2230009-48-8
Chemical Structure
Alogabat
Synonym(s): RG-7816; RO-7017773
- CAS No.: 2230009-48-8
- Formula:C21H23N5O4
- Molecular Weight:409.44
IUPAC Name: 6-((5-methyl-3-(6-methylpyridin-3-yl)isoxazol-4-yl)methoxy)-N-(tetrahydro-2H-pyran-4-yl)pyridazine-3-carboxamide
InChIKey: ACZCJTHHWMBFKC-UHFFFAOYSA-N
SMILES: O=C(C1=NN=C(OCC2=C(C)ON=C2C3=CC=C(C)N=C3)C=C1)NC4CCOCC4
Biological Activity: Alogabat is a positive allosteric modulator (PAM) and agonist (Ki <100 nM) of the GABAA α5 receptor, targeting the α5β3γ2 subunit with a Ki of 8.7 nM. Alogabat increases the expression level of α5β3γ2 in oocytes (1.97-fold). GABAA has been implicated in cognitive impairment associated with central nervous system (CNS) disorders, brain cancer (including brain tumors such as medulloblastoma), and can be used in the study of mild cognitive impairment (MCI), amnestic MCI (aMCI), age-associated memory impairment (AAMI), age-related cognitive decline (ARCD), dementia, Alzheimer's disease (AD), prodromal AD, post-traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cognitive impairment associated with cancer treatment, mental retardation, Parkinson's disease (PD), autism spectrum disorder, fragile X, Rett syndrome, obsessive-compulsive behavior, and substance addiction[1][2].
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Alogabat | 99.93% | Alogabat is a positive allosteric modulator (PAM) and agonist (Ki <100 nM) of the GABAA α5 receptor, targeting the α5β3γ2 subunit with a Ki of 8.7 nM. Alogabat increases the expression level of α5β3γ2 in oocytes (1.97-fold). GABAA has been implicated in cognitive impairment associated with central nervous system (CNS) disorders, brain cancer (including brain tumors such as medulloblastoma), and can be used in the study of mild cognitive impairment (MCI), amnestic MCI (aMCI), age-associated memory impairment (AAMI), age-related cognitive decline (ARCD), dementia, Alzheimer's disease (AD), prodromal AD, post-traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cognitive impairment associated with cancer treatment, mental retardation, Parkinson's disease (PD), autism spectrum disorder, fragile X, Rett syndrome, obsessive-compulsive behavior, and substance addiction. | ||||||||||||||||||||
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- [1]. Bernd Buettelmann, et al. Preparation of new isoxazolyl ether derivatives as GABAA α5 receptor positive allosteric modulators (PAMs). World Intellectual Property Organization, WO2018104419 A1 2018-06-14.
- [2]. Belew Mekonnen, et al. Benzazepine derivatives for the treatment of cognitive impairment and their preparation. World Intellectual Property Organization, WO2024039886 A1 2024-02-22.
Keywords
