VAS3947 | CAS#869853-70-3 | NADPH inhibitor

MedKoo Cat#: 526646 | Name: VAS3947

Description:

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

VAS3947 is a selective inhibitor of NADPH oxidase activity in low micromolar concentrations, interfering neither with ROS detection nor with XOD or eNOS activities. VAS3947 induces apoptosis in AML cells independently of its anti-NOX activity. VAS3947 thiol alkylates cysteine residues of glutathione (GSH), while also interacting with proteins. Remarkably, VAS3947 decreased detectable GSH in the MV-4-11 cell line, thereby suggesting possible oxidative stress induction. Overall, VAS3947 induces apoptosis independently of anti-NOX activity, via UPR activation, mainly due to aggregation and misfolding of proteins.

Chemical Structure

VAS3947

CAS#869853-70-3

Theoretical Analysis

MedKoo Cat#: 526646

Name: VAS3947

CAS#: 869853-70-3

Chemical Formula: C14H10N6OS

Exact Mass: 310.0637

Molecular Weight: 310.34

Elemental Analysis: C, 54.18; H, 3.25; N, 27.08; O, 5.16; S, 10.33

Price and Availability

Size	Price	Availability
10mg	USD 150.00	Ready to ship
25mg	USD 250.00	Ready to ship
50mg	USD 450.00	Ready to ship
100mg	USD 750.00	Ready to ship
200mg	USD 1,350.00	Ready to ship
500mg	USD 2,650.00	Ready to ship

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Related CAS #

No Data

Synonym

VA-S3947; VA S3947; VAS3947

IUPAC/Chemical Name

3-Benzyl-7-(2-oxazolyl)thio-1,2,3-triazolo[4,5-d]pyrimidine

InChi Key

JVZDLDFNSCFLPM-UHFFFAOYSA-N

InChi Code

InChI=1S/C14H10N6OS/c1-2-4-10(5-3-1)8-20-12-11(18-19-20)13(17-9-16-12)22-14-15-6-7-21-14/h1-7,9H,8H2

SMILES Code

C12=NC=NC(SC3=NC=CO3)=C1N=NN2CC4=CC=CC=C4

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

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

Certificate of Analysis

View CoA: current batch, Lot#S22S01C12

QC Data

View QC data: current batch, Lot#S22S01C12

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

VAS 3947, a specific NADPH oxidase (NOX) inhibitor, exerts a potent antiplatelet effect that induces apoptosis independently of anti-NOX activity, via UPR activation, mainly due to aggregation and misfolding of proteins.

In vitro activity:

To determine the cytotoxic effects of VAS3947, eight AML cell lines, covering M0 to M5 stages of the French–American–British (FAB) classification, were treated with increasing concentrations (0.5 µM to 20 µM) of this inhibitor for 72 h. An average dose of 4 µM VAS3947 was chosen for the following experiments. After only 1 day-exposure at this concentration, all cell lines showed reduced cell numbers compared to their corresponding controls, and the difference increased over time. The VAS3947-induced decrease in cell proliferation was mostly explained by apoptosis for KG-1a, KG-1, ML-2, and MV-4-11 cells. The absence of NOX activity in THP-1 and its induction by phorbol 12-myristate 13-acetate (PMA) was confirmed, which, however, is efficiently inhibited by VAS3947. Thus, VAS3947 reduces cell growth and induces cell death in the absence of NOX activity, thereby suggesting possible off-target effects. Reference: Int J Mol Sci. 2020 Jul 31;21(15):5470. https://pubmed.ncbi.nlm.nih.gov/32751795/ To determine the cytotoxic effects of VAS3947, eight AML cell lines, covering M0 to M5 stages of the French–American–British (FAB) classification, were treated with increasing concentrations (0.5 µM to 20 µM) of this inhibitor for 72 h. An average dose of 4 µM VAS3947 was chosen for the following experiments. After only 1 day-exposure at this concentration, all cell lines showed reduced cell numbers compared to their corresponding controls, and the difference increased over time. The VAS3947-induced decrease in cell proliferation was mostly explained by apoptosis for KG-1a, KG-1, ML-2, and MV-4-11 cells. The absence of NOX activity in THP-1 and its induction by phorbol 12-myristate 13-acetate (PMA) was confirmed, which, however, is efficiently inhibited by VAS3947. Thus, VAS3947 reduces cell growth and induces cell death in the absence of NOX activity, thereby suggesting possible off-target effects. Reference: Int J Mol Sci. 2020 Jul 31;21(15):5470. https://pubmed.ncbi.nlm.nih.gov/32751795/

In vivo activity:

TBD

	Solvent	mg/mL	mM
Solubility
	DMSO	100.0	322.24

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 310.34 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.

