MLE-4901

Research use only, not for human use.

A potent, selective, orally active neurokinin 3 (NK3R) antagonist for the treatment of schizophrenia.

A potent, selective, orally active neurokinin 3 (NK3R) antagonist for the treatment of schizophrenia; demonstrates drug-like properties with low metabolic turnover rate in vitro and moderate human plasma protein binding.Schizophrenia Phase 2 Discontinued.

Pavinetant (AZD2624) is a potent and selective NK3 receptor antagonist which is developed for the treatment of schizophrenia. Pavinetant exhibits an inhibitory effect on microsomal CYP3A4/5 activities with apparent IC50 values of 7.1 and 19.8 μM for midazolam and testosterone assays, respectively. No time-dependent inactivation of CYP3A4/5 activity by Pavinetant is observed. Pavinetant demonstrates weak to no inhibition of CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, and CYP2D6.

——

MLE4901 | AZD-2624 | AZD2624 | Pavinetant

GPCR/G Protein

Neurokinin Receptor

Neurokinin Receptor

Neurological Disease

Schizophrenia

941690-55-7

459.56

C26H25N3O3S

>98% (HPLC)

DMSO : ≥ 50 mg/mL 108.80 mM; H2O : < 0.1 mg/mL

O=C(C1=C(NS(=O)(C)=O)C(C2=CC=CC=C2)=NC3=CC=CC=C13)N[C@H](C4=CC=CC=C4)CC

(S)-3-(methylsulfonamido)-2-phenyl-N-(1-phenylpropyl)quinoline-4-carboxamide

(-20℃)

With Ice Pack

≥ 2 years