WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H120201
CAS#: 147116-67-4 (free base)
Description: Maropitan, also known as CJ 11972, is a neurokinin (NK1) receptor antagonist, which was developed by Zoetis specifically for the treatment of motion sickness and vomiting in dogs. It was approved by the FDA in 2007 for use in dogs, and more recently has also been approved for use in cats.
Hodoodo Cat#: H120201
Name: Maropitant free base
CAS#: 147116-67-4 (free base)
Chemical Formula: C32H40N2O
Exact Mass: 468.31
Molecular Weight: 468.673
Elemental Analysis: C, 82.01; H, 8.60; N, 5.98; O, 3.41
Related CAS #: 862543-54-2 (citrate) 359875-09-5 (citrate hydrate) 147116-67-4 (free base)
Synonym: CJ-11,972; CJ 11,972; CJ11,972; CJ-11972; CJ 11972; CJ11972; Maropitant; brand name: Cerenia
IUPAC/Chemical Name: (1R,2S,3S,4R)-2-benzhydryl-N-(5-(tert-butyl)-2-methoxybenzyl)quinuclidin-3-amine
InChi Key: OMPCVMLFFSQFIX-CONSDPRKSA-N
InChi Code: InChI=1S/C32H40N2O/c1-32(2,3)27-15-16-28(35-4)26(21-27)22-33-30-25-17-19-34(20-18-25)31(30)29(23-11-7-5-8-12-23)24-13-9-6-10-14-24/h5-16,21,25,29-31,33H,17-20,22H2,1-4H3/t30-,31-/m0/s1
SMILES Code: COC1=CC=C(C(C)(C)C)C=C1CN[C@@H]2[C@H](C(C3=CC=CC=C3)C4=CC=CC=C4)[N@]5CC[C@]2([H])CC5
Appearance: white 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:
| Biological target: | Ampicillin binds to and inactivates penicillin-binding proteins (PBP) located on the inner membrane of the bacterial cell wall. |
| In vitro activity: | To evaluate if the in vitro activity of ampicillin increases when combined with ceftriaxone. The activity of ampicillin and ceftriaxone was evaluated against six Listeria monocytogenes invasive clinical isolates. Ampicillin and ceftriaxone MICs were determined by the broth microdilution method. Synergy was evaluated by checkerboard and time-kill curves methods. All six L. monocytogenes strains were susceptible to ampicillin (MICs 0.25-0.5 mg/L). A bacteriostatic synergy was demonstrated by the FIC index of 0.5 and a 2.5 log10 CFU reduction on the six strains studied for MIC ampicillin plus 16 mg/L ceftriaxone concentrations. The association of ceftriaxone with ampicillin increases the in vitro activity of ampicillin, and therefore could be a valuable option in the treatment of invasive infection by L. monocytogenes. Reference: Lepe JA, Rodríguez-Villodres A, Martín-Gutiérrez G, Luque R, Aznar J. In vitro study of synergy of ampicillin with ceftriaxone against Listeria monocytogenes. Rev Esp Quimioter. 2019 Oct;32(5):465-468. Epub 2019 Sep 12. PMID: 31515975; PMCID: PMC6790883. |
| In vivo activity: | This study aimed to determine if amoxicillin disturbs the enamel mineralization in in vivo experiments. Fifteen pregnant rats were randomly assigned into three groups to received daily phosphatase-buffered saline or amoxicillin as either 100 or 500 mg/kg. Mice received treatment from day 13 of pregnancy to day 40 postnatal. After birth, the offsprings from each litter continued to receive the same treatment according to their respective group. Calcium (Ca) and phosphorus (P) content in the dental hard tissues were analyzed from 60 upper first molars and 60 upper incisors by the complexometric titration method and colorimetric analysis using a spectrophotometer at 680 nm, respectively. Lower incisors were analyzed by X-ray