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251406 Sigma-AldrichD-Amino Acid Oxidase Inhibitor III, AS057278 - CAS 402-61-9 - Calbiochem

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Literatur
Data Sheet

Synonyme: 5-methyl-1H-pyrazole-3-carboxylic acid, DAAO Inhibitor III

Primary Target: DAAO

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Übersicht

Replacement Information

Key Spec Table

CAS #	Empirical Formula
402-61-9	C₅H₆N₂O₂

Preis & Verfügbarkeit

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Description
Overview	A cell-permeable pyrazolocarboxylic acid that acts as a selective D-amino acid oxidase (DAO/DAAO/DAMOX/OXDA) inhibitor (IC₅₀ = 910 nM against human DAO; [D-ser] = 10 mM) and effectively protects DAO overexpressing cultures from oxidative stress-induced cell death upon D-Ser (50 mM) exposure (ED₅₀ ≤3.95 µM), while exhibiting little affinity toward NMDAR glycine binding site or inhibitory activity against D-aspartate oxidase (DDO/DSOX). Reported to be orally available and blood-brain barrier-permeant in rats and effectively prevent PCP (phencyclidine) from suppressing PPI (prepulse inhibition) response in mice (single 80 mg/kg or 56X 20 mg/kg/12 h b.i.d. oral dosages) in vivo.
Catalogue Number	251406
Brand Family	Calbiochem®
Synonyms	5-methyl-1H-pyrazole-3-carboxylic acid, DAAO Inhibitor III

References
References	Smith, S., et al. 2010. Open Med. Chem. J. 27, 3. Williams, M. 2009. Biochem. Pharmacol. 78, 1360. Adage, T., et al. 2008. Eur. Neuropsychopharmacol. 18, 200.

Product Information
CAS number	402-61-9
Form	White solid
Hill Formula	C₅H₆N₂O₂
Chemical formula	C₅H₆N₂O₂
Reversible	Y
Structure formula Image
Quality Level	MQ100

Applications

Biological Information
Primary Target	DAAO
Primary Target IC<sub>50</sub>	910 nM
Purity	≥99% by HPLC

Physicochemical Information

Dimensions

Materials Information

Toxicological Information

Safety Information according to GHS

Safety Information

Product Usage Statements

Storage and Shipping Information
Ship Code	Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity	Standard Handling
Storage	+2°C to +8°C
Protect from Light	Protect from light
Do not freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Packaging Information
Packaged under inert gas	Packaged under inert gas

Transport Information

Supplemental Information

Specifications

Global Trade Item Number
Bestellnummer	GTIN
251406-50MG	04055977199215

Documentation

Literatur

Übersicht
Smith, S., et al. 2010. Open Med. Chem. J. 27, 3. Williams, M. 2009. Biochem. Pharmacol. 78, 1360. Adage, T., et al. 2008. Eur. Neuropsychopharmacol. 18, 200.

Datenblatt

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision	08-March-2013 JSW
Synonyms	5-methyl-1H-pyrazole-3-carboxylic acid, DAAO Inhibitor III
Description	A cell-permeable pyrazolocarboxylic acid that acts as a selective D-amino acid oxidase (DAO/DAAO/DAMOX/OXDA) inhibitor (IC₅₀ = 910 nM against human DAO; [D-ser] = 10 mM) and effectively protects DAO overexpressing cultures from oxidative stress-induced cell death upon D-Ser (50 mM) exposure (ED₅₀ ≤3.95 µM), while exhibiting little affinity toward NMDAR glycine binding site (6% inhibition at 100 µM), nor inhibitory activity against D-aspartate oxidase (DDO/DSOX; 43% inhibition at 100 µM) or serine racemase (no inhibition at 50 µM). AS057278 is orally available (plasma C_max = 8.089 µg/mL; t_1/2 = 7.21 h; t_max = 1 h post 10 mg/mL oral dosing in rats) and can cross blood-brain barrier (1.622 and 0.578 µg/g brain tissue, respectively, 15 and 60 min post single 10 mg/kg i.v. dosing in rats). Effectively prevents PCP (phencyclidine) from suppressing PPI (prepulse inhibition; prepulse noise = 82 dB, startle noise = 120 dB) response in mice via either long-term oral administration (93% and 70% of no-PCP control PPI level, respectively, with or without 28-day b.i.d, treatment at 20 mg/kg/12 h) or single acute heavy oral dosing (93% and 53% of no-PCP control PPI level, respectively, with or without 80 mg/kg dosing) 60 min prior to PCP treatment (8 mg/kg i.p.) in vivo.
Form	White solid
Intert gas (Yes/No)	Packaged under inert gas
CAS number	402-61-9
Chemical formula	C₅H₆N₂O₂
Structure formula
Purity	≥99% by HPLC
Solubility	DMSO (50 mg/ml)
Storage	Protect from light +2°C to +8°C
Do Not Freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity	Standard Handling
References	Smith, S., et al. 2010. Open Med. Chem. J. 27, 3. Williams, M. 2009. Biochem. Pharmacol. 78, 1360. Adage, T., et al. 2008. Eur. Neuropsychopharmacol. 18, 200.

Kategorien

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Other Inhibitors of Biological Interest

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