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Cat. No.: HY-201403

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LY2775240

LY2775240 is an orally active phosphodiesterase 4 (PDE4) inhibitor with potent inhibitory activity against PDE4A (IC₅₀ = 0.09 nM), PDE4B (IC₅₀ = 0.09 nM) and PDE4D (IC₅₀ = 0.14 nM), and exhibits an IC₅₀ of 2.4 nM against PDE4C. LY2775240 is a highly selective agent that reduces TNFα production upon immune activation. LY2775240 decreases TNFα production in rodent and rhesus monkey models. LY2775240 can be used in the research of psoriasis.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

CAS No.: 1628160-15-5
Formule: C₂₆H₃₅N₃O₆
Masse moléculaire:485.58

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (271 KB)

LY2775240 Chemical Structure

CAS No.: 1628160-15-5

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

PDE4A

0.09 nM (IC₅₀)

PDE4B

0.09
nM (IC₅₀)

PDE4D

0.14 nM (IC₅₀)

PDE4C

2.4 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform Phosphodiesterase (PDE) :

Voir tous les produits spécifiques à Isoform TNF Receptor :

In Vitro

LY2775240 potently inhibits LPS (HY-D1056)-stimulated TNFα secretion in human whole blood with an IC₅₀ of 18 nM^[1].

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

In Vivo

LY2775240 (3-10 mg/kg; p.o.; single dose) significantly reduces LPS-induced TNFα production in mice^[1].

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

Animal Model:

C57Bl/6 (female, 8–10 weeks old, LPS-induced)^[1]
Dosage:

3 mg/kg; 10 mg/kg
Administration:

p.o.; single dose
Result:

Reduced plasma TNFα to 53% of vehicle control at 3 mg/kg; reduced plasma TNFα to 35% of vehicle control at 10 mg/kg.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1628160-15-5
Masse moléculaire 485.58
Formule C₂₆H₃₅N₃O₆
SMILES

[C@H](C)(O)[C@@]1(C)[C@@H](CN(C([C@H](CO)O)=O)C1)C2=CC(OC3CN(C3)C4=CC=C(C)C=N4)=C(OC)C=C2
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (271 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Patel DR, et al. Characterization of LY2775240, a selective phosphodiesterase-4 inhibitor, in nonclinical models and in healthy subjects. Clin Transl Sci. 2021;14(3):1037-1048. [Content Brief]

Calculators

Calculateur de molarité

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Calculateur de dilution

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Pureté et documentation
Références

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LY2775240

Voir tous les produits spécifiques à Isoform Phosphodiesterase (PDE)

Voir tous les produits spécifiques à Isoform TNF Receptor

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

LY2775240 Related Classifications

HY-201403 Related Classifications