Tolvaptan | CAS#150683-30-0 | vasopressin receptor 2 antagonist

MedKoo Cat#: 317142 | Name: Tolvaptan

Description:

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

Tolvaptan is a selective, competitive vasopressin receptor 2 antagonist used to treat hyponatremia (low blood sodium levels) associated with congestive heart failure, cirrhosis, and the syndrome of inappropriate antidiuretic hormone (SIADH). Tolvaptan was approved by the U.S. Food and Drug Administration (FDA) on May 19, 2009.

Chemical Structure

Tolvaptan

CAS#150683-30-0

Theoretical Analysis

MedKoo Cat#: 317142

Name: Tolvaptan

CAS#: 150683-30-0

Chemical Formula: C26H25ClN2O3

Exact Mass: 448.1554

Molecular Weight: 448.95

Elemental Analysis: C, 69.56; H, 5.61; Cl, 7.90; N, 6.24; O, 10.69

Price and Availability

Size	Price	Availability
10mg	USD 90.00	Ready to ship
25mg	USD 150.00	Ready to ship
50mg	USD 250.00	Ready to ship
100mg	USD 450.00	2 Weeks
200mg	USD 750.00	2 Weeks
500mg	USD 1,650.00	2 Weeks
1g	USD 2,950.00	2 Weeks
2g	USD 5,250.00	2 Weeks

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Related CAS #

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Synonym

OPC-41061; OPC 41061; OPC41061; Tolvaptan; trade names Samsca; Jinarc; Resodim.

IUPAC/Chemical Name

N-[4-[(7-chloro-2,3,4,5-tetrahydro-5-hydroxy-1H-1-benzazepin-1-yl)carbonyl]-3-methylphenyl]-2-methyl-benzamide

InChi Key

GYHCTFXIZSNGJT-UHFFFAOYSA-N

InChi Code

InChI=1S/C26H25ClN2O3/c1-16-6-3-4-7-20(16)25(31)28-19-10-11-21(17(2)14-19)26(32)29-13-5-8-24(30)22-15-18(27)9-12-23(22)29/h3-4,6-7,9-12,14-15,24,30H,5,8,13H2,1-2H3,(H,28,31)

SMILES Code

O=C(NC1=CC=C(C(N2CCCC(O)C3=CC(Cl)=CC=C32)=O)C(C)=C1)C4=CC=CC=C4C

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

Certificate of Analysis

View CoA: current batch, Lot#C24S11C29

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

V2 Receptor

In vitro activity:

After intravenous administration of OPC-61815 to rats and dogs, tolvaptan was detected in plasma within 5 min and the bioavailability of tolvaptan was 57.7% and 50.9%, respectively. Binding affinity of OPC-61815 for the human V2 receptor was 1/14 weaker than that of tolvaptan. Reference: Fujiki H, Matsunaga M, Furukawa M, Yamashita T, Nakamura S, Miyazaki T, Mizuguchi H, Menjo Y, Matsuda T, Yamada Y. In vitro and in vivo pharmacological profile of OPC-61815, a water-soluble phosphate ester pro-drug of tolvaptan. J Pharmacol Sci. 2022 Nov;150(3):163-172. doi: 10.1016/j.jphs.2022.08.004. Epub 2022 Aug 28. PMID: 36184121.

In vivo activity:

Further advancing compound 25 in a murine model of ADPKD demonstrated a significantly improved in vivo efficacy compared with the reference compound tolvaptan. Overall, compound 25 holds therapeutic potential for the treatment of ADPKD. Reference: Cao X, Wang P, Yuan H, Zhang H, He Y, Fu K, Fang Q, Liu H, Su L, Yin L, Xu P, Xie Y, Xiong X, Wang J, Zhu X, Guo D. Benzodiazepine Derivatives as Potent Vasopressin V2 Receptor Antagonists for the Treatment of Autosomal Dominant Kidney Disease. J Med Chem. 2022 Jul 14;65(13):9295-9311. doi: 10.1021/acs.jmedchem.2c00567. Epub 2022 May 17. PMID: 35579344.

	Solvent	mg/mL	mM
Solubility
	DMSO	100.0	222.75

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 448.95 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:

In vitro protocol:

1: Fujiki H, Matsunaga M, Furukawa M, Yamashita T, Nakamura S, Miyazaki T, Mizuguchi H, Menjo Y, Matsuda T, Yamada Y. In vitro and in vivo pharmacological profile of OPC-61815, a water-soluble phosphate ester pro-drug of tolvaptan. J Pharmacol Sci. 2022 Nov;150(3):163-172. doi: 10.1016/j.jphs.2022.08.004. Epub 2022 Aug 28. PMID: 36184121. 2: Marroncini G, Anceschi C, Naldi L, Fibbi B, Baldanzi F, Maggi M, Peri A. The V2 receptor antagonist tolvaptan counteracts proliferation and invasivity in human cancer cells. J Endocrinol Invest. 2022 Sep;45(9):1693-1708. doi: 10.1007/s40618-022-01807-5. Epub 2022 May 23. PMID: 35604542; PMCID: PMC9360171.

