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MedKoo Cat#: 585199 | Name: Siguazodan
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Description:

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

Siguazodan is a selective phosphodiesterase inhibitor with anti-platelet action properties. Siguazodan selectively inhibited the major cyclic AMP-hydrolysing PDE in human platelet supernatants. In platelet-rich plasma (PRP), siguazodan inhibited U46619-induced aggregation more potently than that induced by ADP and collagen. Treatment of the PRP with aspirin had no effect on the potency of siguazodan. In washed platelets, siguazodan increased cyclic AMP levels and reduced cytoplasmic free calcium [( Ca2+]i). ADP decreased the ability of siguazodan to raise cyclic AMP and this may explain its lower potency in inhibiting responses to ADP. Siguazodan has anti-platelet actions over the same concentration range that it is an inotrope and vasodilator.

Chemical Structure

Siguazodan
CAS#115344-47-3

Theoretical Analysis

MedKoo Cat#: 585199

Name: Siguazodan

CAS#: 115344-47-3

Chemical Formula: C14H16N6O

Exact Mass: 284.1386

Molecular Weight: 284.32

Elemental Analysis: C, 59.14; H, 5.67; N, 29.56; O, 5.63

Price and Availability

Size Price Availability Quantity
10mg USD 150.00 2 Weeks
25mg USD 250.00 2 Weeks
50mg USD 450.00 2 Weeks
100mg USD 750.00 2 Weeks
200mg USD 1,250.00 2 Weeks
500mg USD 2,850.00 2 Weeks
1g USD 4,250.00 2 Weeks
2g USD 5,850.00 2 Weeks
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Related CAS #
No Data
Synonym
Siguazodan; SK&F 94836; SKF 94836; SKF-94836; SKF94836;
IUPAC/Chemical Name
2-Cyano-1-methyl-3-(4-(4-methyl-6-oxo-1,4,5,6-tetrahydropyridazin-3-yl)phenyl)guanidine
InChi Key
NUHPODZZKHQQET-UHFFFAOYSA-N
InChi Code
InChI=1S/C14H16N6O/c1-9-7-12(21)19-20-13(9)10-3-5-11(6-4-10)18-14(16-2)17-8-15/h3-6,9H,7H2,1-2H3,(H,19,21)(H2,16,17,18)
SMILES Code
O=C1CC(C)C(C2=CC=C(N/C(NC)=N/C#N)C=C2)=NN1
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
>3 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

