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 | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| 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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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|---|
| ME-3183
ME-3183 is an oral selective PDE4 inhibitor with anti-inflammatory activity for studies related to plaque psoriasis. |
| ART-648
ART-648 is a PDE4 inhibitor that may be used in studies related to non-alcoholic steatohepatitis. |
| (E/Z)-HA155
(E/Z)-HA155 is a potent Autotaxin (ATX) type I inhibitor for studies related to cancer, fibrous disorders, inflammation, pain and angiogenesis. |
| Autotaxin-IN-3
Autotaxin-IN-3 is an Autotaxin(ATX) inhibitor with an IC50 value of 2.4 nM. |
| HA155
HA155 is a potent and selective ATX inhibitor with an IC50 value of 5.7 nM. |
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