In vivo protocol:

1: Cao X, Wang P, Yuan H, Zhang H, He Y, Fu K, Fang Q, Liu H, Su L, Yin L, Xu P, Xie Y, Xiong X, Wang J, Zhu X, Guo D. Benzodiazepine Derivatives as Potent Vasopressin V2 Receptor Antagonists for the Treatment of Autosomal Dominant Kidney Disease. J Med Chem. 2022 Jul 14;65(13):9295-9311. doi: 10.1021/acs.jmedchem.2c00567. Epub 2022 May 17. PMID: 35579344. 2: Naldi L, Fibbi B, Polvani S, Cirillo C, Pasella F, Bartolini F, Romano F, Fanelli A, Peri A, Marroncini G. The Vasopressin Receptor Antagonist Tolvaptan Counteracts Tumor Growth in a Murine Xenograft Model of Small Cell Lung Cancer. Int J Mol Sci. 2024 Aug 1;25(15):8402. doi: 10.3390/ijms25158402. PMID: 39125971; PMCID: PMC11313280.

1: 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. 2: Higashihara E, Matsukawa M, Jiang H. Change in kidney volume growth rate and renal outcomes of tolvaptan treatment in autosomal dominant polycystic kidney disease: post-hoc analysis of TEMPO 3:4 trial. Clin Exp Nephrol. 2025 Jan 2. doi: 10.1007/s10157-024-02589-1. Epub ahead of print. PMID: 39747793. 3: 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. 4: Llewellyn DC, Oštarijaš E, Sahadevan S, Nuamek T, Byrne C, Taylor DR, Vincent RP, Dimitriadis GK, Aylwin SJ. Efficacy and safety of low-dose tolvaptan (7.5mg) in the treatment of inpatient hyponatraemia: a retrospective study. Endocr Pract. 2024 Dec 27:S1530-891X(24)00879-6. doi: 10.1016/j.eprac.2024.12.019. Epub ahead of print. PMID: 39733944. 5: Bahlmann-Kroll E, Häckl S, Kramer S, Wulfmeyer VC, Glandorf J, Kaufeld J, Koch A, Hartung D, Schmidt BMW, Schmidt-Ott K, Schmitt R. Empagliflozin in patients with autosomal dominant polycystic kidney disease (EMPA-PKD): study protocol for a randomised controlled trial. BMJ Open. 2024 Dec 15;14(12):e088317. doi: 10.1136/bmjopen-2024-088317. PMID: 39675824; PMCID: PMC11647394. 6: Martínez González Á, González Nunes M, Rodeiro Escobar P, Llópiz Castedo J, Cabaleiro Loureiro A, Martínez Espinosa RP, Ruades Patiño R, Lorenzo Canda G, Aguayo Arjona J, Rodríguez Zorrilla S. Comparative study of the effectiveness of tolvaptan versus urea in patients with hyponatremia caused by SIADH. Rev Clin Esp (Barc). 2024 Dec 3:S2254-8874(24)00155-3. doi: 10.1016/j.rceng.2024.12.001. Epub ahead of print. PMID: 39638091. 7: Chen L, Zhou M, Lv D, Qiu S. Efficacy of Tolvaptan in Older Adults Undergoing Cardiac Surgery: A Single-Center Retrospective Analysis. Braz J Cardiovasc Surg. 2024 Nov 28;e20230507(e20230507):e20230507. doi: 10.21470/1678-9741-2023-0507. PMID: 39607973; PMCID: PMC11606524. 8: Kumar A, Iqbal U, Amin SB, Arsal SA, Ali SMS, Shafique MA, Shahid MS, Naz A, Asuka ES. Evaluating the safety and effectiveness of tolvaptan in patients with heart failure and renal impairment: a systematic review and meta-analysis. Eur J Clin Pharmacol. 2024 Nov 23. doi: 10.1007/s00228-024-03778-3. Epub ahead of print. PMID: 39579178. 9: Yamazaki Y, Niwa H, Ishiyama E, Hori M, Sugo Y, Hirota K. The potential effectiveness of tolvaptan in critically ill patients including cardiac and noncardiac populations: a retrospective observational study. Naunyn Schmiedebergs Arch Pharmacol. 2024 Nov 18. doi: 10.1007/s00210-024-03618-2. Epub ahead of print. PMID: 39556149. 