pde4b2

PF-07038124 HCl is a selective and potent PDE4 inhibitor with an IC50 of 0.5 nM for PDE4B2.PF-07038124 HCl inhibits IL-13, IL-4, and IFNγ, and can be used in the study of skin disorders such as atopic dermatitis and plaque psoriasis.

Roflumilast (APTA 2217) is an orally available, long-acting inhibitor of phosphodiesterase (PDE) type 4 (PDE4), with anti-inflammatory and potential antineoplastic activities. Upon administration, roflumilast and its active metabolite roflumilast N-oxide selectively and competitively bind to and inhibit PDE4, which leads to an increase of both intracellular levels of cyclic-3', 5'-adenosine monophosphate (cAMP) and cAMP-mediated signaling.

ML-030 is a potent and selective inhibitor of PDE4(PDE4A, PDE4A1, PDE4B1, PDE4B2, PDE4C1,and PDE4D2 with IC50 of 6.7 nM, 12.9 nM, 48.2 nM, 37.2 nM, 452 nM and 49.2 nM, respectively)

CI-1044 is an inhibitor of PDE4 (IC50s: 0.29, 0.08, 0.56, 0.09 μM for PDE4A5, PDE4B2, PDE4C2 and PDE4D3).

UK-500001 is a potent PDE4 inhibitor with robust anti-inflammatory activity.

LEO-32731 is a bioactive chemical.

PDE4-IN-8 (Example 5) is a potent Phosphodiesterase 4 (PDE4) inhibitor with an IC50 value of 0.93 nM for PDE4B2. However, it has minimal effects on IL13, IL4, and IFNy, with IC50 values of 4.04 nM, 36.33 nM, and 2394 nM, respectively [1].

PF-07038124 is an inhibitor of PDE4. The IC50 value of PF-07038124 for PDE4B2 is 0.5 nM. PF-07038124 shows inhibitory activities against IFNγ, IL4, and IL-13 with IC50 values of 1.06, 4.1, and 125 nM, respectively [1].

PDE1-IN-4 is a potent and selective inhibitor of PDE1 (phosphodiesterase-1), acting on PDE1C (IC50: 10 nM), PDE1A (IC50: 145 nM) and PDE1B (IC50: 354 nM). PDE1-IN-4 regulates cAMP (3′,5′-cyclic adenosine monophosphate) and cGMP (3′,5′-cyclic guanosine monophosphate) and exhibits antifibrotic effects. PDE1-IN-4 can inhibit TGF-β1-induced differentiation of human lung fibroblasts, and can be used to study idiopathic pulmonary fibrosis (IPF).

PDE4-IN-12 is a potent and safe ubiquitous PDE4 inhibitor with an IC50 of 3.5 nM (SI: 2.71) and also acts on PDE7 with an IC50 of 15 nM (SI: 4.27).

Moexipril-d5 intended for use as an internal standard for the quantification of moexipril by GC- or LC-MS. Moexipril is a prodrug form of the angiotensin converting enzyme (ACE) inhibitor moexiprilat. It is converted to moexiprilat in vivo by side chain ester hydrolysis. Moexipril inhibits ACE in a cell-free assay (IC50 = 2.7 µM for the rabbit enzyme). It also inhibits phosphodiesterase 4 (IC50s = 38, 160, and 230 µM for PDE4B2, PDE4A5 and PDE4D5, respectively). Moexipril (0.1-30 mg kg per day) reduces blood pressure in spontaneously hypertensive rats.1 It also reduces infarct volume in a rat model of focal cerebral ischemia when used at a concentration of 0.01 mg kg.

Moracin M, a phenolic compound found in the skin of Morus alba Linn., effectively inhibits phosphodiesterase-4 (PDE4), exhibiting IC50 values of 2.9 μM and 4.5 μM for PDE4D2 and PDE4B2, respectively, and showing significantly lesser activity on PDE5A1 and PDE9A2 with values over 40 μM and 100 μM, respectively. This compound demonstrates notable anti-inflammatory activity.