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E6005

Cat. No. M6153
E6005 Structure
Synonym:

RVT-501

Size Price Availability Quantity
5mg USD 110 In stock
10mg USD 180 In stock
50mg USD 600 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Protocol
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 472.49
Formula C26H24N4O5
CAS Number 947620-48-6
Purity >99%
Solubility 100 mg/mL in DMSO
Storage at -20°C
References

Validation of a UPLC-MS/MS method for the simultaneous determination of E6005, a phosphodiesterase 4 inhibitor, and its metabolite in human plasma.
Mano Y, et al. J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Aug 15;998-999:31-9. PMID: 26149248.

Antipruritic effect of the topical phosphodiesterase 4 inhibitor E6005 ameliorates skin lesions in a mouse atopic dermatitis model.
Ishii N, et al. J Pharmacol Exp Ther. 2013 Jul;346(1):105-12. PMID: 23674603.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: E6005, RVT-501 supplier, PDE, inhibitors

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