BRL-50481 | CAS#433695-36-4 | PDE7 inhibitor

BRL-50481
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 522521

CAS#: 433695-36-4

Description: BRL-50481 is a drug developed by GlaxoSmithKline which is the first compound that acts as a phosphodiesterase inhibitor selective for the PDE7 subtype. It has been shown to increase mineralisation activity in osteoblasts, suggesting a potential role for PDE7 inhibitors in the treatment of osteoporosis.

Chemical Structure

BRL-50481

CAS# 433695-36-4

Instruction

Theoretical Analysis

MedKoo Cat#: 522521
Name: BRL-50481
CAS#: 433695-36-4
Chemical Formula: C9H12N2O4S
Exact Mass: 244.05
Molecular Weight: 244.270
Elemental Analysis: C, 44.25; H, 4.95; N, 11.47; O, 26.20; S, 13.13

Price and Availability

Size	Price	Availability
25mg	USD 385	2 Weeks
50mg	USD 650	2 Weeks
100mg	USD 1050	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: BRL-50481; BRL 50481; BRL50481.

IUPAC/Chemical Name: N,N,2-Trimethyl-5-nitro-benzenesulfonamide

InChi Key: IFIUFCJFLGCQPH-UHFFFAOYSA-N

InChi Code: InChI=1S/C9H12N2O4S/c1-7-4-5-8(11(12)13)6-9(7)16(14,15)10(2)3/h4-6H,1-3H3

SMILES Code: O=S(C1=CC([N+]([O-])=O)=CC=C1C)(N(C)C)=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, not in water

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 244.27 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: Kaneda T, Kido Y, Tajima T, Urakawa N, Shimizu K. PDE4 and PDE5 regulate cyclic nucleotide contents and relaxing effects on carbachol-induced contraction in the bovine abomasum. J Vet Med Sci. 2015 Jan;77(1):15-9. doi: 10.1292/jvms.14-0248. Epub 2014 Oct 15. PubMed PMID: 25319411; PubMed Central PMCID: PMC4349533.

2: Monzel M, Kuhn M, Bähre H, Seifert R, Schneider EH. PDE7A1 hydrolyzes cCMP. FEBS Lett. 2014 Sep 17;588(18):3469-74. doi: 10.1016/j.febslet.2014.08.005. Epub 2014 Aug 13. PubMed PMID: 25128584.

3: Medina-Rodríguez EM, Arenzana FJ, Pastor J, Redondo M, Palomo V, García de Sola R, Gil C, Martínez A, Bribián A, de Castro F. Inhibition of endogenous phosphodiesterase 7 promotes oligodendrocyte precursor differentiation and survival. Cell Mol Life Sci. 2013 Sep;70(18):3449-62. doi: 10.1007/s00018-013-1340-2. Epub 2013 May 10. PubMed PMID: 23661015.

4: Zhai K, Hubert F, Nicolas V, Ji G, Fischmeister R, Leblais V. β-Adrenergic cAMP signals are predominantly regulated by phosphodiesterase type 4 in cultured adult rat aortic smooth muscle cells. PLoS One. 2012;7(10):e47826. doi: 10.1371/journal.pone.0047826. Epub 2012 Oct 18. PubMed PMID: 23094097; PubMed Central PMCID: PMC3475707.

5: Wunder F, Gnoth MJ, Geerts A, Barufe D. A novel PDE2A reporter cell line: characterization of the cellular activity of PDE inhibitors. Mol Pharm. 2009 Jan-Feb;6(1):326-36. doi: 10.1021/mp800127n. PubMed PMID: 19049345.

6: Zhang L, Murray F, Zahno A, Kanter JR, Chou D, Suda R, Fenlon M, Rassenti L, Cottam H, Kipps TJ, Insel PA. Cyclic nucleotide phosphodiesterase profiling reveals increased expression of phosphodiesterase 7B in chronic lymphocytic leukemia. Proc Natl Acad Sci U S A. 2008 Dec 9;105(49):19532-7. doi: 10.1073/pnas.0806152105. Epub 2008 Nov 25. PubMed PMID: 19033455; PubMed Central PMCID: PMC2614795.

7: Pekkinen M, Ahlström ME, Riehle U, Huttunen MM, Lamberg-Allardt CJ. Effects of phosphodiesterase 7 inhibition by RNA interference on the gene expression and differentiation of human mesenchymal stem cell-derived osteoblasts. Bone. 2008 Jul;43(1):84-91. doi: 10.1016/j.bone.2008.02.021. Epub 2008 Mar 12. PubMed PMID: 18420479.

8: Jackson EK, Ren J, Zacharia LC, Mi Z. Characterization of renal ecto-phosphodiesterase. J Pharmacol Exp Ther. 2007 May;321(2):810-5. Epub 2007 Feb 16. PubMed PMID: 17308037.

9: Smith SJ, Cieslinski LB, Newton R, Donnelly LE, Fenwick PS, Nicholson AG, Barnes PJ, Barnette MS, Giembycz MA. Discovery of BRL 50481 [3-(N,N-dimethylsulfonamido)-4-methyl-nitrobenzene], a selective inhibitor of phosphodiesterase 7: in vitro studies in human monocytes, lung macrophages, and CD8+ T-lymphocytes. Mol Pharmacol. 2004 Dec;66(6):1679-89. Epub 2004 Sep 15. PubMed PMID: 15371556.

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