WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H124976
CAS#: 2025360-90-9 (free base)
Description: Arazasetron is an antiemetic which acts as a 5-HT3 receptor antagonist, pKi = 9.27.
Hodoodo Cat#: H124976
Name: Arazasetron
CAS#: 2025360-90-9 (free base)
Chemical Formula: C17H20ClN3O3
Exact Mass: 349.12
Molecular Weight: 349.820
Elemental Analysis: C, 58.37; H, 5.76; Cl, 10.13; N, 12.01; O, 13.72
This product is not in stock, which may be available by custom synthesis.
For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge).
Quote less than 1g will not be provided. To request quote, please email to sales @hodoodo.com or click below button.
Note: Price will be listed if it is available in the future.
Related CAS #: 123040-69-7 (HCl) 2025360-90-9 (free base) 2025360-91-0 (besylate)
Synonym: R-Azasetron; Azasetron, R; 61JC7L0Q4O; 2025360-90-9; UNII-61JC7L0Q4O
IUPAC/Chemical Name: N-[(3R)-1-azabicyclo[2.2.2]octan-3-yl]-6-chloro-4-methyl-3-oxo-1,4-benzoxazine-8-carboxamide
InChi Key: WUKZPHOXUVCQOR-ZDUSSCGKSA-N
InChi Code: InChI=1S/C17H20ClN3O3/c1-20-14-7-11(18)6-12(16(14)24-9-15(20)22)17(23)19-13-8-21-4-2-10(13)3-5-21/h6-7,10,13H,2-5,8-9H2,1H3,(H,19,23)/t13-/m0/s1
SMILES Code: O=C(C1=C(OCC(N2C)=O)C2=CC(Cl)=C1)N[C@H]3CN4CCC3CC4
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:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 349.82 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: | |
| In vivo protocol: |
1: Fang BX, Chen FC, Zhu D, Guo J, Wang LH. Stability of azasetron-dexamethasone mixture for chemotherapy-induced nausea and vomiting administration. Oncotarget. 2017 Oct 31;8(63):106249-106257. doi: 10.18632/oncotarget.22174. eCollection 2017 Dec 5. PubMed PMID: 29290945; PubMed Central PMCID: PMC5739730.
2: Petremann M, Tran Van Ba C, Broussy A, Romanet C, Dyhrfjeld-Johnsen J. Oral Administration of Clinical Stage Drug Candidate SENS-401 Effectively Reduces Cisplatin-induced Hearing Loss in Rats. Otol Neurotol. 2017 Oct;38(9):1355-1361. doi: 10.1097/MAO.0000000000001546. PubMed PMID: 28796092.
3: Kaito D, Iihara H, Funaguchi N, Endo J, Ito F, Yanase K, Toyoshi S, Sasaki Y, Hirose C, Arai N, Kitahora M, Ohno Y, Itoh Y, Minatoguchi S. Efficacy of Single-dose First-generation 5-HT(3) Receptor Antagonist and Dexamethasone for Preventing Nausea and Vomiting Induced by Low-dose Carboplatin-based Chemotherapy. Anticancer Res. 2017 Apr;37(4):1965-1970. PubMed PMID: 28373467.
4: Koshiyama M, Matsumura N, Imai S, Yamanoi K, Abiko K, Yoshioka Y, Yamaguchi K, Hamanishi J, Baba T, Konishi I. Combination of Aprepitant, Azasetron, and Dexamethasone as Antiemetic Prophylaxis in Women with Gynecologic Cancers Receiving Paclitaxel/Carboplatin Therapy. Med Sci Monit. 2017 Feb 15;23:826-833. PubMed PMID: 28198358; PubMed Central PMCID: PMC5322867.
5: Chen FC, Wang LH, Guo J, Shi XY, Fang BX. Simultaneous Determination of Dexamethasone, Ondansetron, Granisetron, Tropisetron, and Azasetron in Infusion Samples by HPLC with DAD Detection. J Anal Methods Chem. 2017;2017:6749087. doi: 10.1155/2017/6749087. Epub 2017 Jan 11. PubMed PMID: 28168082; PubMed Central PMCID: PMC5266853.
6: Tanaka T, Ago Y, Umehara C, Imoto E, Hasebe S, Hashimoto H, Takuma K, Matsuda T. Role of Prefrontal Serotonergic and Dopaminergic Systems in Encounter-Induced Hyperactivity in Methamphetamine-Sensitized Mice. Int J Neuropsychopharmacol. 2017 May 1;20(5):410-421. doi: 10.1093/ijnp/pyw115. PubMed PMID: 28034961; PubMed Central PMCID: PMC5417057.
7: Han Z, Sun X, Jiang G, Du X. Thalidomide for Control Delayed Vomiting in Cancer Patients Receiving Chemotherapy. J Coll Physicians Surg Pak. 2016 Nov;26(11):900-903. PubMed PMID: 27981924.
8: Sandor ZI, Bencsik T, Dekany A, Bartho L. Serotonin or the Mucosa Do Not Mediate the Motor Effect of Allyl Isothiocyanate in the Guinea-Pig Small Intestine. Pharmacology. 2016;98(5-6):199-203. Epub 2016 Jun 24. PubMed PMID: 27336729.
