Factor D inhibitor 6 - 10mM in DMSO , CAS No.1386455-51-1

CAS: 1386455-51-1 Cat. No.: F655722 분자식: C₂₃H₂₂ClFN₆O₃ 분자량: 484.91

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

개요

Factor D inhibitor 6 is a potent, highly selective and orally active factor D (FD) inhibitor with an IC 50 of 30 nM and a K d of 6 nM. Factor D inhibitor 6 is inactive against factor B, lassical and lectin complement-pathway activation, and a broad assay panel of receptors, ion channels, kinases and proteases

In Vitro

Factor D inhibitor 6 (compound 6) effectively blocks both alternative pathway (AP)-mediated hemolysis in 10% human serum (IC 50 = 6 nM) and AP-induced membrane-attack complex (MAC) formation in lepirudinanticoagulated 50% human whole blood (IC 50 = 0.14 μM). Factor D inhibitor 6 (compound 6) shows modest inhibition of murine FD (IC 50 = 0.86 μM). Factor D inhibitor 6 (compound 6) inhibits both hemolysis and component 3 (C3) deposition on the surface of red blood cells (RBCs) with an IC 50 value of 70 nM, consistent with inhibition of the AP amplification loop. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Factor D inhibitor 6 (Compound 6; 1-10 mg/kg; Oral gavage; once; C57Bl/6 mice) treatment dosed-ependently inhibits complement activation, with full inhibition at 10 mg/kg. Factor D inhibitor 6 shows sustained inhibition of LPS-induced AP activation for at least 8 h post-dose with an EC 50 of 0.034 μM . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57Bl/6 mice induced by lipopolysaccharide (LPS) Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg Administration: Oral gavage; once Result: Dosed-ependently inhibited complement activation, with full inhibition at 10 mg/kg.

IC50& Target:IC50: 30 nM (Factor D), Kd: 6 nM (Factor D)

Specifications

사양 및 순도

10mM in DMSO

생화학 및 생리적 메커니즘

Factor D inhibitor 6 is a potent, highly selective and orally active factor D (FD) inhibitor with an IC 50 of 30 nM and a K d of 6 nM. Factor D inhibitor 6 is inactive against factor B, lassical and lectin complement-pathway activation, and a broad assay

보관 조건

Store at -80°C

배송

Dry ice packs + Cold packs

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작업 유형

INHIBITOR

이름과 식별자

• 분자량: 484.91