Sildenafil Citrate


Catalog No. size PriceQuantity
M7029-2 2mg solid $96
M7029-10 10mg solid $401

Description

Cas:171599-83-0 (citrate)

Product Information

Sildenafil is a selective inhibitor of PDE5 (type 5 cGMP phosphodiesterase) which catalyzes the hydrolysis of 3',5'-cyclic guanosine monophosphate (cGMP). As a PDE5 inhibitor, Sildenafil has been reported to enhance neuro-, synapto- and angiogenesis in rat models of stroke and also is reported to be a mild vasodilator. Sildenafil has also been shown to prevent indomethacin-induced small intestinal ulceration formation through an NO/cGMP- dependent mechanism.

 

Chemical Formula: C28H38N6O11S

 

Molecular Weight: 666.7

 

Elemental Analysis: C, 50.44; H, 5.75; N, 12.61; O, 26.40; S, 4.81

 

Synonym: 

 

Sildenafil Citrate

UK 92480-10

UK-92,480-10

Trade name

Revatio

VIAGRA

 

Chemical Name: 5-(2-ethoxy-5-((4-methylpiperazin-1-yl)sulfonyl)phenyl)-1-methyl-3-propyl-1,4-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one 2-hydroxypropane-1,2,3-tricarboxylate

 

InChi Key:

DEIYFTQMQPDXOT-UHFFFAOYSA-N

 

InChi Code: InChI=1S/C22H30N6O4S.C6H8O7/c1-5-7-17-19-20(27(4)25-17)22(29)24-21(23-19)16-14-15(8-9-18(16)32-6-2)33(30,31)28-12-10-26(3)11-13-28;7-3(8)1-6(13,5(11)12)2-4(9)10/h8-9,14H,5-7,10-13H2,1-4H3,(H,23,24,29);13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)

 

Smiles Code:

CCCC1=NN(C2=C1NC(=NC2=O)C3=C(C=CC(=C3)S(=O)(=O)N4CCN(CC4)C)OCC)C.C(C(=O)O)C(CC(=O)O)(C(=O)O)O

Technical Data:

 

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

 

In Vitro

Pretreatment with 1 μM Sildenafil citrate potentiates the phosphorylation of ERK1/ERK2, an increase in the percentage of cells in S phase and cell proliferation, compared with serotonin stimulation alone (P<0.05). Pretreatment with 1 μM Sildenafil citrate followed by serotonin stimulation leads to dramatic increase in OD value to 0.33, significantly different compared with serotonin stimulation alone (P<0.05). 1 μM Sildenafil obviously enhances the upregulation of ERK1/ERK2 phosphorylation induced by serotonin.

 

In Vivo

In the dog model of erection, Sildenafil citrate significantly increases ICP and ICP/BP but shows no significant effect on BP compared with vehicle. Sildenafil treatment significantly decreases the number of TL+-cells at 10 but not 0.5 mg/kg. At this time point, cells positive for the M1-like marker COX-2+ are found in the ischemic core in PBS-treated animals, whereas they are mostly observed in the penumbra in 10 mg/kg (but not 0.5 mg/kg) Sildenafil-treated animals. In contrast, 8 days after pMCAo the number of microglia/macrophages stained by Iba-1 are significantly reduced by Sildenafil treatment (0.5 and/or 10 mg/kg dose). Sildenafil citrate has been reported to decrease flap necrosis in preclinical animal models by increasing the secretion of growth factors (FGF and VEGF), and histologically is shown to be effective in rat cavernous nerve architecture.

 

 

References

 

  1. Shah PC, Trivedi NA. A meta-analysis on efficacy and tolerability of sildenafil for erectile dysfunction in patients with diabetes mellitus. Indian J Sex Transm Dis AIDS. 2018 Jan-Jun;39(1):1-6. doi: 10.4103/ijstd.IJSTD_99_17. Review. PubMed PMID: 30187018; PubMed Central PMCID: PMC6111643.

 

  1. Andersson KE. PDE5 inhibitors - pharmacology and clinical applications 20 years after sildenafil discovery. Br J Pharmacol. 2018 Jul;175(13):2554-2565. doi: 10.1111/bph.14205. Epub 2018 Apr 25. Review. PubMed PMID: 29667180; PubMed Central PMCID: PMC6003652.

 

  1. Kelly LE, Ohlsson A, Shah PS. Sildenafil for pulmonary hypertension in neonates. Cochrane Database Syst Rev. 2017 Aug 4;8:CD005494. doi: 10.1002/14651858.CD005494.pub4. Review. PubMed PMID: 28777888.

 

  1. Gong B, Ma M, Xie W, Yang X, Huang Y, Sun T, Luo Y, Huang J. Direct comparison of tadalafil with sildenafil for the treatment of erectile dysfunction: a systematic review and meta-analysis. Int Urol Nephrol. 2017 Oct;49(10):1731-1740. doi: 10.1007/s11255-017-1644-5. Epub 2017 Jul 24. Review. PubMed PMID: 28741090; PubMed Central PMCID: PMC5603624.

 

  1. Simonca L, Tulloh R. Sildenafil in Infants and Children. Children (Basel). 2017 Jul 24;4(7). pii: E60. doi: 10.3390/children4070060. Review. PubMed PMID: 28737730; PubMed Central PMCID: PMC5532552.

 

Products are for research use only. Not for human use.

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