2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. Lotamilast

Lotamilast  (Synonyms: RVT-501; E6005)

Cat. No.: HY-12740 Purity: ≥98.0%
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Lotamilast (RVT-501; E6005) is a selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 2.8 nM.

For research use only. We do not sell to patients.

Lotamilast Chemical Structure

Lotamilast Chemical Structure

CAS No. : 947620-48-6

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 94 In-stock
Solution
10 mM * 1 mL in DMSO USD 94 In-stock
Solid
1 mg USD 50 In-stock
5 mg USD 90 In-stock
10 mg USD 144 In-stock
50 mg USD 430 In-stock
100 mg USD 600 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Lotamilast Related Antibodies

Top Publications Citing Use of Products

View All Phosphodiesterase (PDE) Isoform Specific Products:

View All Isoforms
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Lotamilast (RVT-501; E6005) is a selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 2.8 nM.

IC50 & Target

IC50: 2.8 nM (human PDE4)[1]
In Vitro

Lotamilast 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[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Lotamilast Related Antibodies
In Vivo

Lotamilast is currently in phase 2 development for patients with mild-to-moderate atopic dermatitis. In mice models, the topical application of Lotamilast 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[1]. A single topical application of Lotamilast significantly inhibits spontaneous scratching during 1–2 h after application in mice with chronic dermatitis; the inhibition is partial and similar between 0.01% and 0.03%. Topical application of 0.03% Lotamilast to the rostral back significantly inhibits the increased activity of the cutaneous nerve in mice with chronic dermatitis. The cutaneous concentration of cAMP is significantly decreased in mice with chronic dermatitis, and this decrease is reversed by topical Lotamilast application[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

472.49

Formula

C26H24N4O5
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC=C(C(OC)=O)C=C1)NC2=CC=CC(C3=C4C(C=C(OC)C(OC)=C4)=NC(NC)=N3)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (52.91 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1164 mL 10.5822 mL 21.1645 mL
5 mM 0.4233 mL 2.1164 mL 4.2329 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (5.29 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Kinase Assay
[1]

PDE isoenzyme activities are quantified by measuring the formation of [3H]5′-AMP or [[3H]5′-GMP from [[3H]cAMP or [[3H]cGMP using an enzyme isolated from bovine brain (for PDE1), differentiated U-937 cells (for PDE2), human platelets (for PDE3 and PDE5), and U-937 cells (for PDE4). The test compounds (RVT-501), reference compounds, or vehicle (water) is added to a reaction buffer. The reaction is initialized by addition of the enzyme, and the mixture is incubated for 60 minutes at 22°C. After incubation, the reaction is stopped by heating the plate to 60°C for 3 minutes, after which time scintillation proximity assay beads are added. After 20 minutes of shaking at 22°C, the amount of [[3H]5′-AMP or [[3H]5′-GMP is quantified with a scintillation counters[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice: Lotamilast is applied to the hair-clipped rostral back. Observation of hind-paw scratching and electrophysiological recording of the cutaneous nerve branch are conducted. The effects of topical application of E6005 are evaluated 1 h after application, because topical application of the vehicle elicited hind-paw scratching for 40 min. The cutaneous concentration of cAMP is measured by enzyme immunoassay[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1164 mL 10.5822 mL 21.1645 mL 52.9112 mL
5 mM 0.4233 mL 2.1164 mL 4.2329 mL 10.5822 mL
10 mM 0.2116 mL 1.0582 mL 2.1164 mL 5.2911 mL
15 mM 0.1411 mL 0.7055 mL 1.4110 mL 3.5274 mL
20 mM 0.1058 mL 0.5291 mL 1.0582 mL 2.6456 mL
25 mM 0.0847 mL 0.4233 mL 0.8466 mL 2.1164 mL
30 mM 0.0705 mL 0.3527 mL 0.7055 mL 1.7637 mL
40 mM 0.0529 mL 0.2646 mL 0.5291 mL 1.3228 mL
50 mM 0.0423 mL 0.2116 mL 0.4233 mL 1.0582 mL
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Lotamilast Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lotamilast947620-48-6RVT-501 E6005RVT501RVT 501E6005E 6005E-6005Phosphodiesterase (PDE)Inhibitorinhibitorinhibit

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