Mozavaptan free base
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MedKoo CAT#: 100949

CAS#: 137975-06-5 (free base)

Description: Mozavaptan, also known as OPC 31260, is a vasopressin receptor antagonist marketed by Otsuka. In Japan, it was approved in October 2006 for hyponatremia (low blood sodium levels) caused by syndrome of inappropriate antidiuretic hormone (SIADH) due to ADH producing tumors.


Price and Availability

Size Price Shipping out time Quantity
50mg USD 150 2 Weeks
100mg USD 250 2 Weeks
200mg USD 450 2 Weeks
500mg USD 1050 2 Weeks
1g USD 1950 2 Weeks
2g USD 2950 2 Weeks
5g USD 4950 2 Weeks
10g USD 7850 2 Weeks
20g USD 12550 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-31. Prices are subject to change without notice.

Mozavaptan free base, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 100949
Name: Mozavaptan free base
CAS#: 137975-06-5 (free base)
Chemical Formula: C27H29N3O2
Exact Mass: 427.226
Molecular Weight: 427.548
Elemental Analysis: C, 75.85; H, 6.84; N, 9.83; O, 7.48


Related CAS #: 138470-70-9 (HCl)   137975-06-5 (free base)    

Synonym: OPC-31260; OPC 31260; OPC31260; Mozavaptan.

IUPAC/Chemical Name: N-(4-(5-(dimethylamino)-2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl)phenyl)-2-methylbenzamide

InChi Key: WRNXUQJJCIZICJ-UHFFFAOYSA-N

InChi Code: InChI=1S/C27H29N3O2/c1-19-9-4-5-10-22(19)26(31)28-21-16-14-20(15-17-21)27(32)30-18-8-13-24(29(2)3)23-11-6-7-12-25(23)30/h4-7,9-12,14-17,24H,8,13,18H2,1-3H3,(H,28,31)

SMILES Code: O=C(NC1=CC=C(C(N2C3=CC=CC=C3C(N(C)C)CCC2)=O)C=C1)C4=CC=CC=C4C


Technical Data

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


References

1: Yamazaki T, Fukata A, Muraki Y. Imidafenacin exerts the antidiuretic effect by enhancing vasopressin-related responses in orally water-loaded rats. Eur J Pharmacol. 2016 Nov 15;791:72-77. doi: 10.1016/j.ejphar.2016.08.021. PubMed PMID: 27568834.

2: Sharif SA, Calder ED, Delolo FG, Sutherland A. Synthesis of 5-Amino-2,5-dihydro-1H-benzo[b]azepines Using a One-Pot Multibond Forming Process. J Org Chem. 2016 Aug 5;81(15):6697-706. doi: 10.1021/acs.joc.6b01357. PubMed PMID: 27414232.

3: Tabata K, Nishimura Y, Takeda T, Kurita M, Uchiyama T, Suzuki T. Sesquiterpene lactones derived from Saussurea lappa induce apoptosis and inhibit invasion and migration in neuroblastoma cells. J Pharmacol Sci. 2015 Apr;127(4):397-403. doi: 10.1016/j.jphs.2015.01.002. PubMed PMID: 25953266.

4: Verbalis JG, Grossman A, Höybye C, Runkle I. Review and analysis of differing regulatory indications and expert panel guidelines for the treatment of hyponatremia. Curr Med Res Opin. 2014 Jul;30(7):1201-7. doi: 10.1185/03007995.2014.920314. Review. PubMed PMID: 24809970.

5: Izumi Y, Miura K, Iwao H. Therapeutic potential of vasopressin-receptor antagonists in heart failure. J Pharmacol Sci. 2014;124(1):1-6. Review. PubMed PMID: 24401675.

6: Roix J, Saha S. TNF-α blockade is ineffective in animal models of established polycystic kidney disease. BMC Nephrol. 2013 Oct 25;14:233. doi: 10.1186/1471-2369-14-233. PubMed PMID: 24160989; PubMed Central PMCID: PMC4231369.

7: Tamura T, Takeuchi K. Small cell gall bladder carcinoma complicated by syndrome of inappropriate secretion of antidiuretic hormone (SIADH) treated with mozavaptan. BMJ Case Rep. 2013 Jun 11;2013. pii: bcr2013010039. doi: 10.1136/bcr-2013-010039. PubMed PMID: 23761568; PubMed Central PMCID: PMC3702909.

8: Dabrowska MD, Krysiak R, Okopień B. [Hyponatremic hypervolemia in heart failure--the hot spot for vasopressin receptor antagonists?]. Wiad Lek. 2012;65(1):19-30. Review. Polish. PubMed PMID: 22827112.

