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L9919

Sigma-Aldrich

LY2033298

≥98% (HPLC)

Sinonimo/i:

3-Amino-5-chloro-N-cyclopropyl-6-methoxy-4-methyl-thieno[2,3-b]pyridine-2-carboxamide

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About This Item

Formula empirica (notazione di Hill):
C13H14ClN3O2S
Numero CAS:
886047-13-8
Peso molecolare:
311.79
Numero MDL:
MFCD12912423
Codice UNSPSC:
12352200
ID PubChem:
329817677
NACRES:
NA.77

Livello qualitativo

100

Saggio

≥98% (HPLC)

Stato

solid

Condizioni di stoccaggio

desiccated

Colore

off-white to tan

Solubilità

DMSO: >20 mg/mL

Ideatore

Eli Lilly

Temperatura di conservazione

−20°C

Stringa SMILE

COc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl

InChI

1S/C13H14ClN3O2S/c1-5-7-9(15)10(11(18)16-6-3-4-6)20-13(7)17-12(19-2)8(5)14/h6H,3-4,15H2,1-2H3,(H,16,18)
CTEGQKDJTBWFHW-UHFFFAOYSA-N

Azioni biochim/fisiol

LY2033298 is a robust allosteric potentiator that is highly selective for the human M4 muscarinic acetylcholine receptor subtype. LY2033298 potentiates ACh-M4 binding, with no effect at M1/3/5 receptors. LY2033298 can also bind to the M ACh receptor, and mediate either positive or negative allosteric effects depending on the ligand used to probe receptor activity.

Caratteristiche e vantaggi

This compound was developed by Eli Lilly. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Pittogrammi

Health hazard
GHS08

Avvertenze

Danger

Indicazioni di pericolo

H334

Consigli di prudenza

P261 - P284 - P501

Classi di pericolo

Resp. Sens. 1

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

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Certificati d'analisi (COA)

Lot/Batch Number
046M4744V
049K4600

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Vindhya Nawaratne et al.
Molecular pharmacology, 74(4), 1119-1131 (2008-07-17)
The M4 muscarinic acetylcholine (ACh) receptor (mAChR) is a potential therapeutic target but characterized by a lack of subtype-selective ligands. We recently generated "designer receptors exclusively activated by a designer drug" (DREADDs), which contained mutations of two conserved orthosteric-site residues
W Y Chan et al.
Proceedings of the National Academy of Sciences of the United States of America, 105(31), 10978-10983 (2008-08-06)
Current antipsychotics provide symptomatic relief for patients suffering from schizophrenia and related psychoses; however, their effectiveness is variable and many patients discontinue treatment due to side effects. Although the etiology of schizophrenia is still unclear, a leading hypothesis implicates an
Jana K Shirey et al.
Nature chemical biology, 4(1), 42-50 (2007-12-07)
Muscarinic acetylcholine receptors (mAChRs) provide viable targets for the treatment of multiple central nervous system disorders. We have used cheminformatics and medicinal chemistry to develop new, highly selective M4 allosteric potentiators. VU10010, the lead compound, potentiates the M4 response to
Michael Bubser et al.
ACS chemical neuroscience, 5(10), 920-942 (2014-08-20)
Positive allosteric modulators (PAMs) of the M4 muscarinic acetylcholine receptor (mAChR) represent a novel approach for the treatment of psychotic symptoms associated with schizophrenia and other neuropsychiatric disorders. We recently reported that the selective M4 PAM VU0152100 produced an antipsychotic
Jing Wu et al.
European journal of pharmacology, 882, 173274-173274 (2020-06-14)
Opioids strongly inhibit GABAergic neurons in the rostromedial tegmental nucleus (RMTg) that expresses μ-opioid receptors to induce rewarding and psychomotor effects. M3 and M4 muscarinic receptors are co-localized with μ-opioid receptors at these GABAergic neurons. This study explored whether RMTg
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