 uM in vitro assays; inhibits behavioral and neurochemical effects of cocaine in vivo, also dose-dependently reverses amphetamine-induced hyperlocomotion in rats and wild-type mice, blocks amphetamine-induced disruption of the acquisition of contextual fear conditioning. ......by ProbeChem
Selective positive allosteric modulator of M4 muscarinic acetylcholine receptors (mAChRs) (EC50 = 380 nM). Induces 21-fold shift in ACh potency at M4 receptor. Displays no activity at other mAChR subtypes. ......by Tocris Bioscience Inc.
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

4

Physical and Chemical Properties

Appearance:light?yellow?to earth yellow Solid EBNumber:EB000023490

Storage condition

Store at RT by Tocris Bioscience Inc.

Solubility

DMSO >50 mg/mL by MedChemexpress Co., Ltd.
Soluble to 50 mM in DMSO by Tocris Bioscience Inc.
5

Mechanism and Indication

Signaling Pathways Neuronal Signaling GPCR/G Protein
Target mAChR
Research Area Neurological Disease
Indications
6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
VU0152100 - Discovery
VU0152100 - No Development Reported
7

Safety Data of VU0152100

8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AbMole BioScience USA
Apexbio Technology LLC USA
Ark Pharm, Inc. USA
BOC Sciences
Biochempartner Co., Ltd China
CHEMSCENE, LLC 10mg/USD144();50mg/USD636() USA
MedChemexpress Co., Ltd. 10mg/USD144();50mg/USD636() USA
MedKoo Biosciences, Inc. USA
ProbeChem
Shanghai Haoyuan Chemexpress Co., Ltd. 10mg/USD144();50mg/USD636() China
Tocris Bioscience Inc. USA
10

Related Products

Other Forms of 409351-28-6

Name CAS No Formula MW

Recommended Compounds in mAChR

Name CAS No Formula MW
Pilocarpine (Hydrochloride) 54-71-7 C11H17ClN2O2 244.72
Imidafenacin 170105-16-5 C20H21N3O 319.4
Flavoxate (hydrochloride) 3717-88-2 C24H26ClNO4 427.92
Homatropine (Bromide) 51-56-9 C16H22BrNO3 356.25
Benztropine (mesylate) 132-17-2 C22H29NO4S 403.54
Otilonium (bromide) 26095-59-0 C29H43BrN2O4 563.57
Arecoline (hydrobromide) 300-08-3 C8H14BrNO2 236.11
Trospium (chloride) 10405-02-4 C25H30ClNO3 427.96
Tiotropium (bromide hydrate) 139404-48-1 C19H24BrNO5S2 490.43
Revefenacin 864750-70-9 C35H43N5O4 597.747
Oxybutynin (chloride) 1508-65-2 C22H32ClNO3 393.95
Gallamine Triethiodide 65-29-2 C30H60I3N3O3 891.53
Bethanechol (chloride) 590-63-6 C7H17ClN2O2 196.68
Atropine (sulfate monohydrate) 5908-99-6 C34H50N2O11S 694.83
Methscopolamine (bromide) 155-41-9 C18H24BrNO4 398.29
Irsogladine (maleate) 84504-69-8 C13H11Cl2N5O4 372.16
Irsogladine 57381-26-7 C9H7Cl2N5 256.09
Tropicamide 1508-75-4 C17H20N2O2 284.35
Oxybutynin 5633-20-5 C22H31NO3 357.49
Ipratropium (bromide) 22254-24-6 C20H30BrNO3 412.36

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

12

References

13

More Information

VU0152100

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