[CAS NO. 1628730-49-3] Praliciguat

Ships within

Stock

Price

Qty

Total

$0.00

Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis

request a quote

If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [1628730-49-3]

Catalog

AS967730

Brand

Arctom Scientific

CAS

1628730-49-3

DESCRIPTION [1628730-49-3]

Overview

MDL	-
Molecular Weight	534.36
Molecular Formula	C21H14F8N6O2
SMILES	FC1=C(C=CC=C1)CN2C(C3=NOC=C3)=CC(C4=NC=C(F)C(NCC(C(F)(F)F)(O)C(F)(F)F)=N4)=N2

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

Summary

Praliciguat (IW-1973) is a potent and orally active soluble guanylate cyclase stimulator, enhances NO signaling, acts as a vasodilator. Praliciguat (IW-1973) stimulates sGC in HEK-293 cells with an EC ₅₀ of 197 nM ^[1] .

IC50 & Target

EC50: 197 nM (sGC) ^[1]

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02616861	Cyclerion Therapeutics	Healthy	November 2015	Phase 1
NCT03091920	Cyclerion Therapeutics	Diabetes Mellitus, Type 2\|Hypertension	February 28, 2017	Phase 2
NCT03217591	Akebia Therapeutics\|Cyclerion Therapeutics	Type 2 Diabetes Mellitus With Diabetic Nephropathy	August 1, 2017	Phase 2
NCT03499106	Cyclerion Therapeutics	Healthy	April 12, 2018	Phase 1
NCT03254485	Akebia Therapeutics\|Cyclerion Therapeutics	Heart Failure With Preserved Ejection Fraction	November 7, 2017	Phase 2
NCT02906579	Cyclerion Therapeutics	Diabetes Mellitus, Type 2\|Hypertension	September 2016	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL ( 467.85 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8714 mL	9.3570 mL	18.7140 mL
5 mM	0.3743 mL	1.8714 mL	3.7428 mL
10 mM	0.1871 mL	0.9357 mL	1.8714 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 (3.89 mM); Clear solution
2.

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

Solubility: ≥ 2.08 mg/mL (3.89 mM); Clear solution

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

References

[1] Daniel P Zimmer, et al. Abstract 16938: IW-1973 is a Potent Soluble Guanylate Cyclase Stimulator in vitro and in vivo With Extensive Tissue Distribution.

Synonyms

2-Propanol, 1,1,1,3,3,3-hexafluoro-2-[[[5-fluoro-2-[1-[(2-fluorophenyl)methyl]-5-(3-isoxazolyl)-1H-pyrazol-3-yl]-4-pyrimidinyl]amino]methyl]-

1,1,1,3,3,3-Hexafluoro-2-[[[5-fluoro-2-[1-[(2-fluorophenyl)methyl]-5-(3-isoxazolyl)-1H-pyrazol-3-yl]-4-pyrimidinyl]amino]methyl]-2-propanol

Praliciguat

IW 1973

1,1,1,3,3,3-hexafluoro-2-{[(5-fluoro-2-{1-[(2-fluorophenyl)methyl]-5-(1,2-oxazol-3-yl)-1H-pyrazol-3-yl}pyrimidin-4-yl)amino]methyl}propan-2-ol

1,1,1,3,3,3-Hexafluoro-2-[[[5-fluoro-2-(1-(2-fluorobenzyl)-5-(isoxazol-3-yl)-1H-pyrazol-3-yl)pyrimidin-4-yl)amino)methyl)propan-2-ol