1. GPCR/G Protein
  2. Guanylate Cyclase
  3. Nelociguat

Nelociguat (Synonyms: BAY60-4552)

Cat. No.: HY-78237 Purity: 99.73%
Handling Instructions

Nelociguat (BAY60-4552) is a nitric oxide sensitive soluble guanylate cyclase stimulator.

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

Nelociguat Chemical Structure

Nelociguat Chemical Structure

CAS No. : 625115-52-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 119 In-stock
Estimated Time of Arrival: December 31
5 mg USD 108 In-stock
Estimated Time of Arrival: December 31
10 mg USD 168 In-stock
Estimated Time of Arrival: December 31
50 mg USD 336 In-stock
Estimated Time of Arrival: December 31
100 mg USD 540 In-stock
Estimated Time of Arrival: December 31
200 mg USD 708 In-stock
Estimated Time of Arrival: December 31
500 mg USD 924 Get quote
1 g USD 1164 Get quote
5 g   Get quote  
10 g   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Nelociguat (BAY60-4552) is a nitric oxide sensitive soluble guanylate cyclase stimulator.

In Vitro

Soluble guanylate cyclase (sGC) is a key enzyme in the nitric oxide (NO) signalling pathway[1]. Riociguat is metabolized to BAY60-4552 not only via cytochrome P450 isoenzymes 3A4 (CYP3A4), CYP2C8, and CYP2J2, but also via CYP1A1, located in the liver and lungs[2].

In Vivo

GSK2181236A and BAY 60-4552 provide partial benefit against hypertension-induced end-organ damage. In spontaneously hypertensive stroke-prone rats, a low dose of BAY 60-4552 decreases urine output and improved survival. A high dose also reduces urine output, and in addition reduces microalbuminuria and attenuates the increase in mean arterial pressure. Both the 0.3 and 3 mg/kg/day doses of BAY 60-4552 improves survival of 46 and 69%. Seven weeks of treatment with BAY 60-4552 (0.3 and 3.0 mg/kg/day) dose-dependently decreases urine output to 79±11 and 56±10 mL/day[1]. BAY 60-4552, and vardenafil provides synergistic beneficial effects and might therefore salvage patients who experience treatment failures with PDE5 inhibitors after radical prostatectomy[3].

Clinical Trial
Molecular Weight

408.39

Formula

C₁₉H₁₇FN₈O₂

CAS No.

625115-52-8

SMILES

O=C(OC)NC1=C(N)N=C(C2=NN(CC3=CC=CC=C3F)C4=NC=CC=C42)N=C1N

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 : 50 mg/mL (122.43 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4486 mL 12.2432 mL 24.4864 mL
5 mM 0.4897 mL 2.4486 mL 4.8973 mL
10 mM 0.2449 mL 1.2243 mL 2.4486 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 (5.09 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (5.09 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

NelociguatBAY60-4552Guanylate CyclaseInhibitorinhibitorinhibit

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Product Name:
Nelociguat
Cat. No.:
HY-78237
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