Gisadenafil

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

MedKoo CAT#: 319829

CAS#: 334826-98-1

Description: Gisadenafil, also known as UK 369003, is a PDE5 inhibitor under development for the treatment of men with storage lower urinary tract symptoms associated with a clinical diagnosis of overactive bladder.

Chemical Structure

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Gisadenafil
CAS# 334826-98-1
Instruction

Theoretical Analysis

MedKoo Cat#: 319829
Name: Gisadenafil
CAS#: 334826-98-1
Chemical Formula: C23H33N7O5S
Exact Mass: 519.23
Molecular Weight: 519.621
Elemental Analysis: C, 53.16; H, 6.40; N, 18.87; O, 15.39; S, 6.17

Price and Availability

Size Price Availability Quantity
10mg USD -2
25mg USD -2
50mg USD -2
100mg USD -2
200mg USD -2
500mg USD -2
1g USD -1
2g USD -1
5g USD -1
10g USD -1
20g USD -1
50g USD -1
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Synonym: UK 369003; UK369003; UK-369003; UK 369,003; UK369,003; UK-369,003; Gisadenafil

IUPAC/Chemical Name: 5-(2-ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)pyridin-3-yl)-3-ethyl-2-(2-methoxyethyl)-2,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one

InChi Key: YPFZMBHKIVDSNR-UHFFFAOYSA-N

InChi Code: InChI=1S/C23H33N7O5S/c1-5-18-19-20(27-30(18)12-13-34-4)22(31)26-21(25-19)17-14-16(15-24-23(17)35-7-3)36(32,33)29-10-8-28(6-2)9-11-29/h14-15H,5-13H2,1-4H3,(H,25,26,31)

SMILES Code: O=C1C2=NN(CCOC)C(CC)=C2N=C(C3=CC(S(=O)(N4CCN(CC)CC4)=O)=CN=C3OCC)N1

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:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 519.62 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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1: Rawson DJ, Ballard S, Barber C, Barker L, Beaumont K, Bunnage M, Cole S,
Corless M, Denton S, Ellis D, Floc'h M, Foster L, Gosset J, Holmwood F, Lane C,
Leahy D, Mathias J, Maw G, Million W, Poinsard C, Price J, Russel R, Street S,
Watson L. The discovery of UK-369003, a novel PDE5 inhibitor with the potential
for oral bioavailability and dose-proportional pharmacokinetics. Bioorg Med Chem.
2012 Jan 1;20(1):498-509. doi: 10.1016/j.bmc.2011.10.022. Epub 2011 Oct 24.
PubMed PMID: 22100260.


2: Martínez-Salamanca JI, Carballido J, Eardley I, Giuliano F, Gratzke C, Rosen
R, Salonia A, Stief C. Phosphodiesterase type 5 inhibitors in the management of
non-neurogenic male lower urinary tract symptoms: critical analysis of current
evidence. Eur Urol. 2011 Sep;60(3):527-35. doi: 10.1016/j.eururo.2011.05.054.
Epub 2011 Jun 12. Review. PubMed PMID: 21684677.


3: Watson KJ, Davis J, Jones HM. Application of physiologically based
pharmacokinetic modeling to understanding the clinical pharmacokinetics of
UK-369,003. Drug Metab Dispos. 2011 Jul;39(7):1203-13. doi:
10.1124/dmd.111.038224. Epub 2011 Mar 30. PubMed PMID: 21451120.


4: Tamimi NA, Mincik I, Haughie S, Lamb J, Crossland A, Ellis P. A
placebo-controlled study investigating the efficacy and safety of the
phosphodiesterase type 5 inhibitor UK-369,003 for the treatment of men with lower
urinary tract symptoms associated with clinical benign prostatic hyperplasia. BJU
Int. 2010 Sep;106(5):674-80. doi: 10.1111/j.1464-410X.2010.09204.x. PubMed PMID:
20184577.


5: Giuliano FA, Lamb J, Crossland A, Haughie S, Ellis P, Tamimi NA. A
placebo-controlled exploratory study investigating the efficacy and safety of the
phosphodiesterase type 5 inhibitor UK-369,003 for the treatment of men with
storage lower urinary tract symptoms associated with a clinical diagnosis of
overactive bladder. BJU Int. 2010 Sep;106(5):666-73. doi:
10.1111/j.1464-410X.2010.09205.x. PubMed PMID: 20151971.