9: Hashizume J, Higuchi N, Sato K, Kodama Y, Matsunaga N, Sakamoto T, Yamaguchi K, Nakamura T, Kitahara T, Sasaki H. Evaluation of Antiemetic Therapy for Hepatic Transcatheter Arterial Infusion Chemotherapy with Cisplatin. Biol Pharm Bull. 2016;39(4):611-4. doi: 10.1248/bpb.b15-00603. PubMed PMID: 27040634.
10: Ahmadi-Mahmoodabadi N, Nasehi M, Emam Ghoreishi M, Zarrindast MR. Synergistic effect between prelimbic 5-HT3 and CB1 receptors on memory consolidation deficit in adult male Sprague-Dawley rats: An isobologram analysis. Neuroscience. 2016 Mar 11;317:173-83. doi: 10.1016/j.neuroscience.2015.12.010. Epub 2015 Dec 14. PubMed PMID: 26701293.
11: Hasebe S, Ago Y, Nishiyama S, Oka S, Hashimoto H, Takuma K, Matsuda T. Pharmacological profile of encounter-induced hyperactivity in isolation-reared mice. Behav Pharmacol. 2015 Oct;26(7 Spec No):681-90. doi: 10.1097/FBP.0000000000000140. PubMed PMID: 25932719.
12: Nasehi M, Kafi F, Khakpai F, Zarrindast MR. Involvement of the serotonergic system of the ventral hippocampus (CA3) on amnesia induced by ACPA in mice. Behav Brain Res. 2015 Jun 1;286:356-63. doi: 10.1016/j.bbr.2015.03.011. Epub 2015 Mar 11. PubMed PMID: 25771207.
13: Liu J, Tan L, Zhang H, Li H, Liu X, Yan Z, Chen J, Yang H, Zhang D. QoL evaluation of olanzapine for chemotherapy-induced nausea and vomiting comparing with 5-HT3 receptor antagonist. Eur J Cancer Care (Engl). 2015 May;24(3):436-43. doi: 10.1111/ecc.12260. Epub 2014 Nov 18. PubMed PMID: 25404537.
14: Lee HY, Kim HK, Lee KH, Kim BS, Song HS, Yang SH, Kim JH, Kim YH, Kim JG, Kim SW, Kim DW, Kim SY, Park HS. A Randomized Double-Blind, Double-Dummy, Multicenter Trial of Azasetron versus Ondansetron to Evaluate Efficacy and Safety in the Prevention of Delayed Nausea and Vomiting Induced by Chemotherapy. Cancer Res Treat. 2014 Jan;46(1):19-26. doi: 10.4143/crt.2014.46.1.19. Epub 2014 Jan 15. PubMed PMID: 24520219; PubMed Central PMCID: PMC3918522.
15: Nakamura H, Yokoyama H, Takayanagi R, Yoshimoto K, Nakajima A, Okuyama K, Iwase O, Yamada Y. Theoretical evaluation of antiemetic effects of 5-HT3 receptor antagonists for prevention of vomiting induced by cisplatin. Eur J Drug Metab Pharmacokinet. 2015 Mar;40(1):39-44. doi: 10.1007/s13318-014-0175-z. Epub 2014 Jan 28. PubMed PMID: 24470169.
16: Bell R, Duke AA, Gilmore PE, Page D, Bègue L. Anxiolytic-like effects observed in rats exposed to the elevated zero-maze following treatment with 5-HT2/5-HT3/5-HT4 ligands. Sci Rep. 2014 Jan 24;4:3881. doi: 10.1038/srep03881. PubMed PMID: 24457553; PubMed Central PMCID: PMC5379192.
17: Hiramatsu N, Ago Y, Hasebe S, Nishimura A, Mori K, Takuma K, Matsuda T. Synergistic effect of 5-HT1A and σ1 receptor activation on prefrontal dopaminergic transmission under circulating steroid deficiency. Neuropharmacology. 2013 Dec;75:53-61. doi: 10.1016/j.neuropharm.2013.06.026. Epub 2013 Jul 9. PubMed PMID: 23851260.
18: Endo J, Iihara H, Yamada M, Yanase K, Kamiya F, Ito F, Funaguchi N, Ohno Y, Minatoguchi S, Itoh Y. A randomized controlled non-inferiority study comparing the antiemetic effect between intravenous granisetron and oral azasetron based on estimated 5-HT3 receptor occupancy. Anticancer Res. 2012 Sep;32(9):3939-47. PubMed PMID: 22993341.
19: Sun L, Cun D, Yuan B, Cui H, Xi H, Mu L, Chen Y, Liu C, Wang Z, Fang L. Formulation and in vitro/in vivo correlation of a drug-in-adhesive transdermal patch containing azasetron. J Pharm Sci. 2012 Dec;101(12):4540-8. doi: 10.1002/jps.23317. Epub 2012 Sep 12. PubMed PMID: 22972714.
20: Ortega JE, Mendiguren A, Pineda J, Meana JJ. Regulation of central noradrenergic activity by 5-HT(3) receptors located in the locus coeruleus of the rat. Neuropharmacology. 2012 Jun;62(8):2472-9. doi: 10.1016/j.neuropharm.2012.02.018. Epub 2012 Mar 1. PubMed PMID: 22401957.
