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AB120146

AF-DX 384, M2/M4 antagonist

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MW 478.6 Da, Purity >95%. M2/M4 receptor antagonist (Kd values are 1 (M2), 2.2 (M4), 15 (M3) and 55 nM (M1)). Low blood-brain barrier permeability.

대체 명칭 보기

7TM receptor, ACM2_HUMAN, ACM3_HUMAN, ACM4_HUMAN, ACM5_HUMAN, AChR, AChR M5, Acetylcholine receptor muscarinic 5, Acetylcholine receptor, muscarinic, 2, CHKM5MR, CHRM 2, CHRM 3, CHRM1, CM2, Cholinergic receptor muscarinic 1, Cholinergic receptor muscarinic 2, Cholinergic receptor muscarinic 4, Cholinergic receptor muscarinic 5, Cholinergic receptor, muscarinic 2, cardiac, Cholinergic receptor, muscarinic 2, isoform a, Cholinergic receptor, muscarinic 2a, Chrm 4, Chrm 5, EGBRS, FLJ43243, HM 2, HM 3, HM 4, HM 5, HM1, M2 muscarinic receptor, M2-mAChR, M3 muscarinic receptor, M4, M5R, MGC120006, MGC120007, MGC41838, Muscarinic M2 receptor, Muscarinic acetylcholine receptor M1, Muscarinic acetylcholine receptor M2, Muscarinic acetylcholine receptor M3, Muscarinic acetylcholine receptor M4, Muscarinic acetylcholine receptor M5, cholinergic receptor muscarinic 3, chrm2a, m3 muscarinic acetylcholine receptor, m5, muscarinic 3, muscarinic cholinergic m3 receptor, muscarinic m3 receptor

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Chemical Structure - AF-DX 384, M2/M4 antagonist (AB120146)
  • Chemical Structure

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Chemical Structure - AF-DX 384, M2/M4 antagonist (AB120146)

2D chemical structure image of ab120146, AF-DX 384, M2/M4 antagonist

주요 정보

CAS 번호

118290-27-0

Purity

>95%

제형

Solid

form

Molecular weight

478.6 Da

Molecular formula

C<sub>2</sub><sub>7</sub>H<sub>3</sub><sub>8</sub>N<sub>6</sub>O<sub>2</sub>

PubChem

119357

Nature

Synthetic

Solubility

Soluble in DMSO to 50 mM

Soluble in ethanol to 10 mM

생화학적 명칭

N-[2-[2-[(dipropylamino)methyl]piperidin-1-yl]ethyl]-6-oxo-5H-pyrido[2,3-b][1,4]benzodiazepine-11-carboxamide

생물학적 정보

M2/M4 receptor antagonist (Kd values are 1 (M2), 2.2 (M4), 15 (M3) and 55 nM (M1)). Low blood-brain barrier permeability.

Canonical SMILES

CCCN(CCC)CC1CCCCN1CCNC(=O)N2C3=CC=CC=C3C(=O)NC4=C2N=CC=C4

InChi

InChI=1S/C27H38N6O2/c1-3-16-31(17-4-2)20-21-10-7-8-18-32(21)19-15-29-27(35)33-24-13-6-5-11-22(24)26(34)30-23-12-9-14-28-25(23)33/h5-6,9,11-14,21H,3-4,7-8,10,15-20H2,1-2H3,(H,29,35)(H,30,34)

InChiKey

MZDYABXXPZNUCT-UHFFFAOYSA-N

IUPAC Name

N-[2-[2-[(dipropylamino)methyl]piperidin-1-yl]ethyl]-6-oxo-5H-pyrido[2,3-b][1,4]benzodiazepine-11-carboxamide

특성 및 보관 정보

배송 시 보관 조건
Ambient - Can Ship with Ice
적절한 단기 보관 조건
Ambient
적절한 장기 보관 조건
Ambient
보관 정보
The product can be stored for up to 12 months
취급 방법

Need more advice on solubility, usage and handling? Please visit our our product support page for more details.

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Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

추가 정보

This supplementary information is collated from multiple sources and compiled automatically.

Muscarinic acetylcholine receptors also known as mAChRs are a group of G protein-coupled receptors that bind acetylcholine. They include five distinct subtypes: CHRM1 CHRM2 CHRM3 CHRM4 and CHRM5. These receptors have variable molecular masses ranging from approximately 50 to 60 kDa. Expression of muscarinic receptors is widespread present in both central and peripheral nervous systems and in non-neuronal tissues such as heart and smooth muscle. Each subtype has a unique pattern of distribution affecting how the body reacts to stimuli.
Biological function summary

Muscarinic receptors mediate parasympathetic nervous system responses. They do not function in isolation and may form complexes with other membrane proteins. mAChRs play roles in reducing heart rate constricting bronchi increasing secretions and modulating neurochemical activities in the central nervous system. Arecaidine can act as a muscarinic agonist whereas aclidinium serves as a muscarinic antagonist both influencing receptor activity through different pathways.

Pathways

Muscarinic receptors participate in the PI3K/AKT and MAPK signaling pathways. These pathways are key for cellular responses to environmental changes. For example muscarinic receptors in the cardiac tissue influence heart rate through these pathways interacting with proteins like Gi/o proteins. mAChRs also activate pathways involving other G protein receptors like adrenergic receptors to regulate vascular resistance and secretory processes.

Muscarinic receptors are linked to Alzheimer’s disease and chronic obstructive pulmonary disease (COPD). In Alzheimer’s imbalances in muscarinic receptor signaling can disrupt cognitive function. The CHRM1 subtype is particularly implicated in neurotransmission abnormalities associated with this disease. In COPD the CHRM3 subtype’s regulation of bronchoconstriction becomes clinically relevant. Therapeutic targeting of these receptors using antagonists like aclidinium helps manage symptoms and improve patient outcome.

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