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Cat. No. Product Name CAS No. Information
PC-61846

PF 5212372

916136-25-9

PF 5212372 (PLA-950, ZPL-521, ZPL 5212372) is a potent, selective inhibitor of cPLA2 (cytosolic phospholipase A2α) with IC50 of 7 nM; inhibits PGD2 and cysteinyl leukotriene release from anti-IgE-stimulated human lung mast cells with IC50 of 0.29 and 0.45 nM, respectively; inhibits ionomycin-stimulated release of leukotriene B(4), thromboxane A(2), and PGD(2) (IC50 2.6, 2.6, and 4.0 nM, respectively); significantly inhibits AMP-induced contraction of human bronchi.

Dermatitis

Phase 2 Clinical

PC-61387

Lotamilast

947620-48-6

Lotamilast (RVT 501, E6005) is a potent, selective PDE4 inhibitor with IC50 of 2.8 nM, suppresses the production of various cytokines from human lymphocytes and monocytes with IC50 of 0.49-3.1 nM; produces an immediate antipruritic effect as well as an anti-inflammatory effect with reduced expression of cytokines/adhesion molecules in mice after topical application; ameliorates the appearance of atopic dermatitis-like skin lesions in AD models.

Dermatitis

Phase 2 Clinical

PC-61372

Difamilast

937782-05-3

Difamilast (OPA-15406) is a novel potent, selective phosphodiesterase IV (PDE4) inhibitor with preference for PDE4B (IC50=11.2 nM). 

Dermatitis

Phase 2 Clinical

PC-60671

PF-04965842

1622902-68-4

PF-04965842(PF04965842) is a potent, selective, orally bioavailable JAK1 inhibitor with IC50 of 29 nM; exhibits good selective inhibition profile for JAK1 versus other JAK family enzymes (IC50=803/>10,000/1250 nM for JAK2/JAK3/TYK2, respectively); demonstrates efficacy in a rat adjuvant-induced arthritis (rAIA) model.

Dermatitis

Phase 3 Clinical

PC-43202

Asivatrep

1005168-10-4 Asivatrep (PAC-14028) is a potent, selective TRPV1 antagonist with IC50 of 55 nM against capsaicin-induced Ca2+ influx in rat DRG neurons, does not inhibit or activate other TRP channels such as hTRPV2, hTRPV3, hTRPM8 and hTRPA1; inhibits capsaicin-evoked calcium influx in keratinocytes at sub-micromolar concentrations, blocks capsaicin-induced blood perfusion increase, and the accelerated barrier recovery from tape-stripping-induced barrier damages in hairless mice, also attenuates dermatitis-associated barrier damages in Df and OXZ models.

Dermatitis

Phase 3 Clinical

PC-61567

PF-3893787

943057-12-3 PF-3893787 (ZPL 3893787) is a potent and selective H4 receptor antagonist with binding Ki of 2.4 nM; has an IC50 of 1.16 nM on human native isolated eosinophils assessing actin polymerisation; exhibits anti-inflammatory activity.

Dermatitis

Phase 2 Clinical

PC-42760

AN-2728

906673-24-3 A potent PDE4 inhibitor with IC50 of 0.49 uM; also shows inhibition against PDE1A3, PDE3Cat, and PDE7A1; suppresses the release of TNFalpha, IL-12, IL-23 and other cytokines.

Dermatitis

Phase 2 Clinical

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