AWD12−281

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Hodoodo CAT#: H555101

CAS#: 257892-33-4 (free)

Description: AWD 12-281 is a selective phosphodiesterase 4 (PDE4) inhibitor for the treatment of lung inflammation using inhalative administration. AWD 12-281 Is Active in a New Guinea-Pig Model of Allergic Skin Inflammation Predictive of Human Skin Penetration and Suppresses Both Th1 and Th2 Cytokines in Mice. AWD 12-281 is a very promising drug candidate not only for the treatment of lung inflammation using inhalative administration but also for the treatment of atopic dermatitis.


Chemical Structure

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AWD12−281
CAS# 257892-33-4 (free)

Theoretical Analysis

Hodoodo Cat#: H555101
Name: AWD12−281
CAS#: 257892-33-4 (free)
Chemical Formula: C22H13Cl2FN2O3
Exact Mass: 442.03
Molecular Weight: 443.255
Elemental Analysis: C, 59.61; H, 2.96; Cl, 16.00; F, 4.29; N, 6.32; O, 10.83

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @hodoodo.com or click below button.
Note: Price will be listed if it is available in the future.

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Related CAS #: 247584-21-0 (sodium)   257892-33-4 (free)    

Synonym: AWD 12-281; AWD12-281; AWD-12-281; AWD 12281; AWD12281; AWD-12281; GSK 842470; GSK 842470; GSK-842470.

IUPAC/Chemical Name: 1-(3,5-dichloropyridin-4-yl)-2-(1-(4-fluorobenzyl)-5-hydroxy-1H-indol-3-yl)ethane-1,2-dione

InChi Key: DNDXMIVKQRLJGL-UHFFFAOYSA-N

InChi Code: InChI=1S/C22H13Cl2FN2O3/c23-17-8-26-9-18(24)20(17)22(30)21(29)16-11-27(10-12-1-3-13(25)4-2-12)19-6-5-14(28)7-15(16)19/h1-9,11,28H,10H2

SMILES Code: OC1=CC=C2C(C(C(C(C3=C(Cl)C=NC=C3Cl)=O)=O)=CN2CC4=CC=C(F)C=C4)=C1

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 443.26 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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This message contains search results from the National Center for Biotechnology Information (NCBI) at the U.S. National Library of Medicine (NLM). Do not reply directly to this message

Sent On: Fri Jun 12 15:54:25 2020

12 selected items


PubMed Results
Items 1-12 of 12 (Display the 12 citations in PubMed)

1: Giembycz MA. Can the anti-inflammatory potential of PDE4 inhibitors be realized: guarded optimism or wishful thinking? Br J Pharmacol. 2008 Oct;155(3):288-90. doi: 10.1038/bjp.2008.297. Epub 2008 Jul 28. PMID: 18660832; PMCID: PMC2567889.


2: Bäumer W, Hoppmann J, Rundfeldt C, Kietzmann M. Highly selective phosphodiesterase 4 inhibitors for the treatment of allergic skin diseases and psoriasis. Inflamm Allergy Drug Targets. 2007 Mar;6(1):17-26. doi: 10.2174/187152807780077318. PMID: 17352685.


3: Hoppmann J, Bäumer W, Galetzka C, Höfgen N, Kietzmann M, Rundfeldt C. The phosphodiesterase 4 inhibitor AWD 12-281 is active in a new guinea-pig model of allergic skin inflammation predictive of human skin penetration and suppresses both Th1 and Th2 cytokines in mice. J Pharm Pharmacol. 2005 Dec;57(12):1609-17. doi: 10.1211/jpp.57.12.0011. PMID: 16354405.


4: Gutke HJ, Guse JH, Khobzaoui M, Renukappa-Gutke T, Burnet M. AWD-12-281 (inhaled) (elbion/GlaxoSmithKline). Curr Opin Investig Drugs. 2005 Nov;6(11):1149-58. PMID: 16312137.


5: Soto FJ, Hanania NA. Selective phosphodiesterase-4 inhibitors in chronic obstructive lung disease. Curr Opin Pulm Med. 2005 Mar;11(2):129-34. doi: 10.1097/01.mcp.0000151715.58124.9e. PMID: 15699784.


6: Draheim R, Egerland U, Rundfeldt C. Anti-inflammatory potential of the selective phosphodiesterase 4 inhibitor N-(3,5-dichloro- pyrid-4-yl)-[1-(4-fluorobenzyl)-5-hydroxy-indole-3-yl]-glyoxylic acid amide (AWD 12-281), in human cell preparations. J Pharmacol Exp Ther. 2004 Feb;308(2):555-63. doi: 10.1124/jpet.103.059097. Epub 2003 Nov 10. PMID: 14610230.


7: Crocker IC, Townley RG. Therapeutic potential of phosphodiesterase 4 inhibitors in allergic diseases. Drugs Today (Barc). 1999 Jul;35(7):519-35. doi: 10.1358/dot.1999.35.7.548265. PMID: 12973397.


8: Bäumer W, Gorr G, Hoppmann J, Ehinger AM, Rundfeldt C, Kietzmann M. AWD 12-281, a highly selective phosphodiesterase 4 inhibitor, is effective in the prevention and treatment of inflammatory reactions in a model of allergic dermatitis. J Pharm Pharmacol. 2003 Aug;55(8):1107-14. doi: 10.1211/0022357021585. PMID: 12956900.


9: Kuss H, Hoefgen N, Johanssen S, Kronbach T, Rundfeldt C. In vivo efficacy in airway disease models of N-(3,5-dichloropyrid-4-yl)-[1-(4-fluorobenzyl)-5-hydroxy-indole-3-yl]-glyoxylic acid amide (AWD 12-281), a selective phosphodiesterase 4 inhibitor for inhaled administration. J Pharmacol Exp Ther. 2003 Oct;307(1):373-85. doi: 10.1124/jpet.103.053942. Epub 2003 Aug 27. PMID: 12944497.


10: Bäumer W, Gorr G, Hoppmann J, Ehinger AM, Ehinger B, Kietzmann M. Effects of the phosphodiesterase 4 inhibitors SB 207499 and AWD 12-281 on the inflammatory reaction in a model of allergic dermatitis. Eur J Pharmacol. 2002 Jun 20;446(1-3):195-200. doi: 10.1016/s0014-2999(02)01810-1. PMID: 12098602.


11: Ezeamuzie CI. Requirement of additional adenylate cyclase activation for the inhibition of human eosinophil degranulation by phosphodiesterase IV inhibitors. Eur J Pharmacol. 2001 Apr 6;417(1-2):11-8. doi: 10.1016/s0014-2999(01)00821-4. PMID: 11301054.


12: Schmidt DT, Watson N, Dent G, Rühlmann E, Branscheid D, Magnussen H, Rabe KF. The effect of selective and non-selective phosphodiesterase inhibitors on allergen- and leukotriene C(4)-induced contractions in passively sensitized human airways. Br J Pharmacol. 2000 Dec;131(8):1607-18. doi: 10.1038/sj.bjp.0703725. PMID: 11139438; PMCID: PMC1572487.