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MedKoo Cat#: 319751 | Name: Nelociguat
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Nelociguat, also known as BAY60-4552, is a soluble guanylate cyclase stimulator (sGC stimulator). Soluble guanylate cyclase (sGC) is a key enzyme in the nitric oxide (NO) signalling pathway. On binding of NO to its prosthetic haem group, sGC catalyses the synthesis of the second messenger cyclic guanosine monophosphate (cGMP), which promotes vasodilation and inhibits smooth muscle proliferation, leukocyte recruitment, platelet aggregation and vascular remodelling through a number of downstream mechanisms.

Chemical Structure

Nelociguat
Nelociguat
CAS#625115-52-8

Theoretical Analysis

MedKoo Cat#: 319751

Name: Nelociguat

CAS#: 625115-52-8

Chemical Formula: C19H17FN8O2

Exact Mass: 408.1459

Molecular Weight: 408.40

Elemental Analysis: C, 55.88; H, 4.20; F, 4.65; N, 27.44; O, 7.84

Price and Availability

Size Price Availability Quantity
10mg USD 235.00 2 Weeks
25mg USD 400.00 2 Weeks
50mg USD 645.00 2 Weeks
100mg USD 925.00 2 Weeks
250mg USD 1,495.00 2 Weeks
1g USD 2,500.00 2 Weeks
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Synonym
BAY60-4552; BAY 60-4552; BAY-60-4552; BAY604552; BAY-604552; BAY 604552; Nelociguat
IUPAC/Chemical Name
methyl (4,6-diamino-2-(1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl)pyrimidin-5-yl)carbamate
InChi Key
FTQHGWIXJSSWOY-UHFFFAOYSA-N
InChi Code
1S/C19H17FN8O2/c1-30-19(29)24-14-15(21)25-17(26-16(14)22)13-11-6-4-8-23-18(11)28(27-13)9-10-5-2-3-7-12(10)20/h2-8H,9H2,1H3,(H,24,29)(H4,21,22,25,26)
SMILES Code
FC1=CC=CC=C1CN2N=C(C3=NC(N)=C(NC(OC)=O)C(N)=N3)C4=CC=CN=C42
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
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 Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Nelociguat (BAY60-4552) is a nitric oxide sensitive soluble guanylate cyclase stimulator.
In vitro activity:
To evaluate the effects of BAY 60-4552, a stimulator of soluble guanylate cyclase (sGC), and vardenafil on relaxation of HCC strips from PDE5-i nonresponders. BAY 60-4552 and vardenafil have synergistic effects on relaxation of HCC of PDE5-i nonresponders. Reference: J Sex Med. 2013 May;10(5):1268-77. https://pubmed.ncbi.nlm.nih.gov/23421435/
In vivo activity:
The cardiovascular effects of the NO-insensitive sGC activator GSK2181236A [a low, non-depressor dose, and a high dose which lowered mean arterial pressure (MAP) by 5-10 mmHg] and those of equi-efficacious doses of the NO-sensitive sGC stimulator BAY 60-4552 were assessed in (1) Sprague Dawley rats during coronary artery ischemia/reperfusion (I/R) and (2) spontaneously hypertensive stroke prone rats (SHR-SP) on a high salt/fat diet (HSFD). The high dose of BAY 60-4552 reduced urine output and microalbuminuria and attenuated the increase in MAP to a greater extent than did GSK2181236A. Reference: Front Pharmacol. 2012 Jul 5;3:128. https://pubmed.ncbi.nlm.nih.gov/22783192/

