AM103 - ≥99% , CAS No.1147872-22-7

CAS: 1147872-22-7 Cat. No.: A647147 分子式: C₃₆H₃₈N₃NaO₄S 分子量: 631.76 PubChem CID: 129010507

グレード＆純度 ≥99%

Storage

Store at 2-8°C,Protected from light,Desiccated

Shipped In

Wet ice

概要

AM 103 is a potent and selective FLAP inhibitor, with an IC 50 value of 4.2 nM.

In Vitro

AM 103 has an IC 50 value of 349 nM in the human blood LTB4 inhibition assay. AM 103 has an excellent CYP profile against the 5 most common CYP isoforms with IC 50 values greater than 30 μM for CYP2D6 and >50 μM for CYPs 3A4, 2C9 2C19, and 1A2. AM103 is a novel, potent, and selective FLAP inhibitor with IC 50 values of 350, 113, and 117 nM against human, rat, and mouse whole-blood ionophore-stimulated LTB4 production, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

AM 103 has high bioavailability (64%), low clearance (2.9 mL/min/kg), low volume of distribution (0.41 L/kg), and a long i.v. half-life (5.2 h) in dogs. AM 103 (10 mg/kg q.i.d.) inhibits the increase in CysLTs and EPO by approximately 60%, and IL-5 levels are reduced to the concentrations obtained following saline treatment alone in mice . AM103 (1 mg/kg, p.o.) displays >50% inhibition for up to 6 h with a calculated EC 50 of appr 60 nM, in a rat ex vivo whole-blood calcium ionophore-induced LTB4 assay. AM 103 inhibits LTB4 and cysteinyl leukotriene (CysLT) production with ED 50 values of 0.8 and 1 mg/kg, respectively, when rat lung is challenged in vivo with calcium ionophore. In this model, the EC 50 derived from plasma AM103 is appr 330 nM for inhibition of both LTB4 and CysLT. In a model of chronic lung inflammation using ovalbumin-primed and challenged BALB/c mice, AM103 reduces the concentrations of eosinophil peroxidase, CysLTs, and interleukin-5 in the bronchoalveolar lavage fluid. Finally, AM 103 increases survival time in mice exposed to a lethal intravenous injection of platelet-activating factor. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

IC50& Target:IC50: 4.2 nM (FLAP)

仕様

仕様と純度

≥99%

生化学的・生理学的メカニズム

AM 103 is a potent and selective FLAP inhibitor, with an IC 50 value of 4.2 nM.

保管条件

Store at 2-8°C,Protected from light,Desiccated

入荷

Wet ice

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

アクションタイプ

INHIBITOR

純度

≥99%

名前と識別子

カノニカル・スマイル

CC(C)(C)SC1=C(N(C2=C1C=C(C=C2)OCC3=CC=CC=N3)CC4=CC=C(C=C4)C5=CN=C(C=C5)OC)CC(C)(C)C(=O)O.[Na]

InChIKey

VANSVYMYESBUFV-UHFFFAOYSA-N

INCHI

1S/C36H39N3O4S.Na/c1-35(2,3)44-33-29-19-28(43-23-27-9-7-8-18-37-27)15-16-30(29)39(31(33)20-36(4,5)34(40)41)22-24-10-12-25(13-11-24)26-14-17-32(42-6)38-21-26;/h7-19,21H,20,22-23H2,1-6H3,(H,40,41);

PubChem CID

129010507

MeSH用語

3-(3-tert-butylsulfanyl-1-(4-(6-methoxypyridin-3-yl)benzyl)-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl)-2,2-dimethylpropionic acid;AM 103;AM-103;AM103

分子量

631.76

化学的性質と物理的性質

• 溶解度: DMSO : 200 mg/mL (316.58 mM; Need ultrasonic)