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. El Dor M, Dakik H, Polomski M, Haudebourg E, Brachet M, Gouilleux F, Prié G, Zibara K, Mazurier F. VAS3947 Induces UPR-Mediated Apoptosis through Cysteine Thiol Alkylation in AML Cell Lines. Int J Mol Sci. 2020 Jul 31;21(15):5470. doi: 10.3390/ijms21155470. PMID: 32751795; PMCID: PMC7432790. 2. Wind S, Beuerlein K, Eucker T, Müller H, Scheurer P, Armitage ME, Ho H, Schmidt HH, Wingler K. Comparative pharmacology of chemically distinct NADPH oxidase inhibitors. Br J Pharmacol. 2010 Oct;161(4):885-98. doi: 10.1111/j.1476-5381.2010.00920.x. PMID: 20860666; PMCID: PMC2970907.

In vitro protocol:

In vivo protocol:

TBD

1: Szczepanska-Sadowska E, Cudnoch-Jędrzejewska A, Żera T. Molecular Interaction Between Vasopressin and Insulin in Regulation of Metabolism: Impact on Cardiovascular and Metabolic Diseases. Int J Mol Sci. 2024 Dec 11;25(24):13307. doi: 10.3390/ijms252413307. PMID: 39769071. 2: Kato H, Mathis BJ, Shimoda T, Nakajima T, Tokunaga C, Hiramatsu Y. Hemodynamic Management with Vasopressin for Cardiovascular Surgery. Medicina (Kaunas). 2024 Dec 16;60(12):2064. doi: 10.3390/medicina60122064. PMID: 39768943. 3: Mielnicki W, Dyla A, Zając M, Rokicka-Demitraszek N, Smereka J. Does Continuous Renal Replacement Therapy with oXiris in Septic Shock Have Any Positive Impact? Single-Centre Experience with oXiris Therapy in Septic Shock Patients. J Clin Med. 2024 Dec 11;13(24):7527. doi: 10.3390/jcm13247527. PMID: 39768450. 4: Kakeshita K, Imamura T, Hida Y, Onoda H, Koike T, Kinugawa K. Trajectory of Urine Parameters by Adding Herbal Kampo Medicine Goreisan to Tolvaptan in Patients with Congestive Heart Failure. J Clin Med. 2024 Dec 11;13(24):7523. doi: 10.3390/jcm13247523. PMID: 39768446. 5: Chaudhry A, O'Reilly M, Ramsie M, Lee TF, Cheung PY, Schmölzer GM. Effect of vasopressin on brain and cardiac tissue during neonatal cardiopulmonary resuscitation of asphyxiated post-transitional piglets. Resusc Plus. 2024 Dec 14;21:100837. doi: 10.1016/j.resplu.2024.100837. PMID: 39758757; PMCID: PMC11699340. 6: Jalilzadeh Khalet Abad S, Kalashipour Chir G, Heydari P, Fazilat A, Mortazavi Moghadam F, Valilo M. Hormonal disorders in autism spectrum disorders. Horm Mol Biol Clin Investig. 2025 Jan 6. doi: 10.1515/hmbci-2024-0078. Epub ahead of print. PMID: 39752633. 7: Van Nynatten LR, Patel MA, Daley M, Miller MR, Cepinskas G, Slessarev M, Russell JA, Fraser DD. Putative biomarkers of hepatic dysfunction in critically ill sepsis patients. Clin Exp Med. 2025 Jan 3;25(1):28. doi: 10.1007/s10238-024-01545-3. PMID: 39751971; PMCID: PMC11698781. 8: Salcedo-Sifuentes JE, Shih R, Heaney AP, Bergsneider M, Wang MB, Donangelo I, Lee J, Delery W, Karsy M, Kshettry VR, Yuen KCJ, Evans JJ, Barkhoudarian G, Pacione DR, Gardner PA, Fernandez-Miranda JC, Benjamin C, Zada G, Rennert RC, Silverstein JM, Chicoine MR, Kim J, Li G, Little AS, Kim W. Cushing's Disease Clinical Phenotype and Tumor Behavior Vary with Age: Diagnostic and Perioperative Implications. J Clin Endocrinol Metab. 2025 Jan 2:dgae904. doi: 10.1210/clinem/dgae904. Epub ahead of print. PMID: 39745928. 9: Ansari Z, Ahmad A, Khan OS, Reddi V, Castro F. Safety of Colonoscopies in Patients on Advanced Heart Failure Therapies Who Received a Heart Transplant. JGH Open. 2024 Dec 30;9(1):e70090. doi: 10.1002/jgh3.70090. PMID: 39742151; PMCID: PMC11683780. 10: Li L, Ge W, Zhang W, Xu Z, Xu F, Wang Y. Arginine vasopressin and angiotensin II coregulate Aquaporin 2 expression in M-1 cells. Biochem Biophys Res Commun. 2025 Jan;745:151256. doi: 10.1016/j.bbrc.2024.151256. Epub 2024 Dec 28. PMID: 39740402. 