[CAS NO. 274925-86-9] Nebicapone

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PRODUCTS SPECIFICATIONS [274925-86-9]

Catalog

HY-106405

Brand

MCE

CAS

274925-86-9

DESCRIPTION [274925-86-9]

Overview

MDL	-
Molecular Weight	273.24
Molecular Formula	C14H11NO5
SMILES	O=C(C1=CC([N+]([O-])=O)=C(O)C(O)=C1)CC2=CC=CC=C2

For research use only. We do not sell to patients.

Summary

Nebicapone (BIA 3-202), a reversible catechol-O-methyltransferase (COMT) inhibitor, is mainly metabolized by glucuronidation. Nebicapone is mainly peripherally acting inhibitor that decreases the biotransformation of L-DOPA to 3-O-methyl-DOPA by inhibition of COMT , and it is potential for the treatment of Parkinson's disease ^[1] .

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02772614	Bial - Portela C S.A.	Parkinson´s Disease	January 2006	Phase 1
NCT02763839	Bial - Portela C S.A.	Parkinson´s Disease	April 2001	Phase 1
NCT03103399	Bial - Portela C S.A.	Parkinson Disease	September 26, 2006	Phase 2
NCT02778594	Bial - Portela C S.A.	Parkinson´s Disease (PD)	September 2005	Phase 1
NCT02774564	Bial - Portela C S.A.	Parkinson´s Disease	September 2005	Phase 1
NCT02779348	Bial - Portela C S.A.	Healthy	September 2006	Phase 1
NCT02772627	Bial - Portela C S.A.	Parkinson´s Disease	September 2001	Phase 1
NCT03097211	Bial - Portela C S.A.	Parkinson Disease	July 17, 2006	Phase 1
NCT02763852	Bial - Portela C S.A.	Parkinson´s Disease	April 2001	Phase 1
NCT02834507	Bial - Portela C S.A.	Parkinson´s Disease (PD)	March 2005	Phase 2
NCT02763800	Bial - Portela C S.A.	Parkinson´s Disease	September 2000	Phase 1
NCT02763787	Bial - Portela C S.A.	Parkinson´s Disease	April 2000	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL ( 365.98 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.6598 mL	18.2989 mL	36.5979 mL
5 mM	0.7320 mL	3.6598 mL	7.3196 mL
10 mM	0.3660 mL	1.8299 mL	3.6598 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (9.15 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Loureiro AI, et al. Human metabolism of nebicapone (BIA 3-202), a novel catechol-o-methyltransferase inhibitor: characterization of in vitro glucuronidation. Drug Metab Dispos. 2006 Nov;34(11):1856-62.