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

Nerandomilast  (Synonyms: BI 1015550)

Art. -Nr.: HY-153192 Reinheit: 99.99%
COA
SDS
Handling Instructions Technical Support

Nerandomilast (BI 1015550) is an orally active inhibitor of PDE4B with an IC50 value of 7.2 nM. Nerandomilast has good safety and potential applications in inflammation, allergic diseases, pulmonary fibrosis, and chronic obstructive pulmonary disease (COPD).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Nerandomilast

Nerandomilast Chemische Struktur

CAS. Nr. : 1423719-30-5

Größe Preis Verfügbarkeit Menge
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 Auf Lager
Solution
10 mM * 1 mL in DMSO Auf Lager
Solid
1 mg Auf Lager
5 mg Auf Lager
10 mg Auf Lager
25 mg Auf Lager
50 mg Auf Lager
100 mg Auf Lager
200 mg   Angebot einholen  
500 mg   Angebot einholen  

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

This product is a controlled substance and not for sale in your territory.

Kundenbewertung

Based on 2 publication(s) in Google Scholar

Other Forms of Nerandomilast:

Nerandomilast Related Antibodies

Top Publications Citing Use of Products

Alle Phosphodiesterase (PDE) Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

  • Biologische Aktivität

  • Reinheit & Dokumentation

  • Verweise

  • Kundenbewertung

Beschreibung

Nerandomilast (BI 1015550) is an orally active inhibitor of PDE4B with an IC50 value of 7.2 nM. Nerandomilast has good safety and potential applications in inflammation, allergic diseases, pulmonary fibrosis, and chronic obstructive pulmonary disease (COPD)[1][2].

In Vitro

Nerandomilast inhibits Lipopolysaccharides (HY-D1056) induced TNF-α release and Phytohemagglutinin P (HY-N7038A) induced IL-2 release in human PBMCs with IC50 values of 35 nM and 9 nM, respectively[2].
Nerandomilast inhibits TNF-α release in rat whole blood with an IC50 value of 91 nM[2].

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

Nerandomilast Related Antibodies
In Vivo

Nerandomilast (Example 2) (0, 0.3, 1.0 and 3.0 mg/kg; p.o.; single dose) weakens intestinal transport in rats at 1.0 mg/kg without significantly affecting body weight[1].
Nerandomilast prevents inflammation in rat lung tissue with an ED50 value of 0.1 mg/kg[1].
Nerandomilast (0.01, 0.1 and 1.0 mg/kg; p.o.; single dose) reduces the Lipopolysaccharides (HY-D1056) induced TNF-α release with dose-dependent manner in mice plasma[2].
Nerandomilast (0.1, 0.3 and 1.0 mg/kg; p.o.; single dose) inhibits lipopolysaccharides induced neutrophil entry into bronchoalveolar lavage fluid of male Suncus Murinus and Wistar rats[2].
Nerandomilast (2.5 mg/kg and 12.5 mg/kg; p.o.; twice daily for 6 days) effectively improves the damage of Bleomycin (HY-108345) to mice[2].

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

Animal Model: Rats[1].
Dosage: 0, 0.3, 1.0 and 3.0 mg/kg.
Administration: Oral gavage; single dose.
Result: Had minimal toxic and side effects on the intestines and stomach of rats, demonstrating biosafety.
Animal Model: Male Suncus Murinus and Wistar rats; mice[2].
Dosage: 0.01, 0.1, 0.3, 1.0, 2.5 or 12.5 mg/kg.
Administration: Oral gavage; single dose or twice daily for 6 days.
Result: Effectively improved inflammation in lung tissue and reduced the pro-inflammatory factor TNF-α release.
Molekulargewicht

448.97

Formel

C20H25ClN6O2S
CAS. Nr.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=[S@]1C2=C(CC1)N=C(N3CCC(CC3)C4=NC=C(C=N4)Cl)N=C2NC5(CO)CCC5
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 6.67 mg/mL (14.86 mM; ultrasonic and warming and heat to 60°C; 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 2.2273 mL 11.1366 mL 22.2732 mL
5 mM 0.4455 mL 2.2273 mL 4.4546 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molaritätsrechner

  • Verdünnungsrechner

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 0.67 mg/mL (1.49 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 0.67 mg/mL (1.49 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 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.
Reinheit & Dokumentation

Purity: 99.99%

SDS (557 KB)

COA (256 KB)

Handling Instructions (2659 KB)
Verweise

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2273 mL 11.1366 mL 22.2732 mL 55.6830 mL
5 mM 0.4455 mL 2.2273 mL 4.4546 mL 11.1366 mL
10 mM 0.2227 mL 1.1137 mL 2.2273 mL 5.5683 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Nerandomilast 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:

Nerandomilast1423719-30-5BI 1015550BI1015550BI-1015550Phosphodiesterase (PDE)RatsMiceLPSTNF-αIL-2PBMCsInhibitorinhibitorinhibit

Ihre kürzlich angesehenen Produkte:

Online-Anfrage

Your information is safe with us. * Required Fields.

Produktname

  

Requested Quantity *

Name des Antragstellers *

 

Anrede

E-Mail-Addresse *

 

Telefonnummer *

Department

 

Name der Organisation *

City

Bundesland

Country or Region *

      

Bemerkungen

Massenanfrage

Inquiry Information

Produktname:
Nerandomilast
Art. -Nr.:
HY-153192
Menge:
MCE Japan Authorized Agent:

Kundenbewertung

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Produktname

  

Lot #

Name des Antragstellers *

 

E-Mail-Addresse *

Telefonnummer

 

Department *

Name der Organisation *

 

Country or Region *

Bemerkungen

SAFETY DATA SHEET (SDS)

English - EN (557 KB) Français - FR (557 KB) Deutsch - DE (557 KB) Norwegian - NO (557 KB) Español - ES (557 KB) Swedish - SV (557 KB) Italian - IT (557 KB) Korean - KR (557 KB) Portuguese - PT (557 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.