SUVN-911(compound 9h)

  Cat. No.:  DC31008   Featured
Chemical Structure
2414674-71-6
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Field of application
SUVN-911 (compound 9h) is a Novel, Potent, Selective, and Orally Active Neuronal Nicotinic Acetylcholine α4β2 Receptor Antagonist for the Treatment of Depression.Compound 9h is a potent α4β2 receptor ligand with a Ki value of 1.5 nM. It showed >10 μM binding affinity toward the ganglionic α3β4 receptor apart from showing selectivity over 70 other targets. It is orally bioavailable and showed good brain penetration in rats. Marked antidepressant activity and dose-dependent receptor occupancy in rats support its potential therapeutic utility in the treatment of depression. It does not affect the locomotor activity at doses several folds higher than its efficacy dose. It is devoid of cardiovascular and gastrointestinal side effects. Successful long-term safety studies in animals and phase-1 evaluation in healthy humans for safety, tolerability, and pharmacokinetics paved the way for its further development.
Cas No.: 2414674-71-6
Chemical Name: 3-(6-Chloropyridine-3-yloxymethyl)-2-azabicyclo[3.1.0]hexane Hydrochloride
Synonyms: 2414674-70-5(free base),SUVN-911,SUVN911,SUVN 911
SMILES: [C@H]12N[C@H](COC3C=NC(Cl)=CC=3)C[C@H]1C2.[H]Cl
Formula: C11H14Cl2N2O
M.Wt: 261.147
Purity: >97%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a Ki of 1.5 nM. SUVN-911 has antidepressant activity[1].
Target: Ki: 1.5 nM (α4β2 receptor)[1]
In Vivo: SUVN-911 is devoid of cardiovascular and gastrointestinal side effects[1]. SUVN-911 (1.0-10.0 mg/kg; p.o.; daily; for 3 days) shows significant antidepressant effects[1]. SUVN-911 shows metabolic stability in rats[1]. SUVN-911 (3 mg/kg; p.o.) has shown high oral exposures, longer half-lives and adequate brain penetration in Wistar rats[1]. Animal Model: Male Wistar rats (180-230 g)[1] Dosage: 1 mg/kg, 3 mg/kg, 10.0 mg/kg Administration: Oral administration, daily, for 3 days Result: Showed antidepressant like activity with no signs of tachyphylaxis. Animal Model: Male Wistar rats (225 ± 25 gm)[1] Dosage: 3 mg/kg (Pharmacokinetic Analysis) Administration: Oral administration Result: AUC=3507 ng*h/mL, T1/2=3.34 hours.
In Vitro: SUVN-911 displays high selectivity for α4β2 over α3β4 nAChR[1]. SUVN-911 shows good selectivity against over 70 receptors which includes GPCRs, ion channels, enzymes, peptides, steroids, second messengers, growth factors and prostaglandins[1].
References: [1]. Ramakrishna Nirogi, et al. Discovery and Development of 3-(6-Chloropyridine-3-yloxymethyl)-2-azabicyclo[3.1.0]hexane Hydrochloride (SUVN-911): A Novel, Potent, Selective, and Orally Active Neuronal Nicotinic Acetylcholine α4β2 Receptor Antagonist for the Treatment of Depression. J Med Chem. 2020 Mar 26;63(6):2833-2853.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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