11: Kotani Y, Belletti A, D'Amico F, Bonaccorso A, Wieruszewski PM, Fujii T, Khanna AK, Landoni G, Bellomo R. Non-adrenergic vasopressors for vasodilatory shock or perioperative vasoplegia: a meta-analysis of randomized controlled trials. Crit Care. 2024 Dec 30;28(1):439. doi: 10.1186/s13054-024-05212-7. PMID: 39736782; PMCID: PMC11686893. 12: Mińczuk K, Schlicker E, Krzyżewska A, Malinowska B. Angiotensin 1-7 injected into the rat paraventricular nucleus of hypothalamus increases blood pressure and heart rate via various receptors. Neuropharmacology. 2024 Dec 26;266:110279. doi: 10.1016/j.neuropharm.2024.110279. Epub ahead of print. PMID: 39732324. 13: Yamamoto A, Komatsu N, Iwata N, Fujisawa H, Suzuki A, Sugimura Y. A 4-year- old Boy Positive for Anti-rabphilin-3A Antibody and Diagnosed With Lymphocytic Infundibuloneurohypophysitis. JCEM Case Rep. 2024 Dec 26;3(1):luae214. doi: 10.1210/jcemcr/luae214. PMID: 39726668; PMCID: PMC11669861. 14: Roach B, Greene ES, Dridi S. Central regulation of drinking water in divergently selected high-water-efficient young broiler chickens: A minireview. J Neuroendocrinol. 2024 Dec 26:e13488. doi: 10.1111/jne.13488. Epub ahead of print. PMID: 39726215. 15: Galbiati F, Becetti I, Lauze M, Aulinas A, Singhal V, Bredella MA, Lawson EA, Misra M. Increased copeptin may reflect vasopressin-related metabolic changes after bariatric surgery. Obesity (Silver Spring). 2024 Dec 26. doi: 10.1002/oby.24200. Epub ahead of print. PMID: 39725569. 16: Balachandran A, Mishra RK, Effie AO, Raghunathan A, Mathew A, Archana S. A systematic review and meta-analysis of efficacy of vasopressin as a vasoconstrictive and uterotonic drug in laparoscopic myomectomy. J Minim Access Surg. 2024 Oct 1;20(4):363-372. doi: 10.4103/jmas.jmas_272_23. Epub 2024 Oct 9. PMID: 39724600; PMCID: PMC11601973. 17: Sorath F. The Underutilization of Urea in the Treatment of SIADH - An Efficacious but Overlooked Solution. Cureus. 2024 Nov 22;16(11):e74265. doi: 10.7759/cureus.74265. PMID: 39717291; PMCID: PMC11666293. 18: Thwaites L, Nasa P, Abbenbroek B, Dat VQ, Finfer S, Kwizera A, Ling L, Lobo SM, Sinto R, Aditianingsih D, Antonelli M, Arabi YM, Argent A, Azevedo L, Bennett E, Chakrabarti A, De Asis K, De Waele J, Divatia JV, Estenssoro E, Evans L, Faiz A, Hammond NE, Hashmi M, Herridge MS, Jacob ST, Jatsho J, Javeri Y, Khalid K, Chen LK, Levy M, Lundeg G, Machado FR, Mehta Y, Mer M, Son DN, Ospina- Tascón GA, Ostermann M, Permpikul C, Prescott HC, Reinhart K, Rodriguez Vega G, S-Kabara H, Shrestha GS, Waweru-Siika W, Tan TL, Todi S, Tripathy S, Venkatesh B, Vincent JL, Myatra SN. Management of adult sepsis in resource-limited settings: global expert consensus statements using a Delphi method. Intensive Care Med. 2024 Dec 23. doi: 10.1007/s00134-024-07735-7. Epub ahead of print. PMID: 39714613. 19: Isaacs JT, Almeter PJ, Hunter AN, Lyman TA, Zapata SP, Henderson BS, Larkin SA, Plymale AR, Long LM, Bossle MN, Bhaktawara SA, Warren MF, Lozier AM, Melson JD, Fraley SR, Relucio EHL, Felix MA, Reynolds JW, Naseman RW, Puerto DA, Lodder RA. Potential Process Control Issues with Vasopressin. Contact Context. 2024;2024:10.6084/m9.figshare.27669543. doi: 10.6084/m9.figshare.27669543. PMID: 39713721; PMCID: PMC11661826. 20: Gumerova A, Pevnev G, Korkmaz F, Cheliadinova U, Burganova G, Vasilyeva D, Cullen L, Barak O, Sultana F, Zhou W, Sims S, Laurencin V, Frolinger T, Kim SM, Goosens KA, Yuen T, Zaidi M, Ryu V. Gender-specific Single Transcript Level Atlas of Vasopressin and its Receptor (AVPR1a) in the Mouse Brain. bioRxiv [Preprint]. 2024 Dec 10:2024.12.09.627541. doi: 10.1101/2024.12.09.627541. PMID: 39713333; PMCID: PMC11661174.