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

Nerandomilast dihydrate  (Synonyms: BI 1015550 dihydrate)

Cat. No.: HY-153192A Purity: 99.93%
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Nerandomilast (BI 1015550) dihydrate is an orally active inhibitor of PDE4B with an IC50 value of 7.2 nM. Nerandomilast (dihydrate) has good safety and potential applications in inflammation, allergic diseases, pulmonary fibrosis, and chronic obstructive pulmonary disease (COPD).

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

Nerandomilast dihydrate Chemical Structure

Nerandomilast dihydrate Chemical Structure

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5 mg USD 157 In-stock
10 mg USD 252 In-stock
25 mg USD 480 In-stock
50 mg USD 768 In-stock
100 mg USD 1220 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Nerandomilast dihydrate:

Nerandomilast dihydrate Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

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

In Vitro

Nerandomilast (dihydrate) 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 (dihydrate) 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 dihydrate Related Antibodies
In Vivo

Nerandomilast (dihydrate) (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 (dihydrate) prevents inflammation in rat lung tissue with an ED50 value of 0.1 mg/kg[1].
Nerandomilast (dihydrate) (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 (dihydrate) (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 (dihydrate) (2.5 mg/kg and 12.5 mg/kg; p.o.; twice daily for 6 d) 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 d.
Result: Effectively improved inflammation in lung tissue and reduced the pro-inflammatory factor TNF-α release.
Clinical Trial
Molecular Weight

485.00

Formula

C20H29ClN6O4S
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (51.55 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 2.0619 mL 10.3093 mL 20.6186 mL
5 mM 0.4124 mL 2.0619 mL 4.1237 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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 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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). 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 2.0619 mL 10.3093 mL 20.6186 mL 51.5464 mL
5 mM 0.4124 mL 2.0619 mL 4.1237 mL 10.3093 mL
10 mM 0.2062 mL 1.0309 mL 2.0619 mL 5.1546 mL
15 mM 0.1375 mL 0.6873 mL 1.3746 mL 3.4364 mL
20 mM 0.1031 mL 0.5155 mL 1.0309 mL 2.5773 mL
25 mM 0.0825 mL 0.4124 mL 0.8247 mL 2.0619 mL
30 mM 0.0687 mL 0.3436 mL 0.6873 mL 1.7182 mL
40 mM 0.0515 mL 0.2577 mL 0.5155 mL 1.2887 mL
50 mM 0.0412 mL 0.2062 mL 0.4124 mL 1.0309 mL
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Nerandomilast dihydrate 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:

Nerandomilast dihydrateBI 1015550 dihydratePhosphodiesterase (PDE)RatsMiceLPSTNF-αIL-2PBMCsInhibitorinhibitorinhibit

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