MedKoo Cat#: 122964 | Name: VK-II-86
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Description:

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

VK-II-86 is a synthetic analogue of carvedilol that lacks β-adrenoceptor antagonist activity. It targets the ryanodine receptor 2 (RyR2) channel, inhibiting store-overload-induced calcium release (SOICR). Therapeutically, VK-II-86 has been shown to prevent hypokalaemia-induced ventricular arrhythmias by normalizing calcium homeostasis and repolarization reserve. Additionally, it has demonstrated efficacy in reducing ouabain-induced apoptosis and spontaneous contractions in cardiac myocytes, indicating potential in treating digitalis-induced arrhythmias.

Chemical Structure

VK-II-86
VK-II-86
CAS#955371-84-3

Theoretical Analysis

MedKoo Cat#: 122964

Name: VK-II-86

CAS#: 955371-84-3

Chemical Formula: C25H28N2O4

Exact Mass: 420.2049

Molecular Weight: 420.51

Elemental Analysis: C, 71.41; H, 6.71; N, 6.66; O, 15.22

Price and Availability

Size Price Availability Quantity
5mg USD 350.00 2 Weeks
50mg USD 950.00 2 Weeks
100mg USD 1,550.00 2 Weeks
1g USD 4,950.00 2 Weeks
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Related CAS #
No Data
Synonym
VK-II-86; VK-II 86; VK-II86; VKII-86
IUPAC/Chemical Name
4-((9H-carbazol-4-yl)oxy)-1-((2-(2-methoxyphenoxy)ethyl)amino)butan-2-ol
InChi Key
OHYHNEODRHJYSS-UHFFFAOYSA-N
InChi Code
InChI=1S/C25H28N2O4/c1-29-22-10-4-5-11-23(22)31-16-14-26-17-18(28)13-15-30-24-12-6-9-21-25(24)19-7-2-3-8-20(19)27-21/h2-12,18,26-28H,13-17H2,1H3
SMILES Code
OC(CNCCOC1=C(C=CC=C1)OC)CCOC2=CC=CC3=C2C4=C(N3)C=CC=C4
Appearance
To be determined
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
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
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

Preparing Stock Solutions

The following data is based on the product molecular weight 420.51 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
1: Hori A, Inaba H, Hato T, Tanaka K, Sato S, Okamoto M, Horiuchi Y, Paran FJ, Tabe Y, Mori S, Rosales C, Akamatsu W, Murayama T, Kurebayashi N, Sakurai T, Ai T, Miida T. Carvedilol suppresses ryanodine receptor-dependent Ca2+ bursts in human neurons bearing PSEN1 variants found in early onset Alzheimer's disease. PLoS One. 2024 Aug 22;19(8):e0291887. doi: 10.1371/journal.pone.0291887. PMID: 39173065; PMCID: PMC11341060. 2: Sommese LM, Racioppi MF, Shen X, Orlowski A, Valverde CA, Louch WE, Vila Petroff M, Gonano LA. Discordant Ca2+ release in cardiac myocytes: characterization and susceptibility to pharmacological RyR2 modulation. Pflugers Arch. 2022 Jun;474(6):625-636. doi: 10.1007/s00424-022-02678-8. Epub 2022 Mar 2. PMID: 35235009. 3: Robinson VM, Alsalahat I, Freeman S, Antzelevitch C, Barajas-Martinez H, Venetucci L. A carvedilol analogue, VK-II-86, prevents hypokalaemia-induced ventricular arrhythmia through novel multi-channel effects. Br J Pharmacol. 2022 Jun;179(11):2713-2732. doi: 10.1111/bph.15775. Epub 2022 Feb 4. PMID: 34877651. 4: Chakraborty AD, Gonano LA, Munro ML, Smith LJ, Thekkedam C, Staudacher V, Gamble AB, Macquaide N, Dulhunty AF, Jones PP. Activation of RyR2 by class I kinase inhibitors. Br J Pharmacol. 2019 Mar;176(6):773-786. doi: 10.1111/bph.14562. Epub 2019 Jan 30. PMID: 30588601; PMCID: PMC6393232. 5: Gonano LA, Sepúlveda M, Morell M, Toteff T, Racioppi MF, Lascano E, Negroni J, Fernández Ruocco MJ, Medei E, Neiman G, Miriuka SG, Back TG, Chen SRW, Mattiazzi A, Vila Petroff M. Non-β-Blocking Carvedilol Analog, VK-II-86, Prevents Ouabain-Induced Cardiotoxicity. Circ J. 2018 Dec 25;83(1):41-51. doi: 10.1253/circj.CJ-18-0247. Epub 2018 Oct 23. PMID: 30369562. 6: Morgan AJ, Bampali K, Ruas M, Factor C, Back TG, Chen SRW, Galione A. Carvedilol inhibits cADPR- and IP3-induced Ca2+ release. Messenger (Los Angel). 2016 Jun 1;5(1-2):92-99. doi: 10.1166/msr.2016.1050. PMID: 28758053; PMCID: PMC5531262. 7: Zhou Q, Xiao J, Jiang D, Wang R, Vembaiyan K, Wang A, Smith CD, Xie C, Chen W, Zhang J, Tian X, Jones PP, Zhong X, Guo A, Chen H, Zhang L, Zhu W, Yang D, Li X, Chen J, Gillis AM, Duff HJ, Cheng H, Feldman AM, Song LS, Fill M, Back TG, Chen SR. Carvedilol and its new analogs suppress arrhythmogenic store overload- induced Ca2+ release. Nat Med. 2011 Jul 10;17(8):1003-9. doi: 10.1038/nm.2406. PMID: 21743453; PMCID: PMC3268079.