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L9919

Sigma-Aldrich

LY2033298

≥98% (HPLC)

Sinônimo(s):

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

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About This Item

Fórmula empírica (Notação de Hill):
C13H14ClN3O2S
Número CAS:
886047-13-8
Peso molecular:
311.79
Número MDL:
MFCD12912423
Código UNSPSC:
12352200
ID de substância PubChem:
329817677
NACRES:
NA.77

Ensaio

≥98% (HPLC)

forma

solid

condição de armazenamento

desiccated

cor

off-white to tan

solubilidade

DMSO: >20 mg/mL

originador

Eli Lilly

temperatura de armazenamento

−20°C

cadeia de caracteres SMILES

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)

chave InChI

CTEGQKDJTBWFHW-UHFFFAOYSA-N

Ações bioquímicas/fisiológicas

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.

Características e benefícios

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

Pictogramas

Health hazard
GHS08

Palavra indicadora

Danger

Frases de perigo

H334

Declarações de precaução

P261 - P284 - P501

Classificações de perigo

Resp. Sens. 1

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable

Certificados de análise (COA)

Busque Certificados de análise (COA) digitando o Número do Lote do produto. Os números de lote e remessa podem ser encontrados no rótulo de um produto após a palavra “Lot” ou “Batch”.

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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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