10: Jaeger T, Lohrmann E, Ezenekwe A, Enekebe K, Kumar R, Nunna S, Fernandes AW, McCormick L, George V. Liver safety of tolvaptan in patients with autosomal dominant polycystic kidney disease: interim data from a post-authorization safety study. Clin Kidney J. 2024 Oct 30;17(11):sfae324. doi: 10.1093/ckj/sfae324. PMID: 39530110; PMCID: PMC11551523. 11: Ovalles Lacruz A, Mesa N, Vassil ST, Blanco Guertin A, Sharma D. Delayed Emergence of Isolated Secondary Adrenal Insufficiency: A Case Report. Cureus. 2024 Oct 10;16(10):e71209. doi: 10.7759/cureus.71209. PMID: 39525095; PMCID: PMC11550105. 12: Fouillen A, Couvineau P, Gaibelet G, Riché S, Orcel H, Mendre C, Kanso A, Lanotte R, Nguyen J, Dimon J, Urbach S, Sounier R, Granier S, Bonnet D, Cong X, Mouillac B, Déméné H. Biased activation of the vasopressin V2 receptor probed by molecular dynamics simulations, NMR and pharmacological studies. Comput Struct Biotechnol J. 2024 Oct 24;23:3784-3799. doi: 10.1016/j.csbj.2024.10.039. PMID: 39525085; PMCID: PMC11550766. 13: Suzuki S, Kimura K, Yoda N, Fuchida A, Kanzaki Y, Maruyama T, Hashizume N, Kozuka A, Motoki H, Yahikozawa K, Kuwahara K. Association of Early Tolvaptan Treatment and Length of In Hospital Stay in Elderly Patients with Acute Decompensated Heart Failure. JMA J. 2024 Oct 15;7(4):564-570. doi: 10.31662/jmaj.2024-0050. Epub 2024 Sep 20. PMID: 39513060; PMCID: PMC11543316. 14: Zhou L, Wei X, Wang B, Xu Q, Li W. Low-dose tolvaptan to control disease progression in Chinese patients with autosomal dominant polycystic kidney disease: a retrospective cohort study. Transl Androl Urol. 2024 Oct 31;13(10):2307-2321. doi: 10.21037/tau-24-448. Epub 2024 Oct 28. PMID: 39507867; PMCID: PMC11535741. 15: Hammond S, Meng X, Barber J, Mosedale M, Chadwick A, Watkins PB, Naisbitt DJ. Tolvaptan safety in autosomal-dominant polycystic kidney disease; a focus on idiosyncratic drug-induced liver injury liabilities. Toxicol Sci. 2025 Jan 1;203(1):11-27. doi: 10.1093/toxsci/kfae142. PMID: 39495155; PMCID: PMC11664107. 16: Matsuo T, Tanaka T, Tsuji K. Presumed Choroidopathy of IgG4-Related Disease Discovered During 16-Year Follow-Up of a Patient With Polycystic Kidney Disease. Cureus. 2024 Oct 4;16(10):e70865. doi: 10.7759/cureus.70865. PMID: 39493066; PMCID: PMC11531971. 17: Uno T, Hosomi K, Yokoyama S. Evaluation of tolvaptan-associated hepatic disorder using different national pharmacovigilance databases. Sci Rep. 2024 Oct 29;14(1):25943. doi: 10.1038/s41598-024-77052-y. PMID: 39472632; PMCID: PMC11522566. 18: Subhash S, Vijayvargiya S, Parmar A, Sandhu J, Simmons J, Raina R. Reactive Oxygen Species in Cystic Kidney Disease. Antioxidants (Basel). 2024 Sep 30;13(10):1186. doi: 10.3390/antiox13101186. PMID: 39456439; PMCID: PMC11504974. 19: Yan Y, Li XM, Yang Y, Wang FM, Liu H, Tang RN, Zhang XL, Liu BC, Wang B. Tolvaptan and the role of kidney aquaporin-2 abundance in managing volume overload in patients with CKD. Clin Kidney J. 2024 Oct 4;17(10):sfae303. doi: 10.1093/ckj/sfae303. PMID: 39449995; PMCID: PMC11500452. 20: Honda R, Akazawa Y, Inoue K, Higaki T, Yamaguchi O. A case report: pitfalls in antibacterial therapy with rifampicin for mechanical valve endocarditis-the king of drug interactions. Eur Heart J Case Rep. 2024 Sep 23;8(10):ytae525. doi: 10.1093/ehjcr/ytae525. PMID: 39445105; PMCID: PMC11498049.