PDE4 选择性抑制剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S2620 GSK256066

GSK256066是一种选择性的PDE4B(与A-D亚型具有相等的亲和力)抑制剂,IC50为3.2 pM,比作用于PDE1/2/3/5/6选择性高380,000倍以上,作用于PDE4B比作用于PDE7选择性高2500倍以上。Phase 2。

Selective PDE4B, IC50: 3.2 pM
S2131 Roflumilast (B9302-107)

Roflumilast 是一种选择性的PDE4抑制剂,无细胞试验中IC50为0.2-4.3 nM。

Selective PDE4C2, IC50: 4.3 nM; PDE4C1, IC50: 3 nM; PDE4B2, IC50: 0.2 nM; PDE4B1, IC50: 0.7 nM; PDE4A4, IC50: 0.9 nM; PDE4A1, IC50: 0.7 nM
S0127 CP-671305

CP671305 is a potent, selective and orally active inhibitor of phosphodiesterase-4-D with high activities.

Selective PDE4-D, IC50: 3 nM
S6844 BPN14770

BPN14770 is a selective allosteric inhibitor of phosphodiesterase 4D (PDE4D) with IC50 of 7.8 nM and 7.4 nM for PDE4D7 and PDE4D3, respectively.

Selective PDE4D3, IC50: 7.4 nM; PDE4D7, IC50: 7.8 nM
S8034 Apremilast (CC-10004)

Apremilast (CC-10004)是一种口服生物有效的PDE4TNF-α抑制剂,IC50分别为74 nM和77 nM。

Selective PDE4, IC50: 74 nM
S1455 Cilomilast

Cilomilast是一种有效的PDE4抑制剂,IC50为110 nM,具有抗炎活性和弱的中枢神经系统活性。Phase 3。

Selective HPDE4, IC50: 120 nM; LPDE4, IC50: 100 nM
S1430 Rolipram (ZK-62711)

PDE4的选择性抑制剂,rolipram,抑制免疫纯化的PDE4BPDE4D活性,IC50分别为130 nM和240 nM。具有抗炎活性。

Selective PDE4B, IC50: 130 nM
S2127 S-(+)-Rolipram

S- (+)-Rolipram抑制人体单核细胞环AMP特异性的PDE4IC50为0.75 μM,作用于中枢神经系统,具有消炎和抗抑郁活性,比其R-对映体作用效果稍弱。

Selective PDE4, IC50: 0.75 μM
S5014 Crisaborole (AN2728)

Crisaborole (AN2728) is a small-molecule, boron-based, selective PDE4 inhibitor and has broad-spectrum anti-inflammatory activity.

Selective
S4837 Ibudilast

Ibudilast (KC-404, AV411, MN166) is a relatively non-selective phosphodiesterase inhibitor with anti-inflammatory and neuroprotective activities.

Pan PDE4, IC50: 0.08 μM
S2320 Luteolin

Luteolin是一种非选择性的PDE抑制剂,作用于PDE1-5Ki分别为15.0 μM, 6.4 μM, 13.9 μM, 11.1 μM和9.5 μM。Phase 2.

Pan PDE4, Ki: 11.1 μM
S5836 IBMX

IBMX (Isobutylmethylxanthine, 1-Methyl-3-Isobutylxanthine) is a nonspecific inhibitor of phosphodiesterase (PDE) with IC50 values of 6.5±1.2, 26.3±3.9 and 31.7±5.3 μM for PDE3, 4 and 5 respectively. It may enhance the intracellular cAMP levels and also acts as an adenosine (A1) receptor antagonist.

Pan PDE4, IC50: 26.3 μM
S4090 Fenspiride HCl

Fenspiride是一种支气管扩张剂,具有抗炎特性,作用于人离体的支气管,抑制磷酸二酯酶4和磷酸二酯酶3活性,logIC50值分别为4.16和3.44。

Pan PDE4, pIC50: 4.16