Cipamfylline | CAS# 132210-43-6 | Potent and selective inhibitor of PDE-4, Antiviral

Cipamfylline
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 412939

CAS#: 132210-43-6

Description: Cipamfylline is a xanthine, a theophylline analogue, and is a potent and selective inhibitor of phosphodiesterase type 4 (PDE-4). Cipamfylline was tested in patients with a diagnosis of atopic dermatitis and in two human models of acute and chronic irritant contact dermatitis. The outcome of the study revealed that cipamfylline was more effective than vehicle in treating atopic dermatitis, but less effective than a group II steroid, hydrocortisone-17-butyrate both in the treatment of atopic dermatitis and irritant contact dermatitis. The absorption of cipamfylline and the subsequent systemic exposure might be the reason why further clinical studies with higher doses of cipamfylline have not been published.

Chemical Structure

Cipamfylline

CAS# 132210-43-6

Instruction

Theoretical Analysis

MedKoo Cat#: 412939
Name: Cipamfylline
CAS#: 132210-43-6
Chemical Formula: C13H17N5O2
Exact Mass: 275.14
Molecular Weight: 275.310
Elemental Analysis: C, 56.71; H, 6.22; N, 25.44; O, 11.62

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 650	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: Cipamfylline; BRL61063; BRL-61063; BRL 61063

IUPAC/Chemical Name: 1H-Purine-2,6-dione, 8-amino-1,3-bis(cyclopropylmethyl)-3,7-dihydro-

InChi Key: KSPYMJJKQMWWNB-UHFFFAOYSA-N

InChi Code: InChI=1S/C13H17N5O2/c14-12-15-9-10(16-12)17(5-7-1-2-7)13(20)18(11(9)19)6-8-3-4-8/h7-8H,1-6H2,(H3,14,15,16)

SMILES Code: O=C(N1CC2CC2)N(CC3CC3)C4=C(NC(N)=N4)C1=O

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:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 275.31 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.

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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1: Griffiths CE, Van Leent EJ, Gilbert M, Traulsen J; Cipamyflline Study Group. Randomized comparison of the type 4 phosphodiesterase inhibitor cipamfylline cream, cream vehicle and hydrocortisone 17-butyrate cream for the treatment of atopic dermatitis. Br J Dermatol. 2002 Aug;147(2):299-307. doi: 10.1046/j.1365-2133.2002.04894.x. PMID: 12174103.

2: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 Apr;25(3):225-48. PMID: 12743628.

3: Kucharekova M, Hornix M, Ashikaga T, T'kint S, de Jongh GJ, Schalkwijk J, van de Kerkhof PC, van der Valk PG. The effect of the PDE-4 inhibitor (cipamfylline) in two human models of irritant contact dermatitis. Arch Dermatol Res. 2003 Apr;295(1):29-32. doi: 10.1007/s00403-003-0389-4. Epub 2003 Mar 4. PMID: 12709818.

4: Nankervis H, Thomas KS, Delamere FM, Barbarot S, Rogers NK, Williams HC. Scoping systematic review of treatments for eczema. Southampton (UK): NIHR Journals Library; 2016 May. PMID: 27280278.

5: Bayes M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 May;25(4):317-40. PMID: 12808477.

6: 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.

7: Hiyama H, Arichika N, Okada M, Koyama N, Tahara T, Haruta J. Pharmacological Profile of Difamilast, a Novel Selective Phosphodiesterase 4 Inhibitor, for Topical Treatment of Atopic Dermatitis. J Pharmacol Exp Ther. 2023 Jul;386(1):45-55. doi: 10.1124/jpet.123.001609. Epub 2023 Apr 11. PMID: 37041087.

8: Cramer RD, Jilek RJ, Andrews KM. Dbtop: topomer similarity searching of conventional structure databases. J Mol Graph Model. 2002 Jun;20(6):447-62. doi: 10.1016/s1093-3263(01)00146-2. PMID: 12071279.

9: Day JP, Lindsay B, Riddell T, Jiang Z, Allcock RW, Abraham A, Sookup S, Christian F, Bogum J, Martin EK, Rae RL, Anthony D, Rosair GM, Houslay DM, Huston E, Baillie GS, Klussmann E, Houslay MD, Adams DR. Elucidation of a structural basis for the inhibitor-driven, p62 (SQSTM1)-dependent intracellular redistribution of cAMP phosphodiesterase-4A4 (PDE4A4). J Med Chem. 2011 May 12;54(9):3331-47. doi: 10.1021/jm200070e. Epub 2011 Apr 13. PMID: 21456625.

10: Lehto M, Savinko T, Wolff H, Kvist PH, Kemp K, Lauerma A, Alenius H. A murine model of epicutaneous protein sensitization is useful to study efficacies of topical drugs in atopic dermatitis. Int Immunopharmacol. 2010 Apr;10(4):377-84. doi: 10.1016/j.intimp.2010.01.001. Epub 2010 Jan 13. PMID: 20074670.

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