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A-69412

Catalog No. T10208 CAS 123606-23-5

Synonyms: N-1-(Fur-3-ylethyl)-N-hydroxyurea

A-69412 (N-1-(Fur-3-ylethyl)-N-hydroxyurea) is a reversible, specific inhibitor of the hydrophilic 5-lipoxygenase. It has the potential to treat ulcerative colitis and asthma, and possibly other inflammatory and allergic conditions.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

A-69412, CAS 123606-23-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 195.00
5 mg	In stock	$ 449.00
10 mg	In stock	$ 659.00
25 mg	In stock	$ 987.00
50 mg	In stock	$ 1,390.00
100 mg	In stock	$ 1,880.00
500 mg	In stock	$ 3,780.00
1 mL * 10 mM (in DMSO)	In stock	$ 342.00

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Purity: 99.89%

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Description	A-69412 (N-1-(Fur-3-ylethyl)-N-hydroxyurea) is a reversible, specific inhibitor of the hydrophilic 5-lipoxygenase. It has the potential to treat ulcerative colitis and asthma, and possibly other inflammatory and allergic conditions.
Targets&IC50	5-LOX:1 μM, LTB4:1 μM
In vitro	A-69412 inhibits the formation of 5-HETE by the 20000×g supernatant of RBL-I cells in a dose-dependent fashion. A-69412 also inhibits the formation of LTB4 in calcium ionophore A23187 stimulated human PMNL (IC50=8.9 μM). A-69412 is more potent in inhibiting LTB4 formation in ionophore-stimulated human whole blood. The potency of A-69412 in a number of assays using several donors consistently show activity in the low micromolar range (mean IC50=1.4 μM, range 0.5-3 μM, 9 donors), several-fold more potent than its activity in the other in vitro assays[1].
In vivo	Oral administration of A-69412 effectively inhibits leukotriene production across various species, demonstrating its potent, long-acting nature. In rats, A-69412 exhibits strong inhibition of leukotriene formation with an oral effective dose (ED50) of 5 mg/kg. Similarly, in dogs, a single dose of 5 mg/kg ensures nearly complete leukotriene inhibition for up to 16 hours, with plasma concentrations measuring 38 μM at 0.5 hours post-dose and reducing to 5 μM at 16 hours. These results align with ex vivo observations of 100% inhibition at 0.5 hours and 90% at 16 hours post-dosing. Moreover, A-69412 outperforms zileuton in cynomolgus monkeys, maintaining over 50% inhibition of LTB4 biosynthesis for 8 hours compared to zileuton's effectiveness within just the first 2 hours post-dosing. In rat models of anaphylactic reaction, oral A-69412 dose-dependently curbs leukotriene production in the peritoneal cavity, with blood levels ranging between 4 to 100 μM for doses of 2 to 50 mg/kg. Remarkably, A-69412 continues to significantly inhibit leukotriene production when administered up to 8 hours before the antigen challenge, with plasma concentrations ranging from 44 μM at 0.5 hours to 10 μM at 8 hours post-dosing[1].
Animal Research	A-69412 is suspended in 0.2% methylcellulose with a Potter-Elvehjem homogenizer equipped with a Teflon-coated pestle and administered orally (20 mg/kg) to beagle dogs, cynomolgus monkeys, and male SD rats. Zileuton is used for comparison. All animals are fasted overnight before dosing but allowed water ad libitum. Heparinized blood samples are obtained before and at various times after compound administration in the dog and monkey studies. Groups of rats are dosed with vehicle or A-69412 and 1 h and 15 min later, the animals are sacrificed and blood collected by cardiac puncture into heparinized syringes. Aliquots of blood from all the three species are incubated at 37°C with 50 μM calcium ionophore, A23187. After 30min, the blood is placed in an ice bath and analyzed for LTB4.

Synonyms	N-1-(Fur-3-ylethyl)-N-hydroxyurea
Molecular Weight	170.17
Formula	C7H10N2O3
CAS No.	123606-23-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45 mg/mL (264.44 mM)

References and Literature

1. Bell RL, et al. The properties of A-69412: a small hydrophilic 5-lipoxygenase inhibitor. Agents Actions. 1993 Mar; 38(3-4):178-87.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compound Library Bioactive Compounds Library Max

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

A-69412 123606-23-5 Metabolism Lipoxygenase A 69412 A69412 N-1-(Fur-3-ylethyl)-N-hydroxyurea inhibitor inhibit

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