[CAS NO. 347887-36-9] Fedovapagon

Name: Fedovapagon
Brand: Arctom Scientific
SKU: AS045618

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PRODUCTS SPECIFICATIONS [347887-36-9]

Fulfillment

Catalog

AS045618

Brand

Arctom Scientific

CAS

347887-36-9

DESCRIPTION [347887-36-9]

Overview

MDL	MFCD19443737
Molecular Weight	462.58
Molecular Formula	C27H34N4O3
SMILES	CC1=C(CNC(N2CCC[C@]2(C(N(C)C)=O)[H])=O)C=CC(C(N3CCCCC4=C3C=CC=C4)=O)=C1

For research use only. We do not sell to patients.

Summary

Fedovapagon (VA106483) is a selective and orally active vasopressin V2 receptor (V2R) agonist with an EC ₅₀ of 24 nM. Fedovapagon can be used in the research of nocturia ^[1] .

IC50 & Target

V2 Receptor

24 nM (EC ₅₀ )

In Vivo

Fedovapagon (1 mg/kg, oral administration) inhibits urine output with 81% inhibition rate in rats ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Brattleboro rats ^[1]
Dosage:	1 mg/kg, 3 mg/kg
Administration:	Oral administration
Result:	Reduced urine volume with almost full inhibition of urine output for 2 h. Returned the urine to normal levels 5 h after dosing.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02537288	Vantia Ltd	Healthy	October 2015	Phase 1
NCT00879216	Vantia Ltd	Nocturia	April 2009	Phase 1
NCT01171391	Vantia Ltd	Nocturia	July 2010	Phase 1
NCT02440841	Vantia Ltd	Nocturia	May 2015	Phase 1
NCT00879138	Vantia Ltd\|Veeda Clinical Research	Nocturia	August 2008	Phase 1\|Phase 2
NCT01038843	Vantia Ltd	Nocturia	December 2009	Phase 2
NCT01330927	Vantia Ltd	Nocturia\|Benign Prostatic Hypertrophy (BPH)	March 2011	Phase 1
NCT00922740	Vantia Ltd	Nocturia	June 2009	Phase 1
NCT02637960	Vantia Ltd	Nocturia	March 2016	Phase 2\|Phase 3
NCT01656239	Vantia Ltd	Nocturia	August 2012	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : ≥ 125 mg/mL ( 270.22 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1618 mL	10.8089 mL	21.6179 mL
5 mM	0.4324 mL	2.1618 mL	4.3236 mL
10 mM	0.2162 mL	1.0809 mL	2.1618 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (4.50 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (4.50 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (4.50 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Yea CM, et al. New benzylureas as a novel series of potent, nonpeptidic vasopressin V2 receptor agonists. J Med Chem. 2008 Dec 25;51(24):8124-34.