Preparing Stock Solutions

The following data is based on the product molecular weight 408.40 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Albersen M, Linsen L, Tinel H, Sandner P, Van Renterghem K. Synergistic effects of BAY 60-4552 and vardenafil on relaxation of corpus cavernosum tissue of patients with erectile dysfunction and clinical phosphodiesterase type 5 inhibitor failure. J Sex Med. 2013 May;10(5):1268-77. doi: 10.1111/jsm.12095. Epub 2013 Feb 19. PMID: 23421435. 2. Costell MH, Ancellin N, Bernard RE, Zhao S, Upson JJ, Morgan LA, Maniscalco K, Olzinski AR, Ballard VL, Herry K, Grondin P, Dodic N, Mirguet O, Bouillot A, Gellibert F, Coatney RW, Lepore JJ, Jucker BM, Jolivette LJ, Willette RN, Schnackenberg CG, Behm DJ. Comparison of soluble guanylate cyclase stimulators and activators in models of cardiovascular disease associated with oxidative stress. Front Pharmacol. 2012 Jul 5;3:128. doi: 10.3389/fphar.2012.00128. PMID: 22783192; PMCID: PMC3389674. 3. Oudot A, Behr-Roussel D, Poirier S, Sandner P, Bernabé J, Alexandre L, Giuliano F. Combination of BAY 60-4552 and vardenafil exerts proerectile facilitator effects in rats with cavernous nerve injury: a proof of concept study for the treatment of phosphodiesterase type 5 inhibitor failure. Eur Urol. 2011 Nov;60(5):1020-6. doi: 10.1016/j.eururo.2011.07.052. Epub 2011 Jul 30. PMID: 21839578.
In vitro protocol:
1. Albersen M, Linsen L, Tinel H, Sandner P, Van Renterghem K. Synergistic effects of BAY 60-4552 and vardenafil on relaxation of corpus cavernosum tissue of patients with erectile dysfunction and clinical phosphodiesterase type 5 inhibitor failure. J Sex Med. 2013 May;10(5):1268-77. doi: 10.1111/jsm.12095. Epub 2013 Feb 19. PMID: 23421435.
In vivo protocol:
1. Costell MH, Ancellin N, Bernard RE, Zhao S, Upson JJ, Morgan LA, Maniscalco K, Olzinski AR, Ballard VL, Herry K, Grondin P, Dodic N, Mirguet O, Bouillot A, Gellibert F, Coatney RW, Lepore JJ, Jucker BM, Jolivette LJ, Willette RN, Schnackenberg CG, Behm DJ. Comparison of soluble guanylate cyclase stimulators and activators in models of cardiovascular disease associated with oxidative stress. Front Pharmacol. 2012 Jul 5;3:128. doi: 10.3389/fphar.2012.00128. PMID: 22783192; PMCID: PMC3389674. 2. Oudot A, Behr-Roussel D, Poirier S, Sandner P, Bernabé J, Alexandre L, Giuliano F. Combination of BAY 60-4552 and vardenafil exerts proerectile facilitator effects in rats with cavernous nerve injury: a proof of concept study for the treatment of phosphodiesterase type 5 inhibitor failure. Eur Urol. 2011 Nov;60(5):1020-6. doi: 10.1016/j.eururo.2011.07.052. Epub 2011 Jul 30. PMID: 21839578.
1: Zhao X, Wang Z, Wang Y, Zhang H, Blode H, Yoshikawa K, Becker C, Unger S, Frey R, Cui Y. Pharmacokinetics of the Soluble Guanylate Cyclase Stimulator Riociguat in Healthy Young Chinese Male Non-Smokers and Smokers: Results of a Randomized, Double-Blind, Placebo-Controlled Study. Clin Pharmacokinet. 2015 Oct 27. [Epub ahead of print] PubMed PMID: 26507720. 2: Stasch JP, Schlossmann J, Hocher B. Renal effects of soluble guanylate cyclase stimulators and activators: a review of the preclinical evidence. Curr Opin Pharmacol. 2015 Apr;21:95-104. doi: 10.1016/j.coph.2014.12.014. Epub 2015 Jan 31. Review. PubMed PMID: 25645316. 3: Gnoth MJ, Hopfe PM, Czembor W. Determination of riociguat and its major human metabolite M-1 in human plasma by stable-isotope dilution LCMS/MS. Bioanalysis. 2015;7(2):193-205. doi: 10.4155/bio.14.257. PubMed PMID: 25587836. 4: Stasch JP, Evgenov OV. Soluble guanylate cyclase stimulators in pulmonary hypertension. Handb Exp Pharmacol. 2013;218:279-313. doi: 10.1007/978-3-642-38664-0_12. Review. PubMed PMID: 24092345. 5: Albersen M, Linsen L, Tinel H, Sandner P, Van Renterghem K. Synergistic effects of BAY 60-4552 and vardenafil on relaxation of corpus cavernosum tissue of patients with erectile dysfunction and clinical phosphodiesterase type 5 inhibitor failure. J Sex Med. 2013 May;10(5):1268-77. doi: 10.1111/jsm.12095. Epub 2013 Feb 19. PubMed PMID: 23421435. 6: Costell MH, Ancellin N, Bernard RE, Zhao S, Upson JJ, Morgan LA, Maniscalco K, Olzinski AR, Ballard VL, Herry K, Grondin P, Dodic N, Mirguet O, Bouillot A, Gellibert F, Coatney RW, Lepore JJ, Jucker BM, Jolivette LJ, Willette RN, Schnackenberg CG, Behm DJ. Comparison of soluble guanylate cyclase stimulators and activators in models of cardiovascular disease associated with oxidative stress. Front Pharmacol. 2012 Jul 5;3:128. doi: 10.3389/fphar.2012.00128. eCollection 2012. PubMed PMID: 22783192; PubMed Central PMCID: PMC3389674. 7: Mirone V, Verze P. Are we finally on the right track in treating "difficult" erectile dysfunction patients? Eur Urol. 2011 Nov;60(5):1027-8. doi: 10.1016/j.eururo.2011.08.013. Epub 2011 Aug 16. PubMed PMID: 21893378. 8: Oudot A, Behr-Roussel D, Poirier S, Sandner P, Bernabé J, Alexandre L, Giuliano F. Combination of BAY 60-4552 and vardenafil exerts proerectile facilitator effects in rats with cavernous nerve injury: a proof of concept study for the treatment of phosphodiesterase type 5 inhibitor failure. Eur Urol. 2011 Nov;60(5):1020-6. doi: 10.1016/j.eururo.2011.07.052. Epub 2011 Jul 30. PubMed PMID: 21839578.

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