Name: Udenafil
Brand: Selleck Chemicals
SKU: S6433
Rating: 5 (1 reviews)

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Quality Control

Batch: S643301 DMSO]100 mg/mL]false]Ethanol]25 mg/mL]false]Water]Insoluble]false Purity: 99.99%

Cited in Nature Medicine for its top-tier quality
COA
SDS
Datasheet

99.99

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite
Other PDE Inhibitors	Rolipram IBMX (3-Isobutyl-1-methylxanthine) Icariin Cilomilast Mardepodect (PF-2545920) Deltarasin PF-8380 Enpp-1-IN-1 Ibudilast BRL-50481

Chemical Information, Storage & Stability

Molecular Weight	516.66	Formula	C₂₅H₃₆N₆O₄S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	268203-93-6	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCCC1=NN(C2=C1N=C(NC2=O)C3=C(C=CC(=C3)S(=O)(=O)NCCC4CCCN4C)OCCC)C

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (193.55 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 25 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	PDE5 (Cell-free assay) 8.25 nM PDE3 (Cell-free assay) 52 nM PDE6 (Cell-free assay) 53.3 nM PDE2 (Cell-free assay) 101 nM
In vitro	The inhibitory effect of udenafil on PDE5 is about 150-fold greater than that on PDE1 (selectivity ratio of 149). PDE11 selectivity of this compound (selectivity ratio of 96) is relatively high, indicating a very low probability of inhibition of PDE11 at therapeutic doses of this chemical. The IC50 values for PDE2, PDE3, and PDE6 of this compound are 101±15.1 nM, 52.0±3.53 nM, and 53.3±2.47 nM respectively.
In vivo	Udenafil is rapidly absorbed, reaching peak plasma concentrations at 0.8-1.3 h, then declining monoexponentially with a terminal half-life (T_1/2) between 7.3 and 12.1 hours, giving it the unique pharmacokinetics of both relatively rapid onset and long duration. This compound has also been shown in preclinical studies to have potent erectogenic properties in rats and rabbits with a broad safety margin. Absolute oral bioavailability of this chemical is only 38% in rats. This low oral bioavailability appears to be mainly due to a considerable intestinal first-pass effect.
References	[1] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4027935/ [2] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3607490/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01928563	Unknown status	Healthy Male Subjects	Dong-A Pharmaceutical Co. Ltd.\|Dong-A ST Co. Ltd.	September 2013	Phase 1
NCT01929213	Unknown status	Healthy Volunteers	Dong-A Pharmaceutical Co. Ltd.\|Dong-A ST Co. Ltd.	August 2013	Phase 1
NCT01108900	Completed	Erectile Dysfunction	Pfizer''s Upjohn has merged with Mylan to form Viatris Inc.\|Pfizer	July 2010	--

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Udenafil PDE inhibitor

Chemical Structure

Molecular Weight: 516.66