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Cat. No.: HY-183463

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D 22888

D 22888 is an orally active PDE4 inhibitor, with human PDE4 IC₅₀ of 0.153 μM, and selectivity over PDE3 and PDE5. D 22888 elevates intracellular cAMP levels to modulate target cell functions. D 22888 acts as a relaxant of human bronchial ring inherent tone. D 22888 inhibits opsonized zymosan-induced superoxide anion generation by human eosinophils. D 22888 reduces bronchoalveolar lavage eosinophil numbers in allergen-challenged sensitized guinea pigs via single or chronic oral dosing. D 22888 can be used for the research of bronchial asthma.

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CAS No.: 182282-60-6
화학식: C₁₆H₂₀N₄O₂
분자량:300.36

보관:

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

Data Sheet (286 KB)

D 22888 Chemical Structure

CAS No.: 182282-60-6

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Use of MCE Products

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[1]

PDE4

0.153 μM (IC₅₀)

All Phosphodiesterase (PDE) Isoforms :

In Vitro

OthersLocal Vascular RegulationOxidative Stress

Others

D-22888 potently and selectively inhibits human PMNL PDE4 with an IC₅₀ of 153 nM, exhibiting much weaker inhibition of human platelet PDE3 and PDE5^[1].

Local Vascular Regulation

D-22888 (up to 10 μM; equilibration for each concentration until response stabilized) has minimal effect on PGF₂α-induced tone in human pulmonary artery rings at concentrations up to 10 μM^[1].

Oxidative Stress

D-22888 (1-10 μM; 5 min pre-incubation, followed by 30 min incubation with opsonized zymosan (OZ)) inhibits opsonized zymosan-induced superoxide anion generation in human eosinophils in a concentration-dependent manner with an IC₅₀ of 3.1 μM^[1].

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

In Vivo

Innate Immunity

D-22888 (10-30 mg/kg; p.o.; single dose 2 h pre-challenge, single dose 4 h post-challenge, twice daily for 3 days) dose-dependently inhibits allergen-induced bronchoalveolar eosinophilia in actively sensitized guinea pigs, with up to 88% inhibition observed with 30 mg/kg twice daily for 3 days^[1].

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

Animal Model:

Dunkin-Hartley (male, 200-250 g, actively sensitized with two subcutaneous injections of 10 μg ovalbumin + 1 mg Al(OH)₃ 14 days apart, challenged with ovalbumin aerosol 7 days after the second injection)^[1]
Dosage:

10 mg/kg (pre-challenge single dose); 30 mg/kg (pre-challenge single dose); 30 mg/kg (post-challenge single dose); 30 mg/kg (twice daily for 3 days)
Administration:

p.o. (single dose 2 h pre-challenge); p.o. (single dose 4 h post-challenge); p.o. (twice daily for 3 days, last dose 2 h pre-challenge)
Result:

Reduced allergen-induced bronchoalveolar lavage eosinophilia by 48%.
Reduced allergen-induced bronchoalveolar lavage eosinophilia by 73%.
Reduced allergen-induced bronchoalveolar lavage eosinophilia by 68%.
Reduced allergen-induced bronchoalveolar lavage eosinophilia by 88%.

Chemical Information

CAS No. 182282-60-6
분자량 300.36
화학식 C₁₆H₂₀N₄O₂
SMILES

O=C1C2=C(C)N=C(CC)N2C3=NC(OC)=CC=C3N1CCC
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 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)
Handling Instructions (2659 KB)

References

[1]. Dent G, et al. Effects of a selective PDE4 inhibitor, D-22888, on human airways and eosinophils in vitro and late phase allergic pulmonary eosinophilia in guinea pigs. Pulmonary pharmacology & therapeutics. 1998 Feb;11(1):13-21.

Calculators

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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