インテグラーゼ

シグナル伝達経路

研究分野

  • 阻害剤の選択性比較
  • 溶解度
カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S2005 Raltegravir (MK-0518) <1 mg/mL 88 mg/mL <1 mg/mL
S2001 Elvitegravir (GS-9137, JTK-303) <1 mg/mL 89 mg/mL 35 mg/mL
S2667 Dolutegravir (GSK1349572) <1 mg/mL 83 mg/mL <1 mg/mL
S1366 BMS-707035 <1 mg/mL 38 mg/mL <1 mg/mL
S2765 MK-2048 <1 mg/mL 9 mg/mL <1 mg/mL
S5245 Raltegravir potassium <1 mg/mL 96 mg/mL 10 mg/mL
S7766 Cabotegravir (GSK744, GSK1265744) <1 mg/mL 38 mg/mL <1 mg/mL
S4642 Dolutegravir Sodium <1 mg/mL 0.2 mg/mL <1 mg/mL
S4187 Salicylanilide <1 mg/mL 43 mg/mL 18 mg/mL
製品コード 製品説明 文献中の使用例 お客様のフィードバック
S2005

Raltegravir (MK-0518)

Raltegravir (MK-0518) is a potent integrase (IN) inhibitor for WT and S217Q PFV IN with IC50 of 90 nM and 40 nM in cell-free assays, respectively. It shows greater than 1000-fold selectivity for HIV-1 IN over several related Mg2+-dependent enzyme such as HCV polymerase, HIV reverse transcriptase, HIV RNaseH and human α-, β-, γ-polymerases.

S2001

Elvitegravir (GS-9137, JTK-303)

Elvitegravir (GS-9137, JTK-303) is an HIV integrase inhibitor for HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM in cell-free assays, respectively.

S2667

Dolutegravir (GSK1349572)

Dolutegravir (GSK1349572) is a two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM in a cell-free assay, modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H.

S1366

BMS-707035

BMS-707035 is a specific HIV-I integrase (IN) inhibitor with IC50 of 15 nM. Phase 2.

S2765

MK-2048

MK-2048 is a potent inhibitor of integrase (IN) and INR263K with IC50 of 2.6 nM and 1.5 nM, respectively.

S5245

Raltegravir potassium

Raltegravir Potassium is the orally bioavailable potassium salt of raltegravir, the first approved human immunodeficiency virus type 1 (HIV-1) integrase inhibitor.

S7766

Cabotegravir (GSK744, GSK1265744)

Cabotegravir (GSK744, GSK1265744) is a long-acting HIV integrase inhibitor against a broad range of HIV subtypes, and inhibits the HIV-1 integrase catalyzed strand transfer reaction with IC50 of 3.0 nM. Phase 2.

S4642

Dolutegravir Sodium

Dolutegravir is a HIV integrase inhibitor with IC50 of 2.7 nM.

S4187

Salicylanilide

Salicylanilides are a group of compounds with a wide range of biological activities including antiviral potency, antibacterial (including antimycobacterial) and antifungal activities.

Tags: Integrase activity | Integrase inhibitors mechanism | HIV Integrase inhibitor mechanism | Integrase assay | HIV Integrase assay | Integrase inhibitor drugs | HIV Integrase inhibitor drugs | Integrase inhibitor resistance testing | Integrase inhibitor review