Praliciguat free base · Synonyms: IW-1973

Praliciguat (IW-1973) is a potent and orally active soluble guanylate cyclase stimulator, enhances NO signaling, acts as a vasodilator.

For research use only. Not for human or veterinary use.

Target Guanylate Cyclase Apoptosis

Research area Cardiovascular Disease Metabolic Disease

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Data Sheet SDS COA

Praliciguat structure

CAS No.: 1628730-49-3

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
10 mg	USD 420.00	BP-01911-10mg	In stock	Get quote
25 mg	USD 620.00	BP-01911-25mg	In stock	Get quote
50 mg	USD 920.00	BP-01911-50mg	In stock	Get quote
250 mg	USD 1,920.00	BP-01911-250mg	In stock	Get quote
500 mg	Inquire	BP-01911-500mg	In stock	Inquire
1 g	Inquire	BP-01911-1g	Inquire	Inquire

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Description

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 EC50 of 197 nM.

Biological activity

In Vitro Praliciguat stimulates soluble guanylate cyclase in HEK-293 cells with an EC50 of 197 nM. Praliciguat demonstrates concentration-dependent relaxation of pre-contracted subcutaneous resistance arteries (EC50 = 34.7 nM). Praliciguat (10 μM, 48 h) inhibits the expression of proinflammatory cytokines and secretion of monocyte chemoattractant protein 1 in TNF-α-challenged proximal tubular epithelial cells (RPTC). Praliciguat (1-10 μM, 48 h) inhibits TGF-β-mediated apoptosis in RPTC. In Vivo Praliciguat (1 mg/kg, p.o.) reduces arterial pressure (MAP) in normotensive and hypertensive rats. Praliciguat (1-10 mg/kg, p.o.) attenuates proteinuria in obese ZSF1 rats model of diabetic nephropathy. Praliciguat (1-10 mg/kg, p.o., daily for 2-7 weeks) attenuates inflammation, fibrosis, and end-organ damage in the Dahl rats model of cardiorenal failure.

Identifiers

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
InChIKey: CYSJNTQNMDWAJV-UHFFFAOYSA-N

Specifications

MW (average): 534.3621
Formula: C₂₁H₁₄F₈N₆O₂
CAS No.: 1628730-49-3
Physical state: Solid
Color: White to off-white
Shipping: 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: Powder -20 ℃, 3 years; 4℃ 2 year; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO 250 mg/mL

Documents

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.

[2]. Liu G, et al. Praliciguat inhibits progression of diabetic nephropathy in ZSF1 rats and suppresses inflammation and apoptosis in human renal proximal tubular cells. Am J Physiol Renal Physiol. 2020 Oct 1;319(4):F697-F711.

[3]. Shea CM, et al. Soluble guanylate cyclase stimulator praliciguat attenuates inflammation, fibrosis, and end-organ damage in the Dahl model of cardiorenal failure. Am J Physiol Renal Physiol. 2020 Jan 1;318(1):F148-F159.

Same target

Search Guanylate Cyclase

Same research area

Search Cardiovascular Disease