AR-9281

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C18H29N3O2
Molecular Weight	319.4418
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CC(=O)N1CCC(CC1)NC(=O)NC23CC4CC(CC(C4)C2)C3

InChI

InChIKey=HUDQLWBKJOMXSZ-UHFFFAOYSA-N

InChI=1S/C18H29N3O2/c1-12(22)21-4-2-16(3-5-21)19-17(23)20-18-9-13-6-14(10-18)8-15(7-13)11-18/h13-16H,2-11H2,1H3,(H2,19,20,23)

HIDE SMILES / InChI

Molecular Formula	C18H29N3O2
Molecular Weight	319.4418
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Approval Year

Targets

Targets

Primary Target	Pharmacology	Condition	Potency
Epoxide hydratase 4	Inhibitor 8,297		7.0 nM [IC50]

Substance Class	Chemical
Record UNII	4HA03Q8EZ9
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

AR-9281

Common Name

English

UREA, N-(1-ACETYL-4-PIPERIDINYL)-N'-TRICYCLO(3.3.1.13,7)DEC-1-YL-

Systematic Name

English

1-(ADAMANTANE-1-YL)-3-(1-ACETYLPIPERIDINE-4-YL)UREA

Systematic Name

English

J3.137.087F

Code

English

APAU

Common Name

English

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Code System

Code

Type

Description

FDA UNII

4HA03Q8EZ9

PRIMARY

PUBCHEM

12000797

PRIMARY

DRUG BANK

DB06345

PRIMARY

CAS

1231741-41-5

NO STRUCTURE GIVEN

CAS

913548-29-5

PRIMARY

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Related Record

Type

Details


					JEH09DQZ6V

BIFUNCTIONAL EPOXIDE HYDROLASE 2

TARGET -> INHIBITOR

Amount:

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Related Record

Type

Details


					4HA03Q8EZ9

AR-9281

ACTIVE MOIETY

Comments:

AR9281, a potent and selective inhibitor of soluble epoxide hydrolase (s-EH), is in clinical development targeting hypertension and type 2 diabetes. The safety, pharmacokinetics, and pharmacodynamics of AR9281 were evaluated in double-blind, randomized, placebo-controlled, ascending, single oral dose (10-1000 mg) and multiple dose (100-400 mg every 8 hours for 7 days) studies in healthy subjects. AR9281 was well tolerated, and no dose-related adverse events were observed during either study. The drug was rapidly absorbed with a mean terminal half-life ranging from 3 to 5 hours. The area under the plasma concentration-time curve increased in an approximately dose-proportional manner up to the 500-mg dose and exhibited a greater than dose linearity at higher doses. AR9281 directly and dose-dependently inhibited blood s-EH activity with 90% inhibition or greater over an 8-hour period at the 250-mg dose and over a 12-hour period at the 500-mg dose. Multiple doses of AR9281 ranging from 100 to 400 mg every 8 hours resulted in a sustained inhibition of s-EH activity at 90% or greater during the trough. The current studies provide proof of safety and target inhibition of AR9281 in healthy subjects. AR9281 pharmacokinetic and pharmacodynamic characteristics support a twice-daily or thrice-daily dosing regimen in patients.

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