All AbMole products are for research use only, cannot be used for human consumption.
In vitro: RVT-501 potently and selectively inhibits human PDE4 activity with an IC50 of 2.8 nM and suppresses the production of various cytokines from human lymphocytes and monocytes with IC50 values ranging from 0.49 to 3.1 nM.
In vivo: RVT-501 is currently in phase 2 development for patients with mild-to-moderate atopic dermatitis. In mice models, the topical application of RVT-501 produces an immediate antipruritic effect as well as an anti-inflammatory effect with reduced expression of cytokines/adhesion molecules. On the basis of these observed effects, topical RVT-501 ameliorates the appearance of atopic dermatitis-like skin lesions in two types of AD models, hapten- and mite-elicited models, exhibiting inhibitory effects comparable to that of tacrolimus.
| Cell Experiment | |
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| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
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| Animal models | NC/Nga mice |
| Formulation | 4% SDS solution |
| Dosages | 10 μl/g |
| Administration | s.c. |
| Molecular Weight | 472.49 |
| Formula | C26H24N4O5 |
| CAS Number | 947620-48-6 |
| Solubility (25°C) | 100 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PDE Products |
|---|
| MR-L2
MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4), activates representative PDE4 long-isoform variants (PDE4A4, PDE4B1, PDE4C3, PDE4D5). MR-L2 suppresses PGE2-induced MDCK cell cyst formation with an EC50 of 1.2 μM. |
| MMPX
MMPX is a potent PDE1 inhibitor. |
| T-0156
T-0156 is a potent and selective phosphodiesterase type 5 (PDE5) inhibitor. |
| TPN171
TPN171 is a potent, selective and oral bioavailable inhibitor of phosphodiesterase type 5 (PDE5) with an IC50 of 0.62 nM, being developed for the treatment of pulmonary arterial hypertension (PAH). |
| Mesopram
Mesopram (Daxalipram) is an orally active phosphodiesterase (PDE) 4 inhibitor. |
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Products are for research use only. Not for human use. We do not sell to patients.
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