Preparing Stock Solutions

The following data is based on the product molecular weight 284.32 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
1: Yan JQ, Liu M, Ma YL, Le KD, Dong B, Li GH. Inferences of carboplatin response-related signature by integrating multiomics data in ovarian serous cystadenocarcinoma. Exp Biol Med (Maywood). 2022 Jun;247(11):910-920. doi: 10.1177/15353702221083254. Epub 2022 Mar 12. PMID: 35285286; PMCID: PMC9189566. 2: Venkatasamy R, Spina D. Novel relaxant effects of RPL554 on guinea pig tracheal smooth muscle contractility. Br J Pharmacol. 2016 Aug;173(15):2335-51. doi: 10.1111/bph.13512. Epub 2016 Jul 7. PMID: 27174172; PMCID: PMC4945770. 3: BinMahfouz H, Borthakur B, Yan D, George T, Giembycz MA, Newton R. Superiority of combined phosphodiesterase PDE3/PDE4 inhibition over PDE4 inhibition alone on glucocorticoid- and long-acting β2-adrenoceptor agonist- induced gene expression in human airway epithelial cells. Mol Pharmacol. 2015 Jan;87(1):64-76. doi: 10.1124/mol.114.093393. Epub 2014 Oct 16. PMID: 25324049. 4: Sosroseno W, Sugiatno E. Cyclic-AMP-dependent proliferation of a human osteoblast cell line (HOS cells) induced by hydroxyapatite: effect of exogenous nitric oxide. Acta Biomed. 2008 Aug;79(2):110-6. PMID: 18788505. 5: Kantarci S, Donahoe PK. Congenital diaphragmatic hernia (CDH) etiology as revealed by pathway genetics. Am J Med Genet C Semin Med Genet. 2007 May 15;145C(2):217-26. doi: 10.1002/ajmg.c.30132. PMID: 17436295. 6: Sosroseno W, Musa M, Ravichandran M, Fikri Ibrahim M, Bird PS, Seymour GJ. The role of cyclic-AMP on arginase activity by a murine macrophage cell line (RAW264.7) stimulated with lipopolysaccharide from Actinobacillus actinomycetemcomitans. Oral Microbiol Immunol. 2006 Dec;21(6):347-52. doi: 10.1111/j.1399-302X.2006.00300.x. PMID: 17064391. 7: Faisy C, Risse PA, Naline E, Guerot E, Fagon JY, Devillier P, Advenier C. Phosphodiesterase 4 inhibitors modulate beta2-adrenoceptor agonist-induced human airway hyperresponsiveness. Life Sci. 2006 Oct 12;79(20):1929-35. doi: 10.1016/j.lfs.2006.06.020. Epub 2006 Jun 20. PMID: 16820175. 8: Lau HY, Kam MF. Inhibition of mast cell histamine release by specific phosphodiesterase inhibitors. Inflamm Res. 2005 Apr;54 Suppl 1:S05-6. doi: 10.1007/s00011-004-0401-2. PMID: 15928811. 9: Eskandari N, Wickramasinghe T, Peachell PT. Effects of phosphodiesterase inhibitors on interleukin-4 and interleukin-13 generation from human basophils. Br J Pharmacol. 2004 Aug;142(8):1265-72. doi: 10.1038/sj.bjp.0705892. Epub 2004 Jul 20. PMID: 15265810; PMCID: PMC1575198. 10: Gillespie JI. Phosphodiesterase-linked inhibition of nonmicturition activity in the isolated bladder. BJU Int. 2004 Jun;93(9):1325-32. doi: 10.1111/j.1464-410X.2004.04840.x. PMID: 15180632. 11: Delgado M, Fuentes JA, Fernandez-Alfonso MS. Histamine up-regulates phosphodiesterase IV activity in U-937 cells through H2 receptor stimulation and cAMP increase. Med Sci Monit. 2003 Jun;9(6):BR212-9. PMID: 12824943. 12: Bardou M, Goirand F, Bernard A, Guerard P, Gatinet M, Devillier P, Dumas JP, Morcillo EJ, Rochette L, Dumas M. Relaxant effects of selective phosphodiesterase inhibitors on U46619 precontracted human intralobar pulmonary arteries and role of potassium channels. J Cardiovasc Pharmacol. 2002 Jul;40(1):153-61. doi: 10.1097/00005344-200207000-00019. PMID: 12072589. 13: Bardou M, Goirand F, Marchand S, Rouget C, Devillier P, Dumas JP, Morcillo EJ, Rochette L, Dumas M. Hypoxic vasoconstriction of rat main pulmonary artery: role of endogenous nitric oxide, potassium channels, and phosphodiesterase inhibition. J Cardiovasc Pharmacol. 2001 Aug;38(2):325-34. doi: 10.1097/00005344-200108000-00018. PMID: 11483882. 14: Rickards KJ, Page CP, Lees P, Cunningham FM. Phosphodiesterase activity in neutrophils from horses with chronic obstructive pulmonary disease. Vet Immunol Immunopathol. 2000 Oct 31;76(3-4):319-30. doi: 10.1016/s0165-2427(00)00220-8. PMID: 11044563. 15: De Witt BJ, Marrone JR, Kadowitz PJ. Comparison of responses to siguazodan, rolipram, and zaprinast in the feline pulmonary vascular bed. Eur J Pharmacol. 2000 Oct 13;406(2):233-8. doi: 10.1016/s0014-2999(00)00501-x. PMID: 11020486. 16: Landells LJ, Spina D, Souness JE, O'Connor BJ, Page CP. A biochemical and functional assessment of monocyte phosphodiesterase activity in healthy and asthmatic subjects. Pulm Pharmacol Ther. 2000;13(5):231-9. doi: 10.1006/pupt.2000.0248. PMID: 11003567. 17: Hammermann R, Hey C, Schäfer N, Racké K. Phosphodiesterase inhibitors and forskolin Up-regulate arginase activity in rabbit alveolar macrophages. Pulm Pharmacol Ther. 2000;13(3):141-7. doi: 10.1006/pupt.2000.0240. PMID: 10873552. 18: Banner KH, Dimitriou G, Kinali M, Page CP, Greenough A. Evidence to suggest that the phosphodiesterase 4 isoenzyme is present and involved in the proliferation of umbilical cord blood mononuclear cells. Clin Exp Allergy. 2000 May;30(5):706-12. doi: 10.1046/j.1365-2222.2000.00813.x. PMID: 10792363. 19: Ahmad M, Abdel-Wahab YH, Tate R, Flatt PR, Pyne NJ, Furman BL. Effect of type-selective inhibitors on cyclic nucleotide phosphodiesterase activity and insulin secretion in the clonal insulin secreting cell line BRIN-BD11. Br J Pharmacol. 2000 Mar;129(6):1228-34. doi: 10.1038/sj.bjp.0703165. PMID: 10725272; PMCID: PMC1571945. 20: Bardou M, Cortijo J, Loustalot C, Taylor S, Perales-Marín A, Mercier FJ, Dumas M, Deneux-Tharaux C, Frydman R, Morcillo EJ, Advenier C. Pharmacological and biochemical study on the effects of selective phosphodiesterase inhibitors on human term myometrium. Naunyn Schmiedebergs Arch Pharmacol. 1999 Oct;360(4):457-63. doi: 10.1007/s002109900092. PMID: 10551283.