pde4b2

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.

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

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.

PDE4B-IN-5 (compound 84) is a PDE4B inhibitor with an IC50 value of less than 10 nM, and it exhibits anti-inflammatory properties.

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).

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.

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)

PDE4-IN-29 (Compound 55) is an orally active and selective inhibitor of PDE4, targeting subtypes such as PDE4A1, PDE4B2, and PDE4D3, with an IC50 value for PDE4D3 of less than 5 nM. It inhibits the degradation of cyclic adenosine monophosphate (cAMP), elevating intracellular cAMP levels and suppressing the release of inflammatory mediators like TNF-α. PDE4-IN-29 holds potential for research in inflammatory diseases such as psoriasis, atopic dermatitis, and chronic obstructive pulmonary disease.

LH17 is a derivative of Kaempferol and serves as a potent and selective inhibitor of PDE4, with PDE4D2 IC50 at 73 nM and PDE4B2 IC50 at 190 nM. It demonstrates over 136-fold selectivity against other PDE isoenzymes (PDE1B/2A/3A/5A/8A/9A/10A) with IC50s greater than 10000 nM, except for PDE7A1 which has an IC50 of 300 nM. LH17 exhibits unique interactions with the M pocket of PDE4. In vitro and in vivo models show that LH17 has significant antifibrotic effects. This compound is applicable in the study of idiopathic pulmonary fibrosis (IPF).

PDE4/5-IN-1 is a selective dual inhibitor of phosphodiesterase 4/5 (PDE4/5). It functionally inhibits the activities of PDE5, PDE4B2, and PDE4D2. Additionally, PDE4/5-IN-1 relaxes isolated rat prostate tissue, enhances nitric oxide-induced relaxation of isolated rat prostate tissue, and reduces α-1 adrenergic receptor-mediated contraction responses in isolated rat prostate tissue. This compound also inhibits the proliferation of human hyperplastic prostate cells and can be used in research related to benign prostatic hyperplasia.

Moexipril-D5 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 (T63377) 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 (T63377) (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.