9: Takahashi K, Makita N, Manaka K, Hisano M, Akioka Y, Miura K, Takubo N, Iida A, Ueda N, Hashimoto M, Fujita T, Igarashi T, Sekine T, Iiri T. V2 vasopressin receptor (V2R) mutations in partial nephrogenic diabetes insipidus highlight protean agonism of V2R antagonists. J Biol Chem. 2012 Jan 13;287(3):2099-106. doi: 10.1074/jbc.M111.268797. PubMed PMID: 22144672; PubMed Central PMCID: PMC3265889.

10: Devuyst O, Wang X, Serra A. Vasopressin-2 receptor antagonists in autosomal dominant polycystic kidney disease: from man to mouse and back. Nephrol Dial Transplant. 2011 Aug;26(8):2423-5. doi: 10.1093/ndt/gfr380. PubMed PMID: 21803730.

11: Meijer E, Gansevoort RT, de Jong PE, van der Wal AM, Leonhard WN, de Krey SR, van den Born J, Mulder GM, van Goor H, Struck J, de Heer E, Peters DJ. Therapeutic potential of vasopressin V2 receptor antagonist in a mouse model for autosomal dominant polycystic kidney disease: optimal timing and dosing of the drug. Nephrol Dial Transplant. 2011 Aug;26(8):2445-53. doi: 10.1093/ndt/gfr069. PubMed PMID: 21393612.

12: Villabona C. [Vasopressin receptor antagonists: the vaptans]. Endocrinol Nutr. 2010 May;57 Suppl 2:41-52. doi: 10.1016/S1575-0922(10)70021-8. Review. Spanish. PubMed PMID: 21130961.

13: Ectopic ADH Syndrome Therapeutic Research Group., Yamaguchi K, Shijubo N, Kodama T, Mori K, Sugiura T, Kuriyama T, Kawahara M, Shinkai T, Iguchi H, Sakurai M. Clinical implication of the antidiuretic hormone (ADH) receptor antagonist mozavaptan hydrochloride in patients with ectopic ADH syndrome. Jpn J Clin Oncol. 2011 Jan;41(1):148-52. doi: 10.1093/jjco/hyq170. PubMed PMID: 21087977.

14: Takada M, Fujimaki-Aoba K, Hokari S. Vasotocin- and mesotocin-induced increases in short-circuit current across tree frog skin. J Comp Physiol B. 2011 Feb;181(2):239-48. doi: 10.1007/s00360-010-0523-5. PubMed PMID: 20981549.

15: Nishimura M, Kakigi A, Takeda T, Okada T, Doi K. Bumetanide-induced enlargement of the rat intrastrial space and effects of a vasopressin type 2 antagonist. ORL J Otorhinolaryngol Relat Spec. 2010;71 Suppl 1:10-5. doi: 10.1159/000265114. PubMed PMID: 20185944.

16: Takeda T, Takeda S, Kakigi A, Okada T, Nishioka R, Taguchi D, Nishimura M, Nakatani H. Hormonal aspects of Ménière's disease on the basis of clinical and experimental studies. ORL J Otorhinolaryngol Relat Spec. 2010;71 Suppl 1:1-9. doi: 10.1159/000265113. Review. PubMed PMID: 20185943.

17: Takada M, Fujimaki-Aoba K, Hokari S. Effects of arginine vasotocin and mesotocin on the activation and development of amiloride-blockable short-circuit current across larval, adult, and cultured larval bullfrog skins. J Comp Physiol B. 2010 Mar;180(3):393-402. doi: 10.1007/s00360-009-0424-7. PubMed PMID: 19949800.

18: Yeung PK, Lo AC, Leung JW, Chung SS, Chung SK. Targeted overexpression of endothelin-1 in astrocytes leads to more severe cytotoxic brain edema and higher mortality. J Cereb Blood Flow Metab. 2009 Dec;29(12):1891-902. doi: 10.1038/jcbfm.2009.175. PubMed PMID: 19707218.

19: Shibata H. [Treatment for the electrolytic disorders in cancer patients]. Gan To Kagaku Ryoho. 2008 Dec;35(13):2330-3. Japanese. PubMed PMID: 19098400.

20: Bie P, Mølstrøm S, Wamberg S. Normotensive sodium loading in conscious dogs: regulation of renin secretion during beta-receptor blockade. Am J Physiol Regul Integr Comp Physiol. 2009 Feb;296(2):R428-35. doi: 10.1152/ajpregu.90753.2008. PubMed PMID: 19073902.