microtomography, it was measured the electron density of lingual and buccal enamel, and the enamel and dentin thickness. Differences in Ca and P content and electron density among the groups were analyzed by one-way ANOVA. There was no significant difference on enamel electron density and thickness among the groups (p > 0.05). However, in incisors, the higher dose of amoxicillin decreased markedly the electron density in some rats. There were no statistically significant differences in Ca (p = 0.180) or P content (p = 0.054), although the higher dose of amoxicillin could affect the enamel in some animals. The amoxicillin did not significantly alter the enamel mineralization and thickness in rats. Reference: Feltrin-Souza J, Jeremias F, Alaluusua S, Sahlberg C, Santos-Pinto L, Jernvall J, Sova S, Cordeiro RCL, Cerri PS. The effect of amoxicillin on dental enamel development in vivo. Braz Oral Res. 2020 Sep 4;34:e116. doi: 10.1590/1807-3107bor-2020.vol34.0116. PMID: 32901731. |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 33.3 | 71.12 | |
| H20 | 0.0 | 0.21 |
The following data is based on the product molecular weight 468.67 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: | Lepe JA, Rodríguez-Villodres A, Martín-Gutiérrez G, Luque R, Aznar J. In vitro study of synergy of ampicillin with ceftriaxone against Listeria monocytogenes. Rev Esp Quimioter. 2019 Oct;32(5):465-468. Epub 2019 Sep 12. PMID: 31515975; PMCID: PMC6790883. |
| In vitro protocol: | Lepe JA, Rodríguez-Villodres A, Martín-Gutiérrez G, Luque R, Aznar J. In vitro study of synergy of ampicillin with ceftriaxone against Listeria monocytogenes. Rev Esp Quimioter. 2019 Oct;32(5):465-468. Epub 2019 Sep 12. PMID: 31515975; PMCID: PMC6790883. |
| In vivo protocol: | Feltrin-Souza J, Jeremias F, Alaluusua S, Sahlberg C, Santos-Pinto L, Jernvall J, Sova S, Cordeiro RCL, Cerri PS. The effect of amoxicillin on dental enamel development in vivo. Braz Oral Res. 2020 Sep 4;34:e116. doi: 10.1590/1807-3107bor-2020.vol34.0116. PMID: 32901731. |
1: Johnson RA. Maropitant prevented vomiting but not gastroesophageal reflux in anesthetized dogs premedicated with acepromazine-hydromorphone. Vet Anaesth Analg. 2013 Dec 16. doi: 10.1111/vaa.12120. [Epub ahead of print] PubMed PMID: 24330310.
2: Niyom S, Boscan P, Twedt DC, Monnet E, Eickhoff JC. Effect of maropitant, a neurokinin-1 receptor antagonist, on the minimum alveolar concentration of sevoflurane during stimulation of the ovarian ligament in cats. Vet Anaesth Analg. 2013 Jul;40(4):425-31. doi: 10.1111/vaa.12017. Epub 2013 Feb 13. PubMed PMID: 23406526.
3: Lesman SP, Boucher JF, Grover GS, Cox SR, Bidgood TL. The pharmacokinetics of maropitant citrate dosed orally to dogs at 2 mg/kg and 8 mg/kg once daily for 14 days consecutive days. J Vet Pharmacol Ther. 2013 Oct;36(5):462-70. doi: 10.1111/jvp.12027. Epub 2012 Nov 20. PubMed PMID: 23167698.
4: Hay Kraus BL. Efficacy of maropitant in preventing vomiting in dogs premedicated with hydromorphone. Vet Anaesth Analg. 2013 Jan;40(1):28-34. doi: 10.1111/j.1467-2995.2012.00788.x. Epub 2012 Oct 20. PubMed PMID: 23082784.
5: Boscan P, Monnet E, Mama K, Twedt DC, Congdon J, Steffey EP. Effect of maropitant, a neurokinin 1 receptor antagonist, on anesthetic requirements during noxious visceral stimulation of the ovary in dogs. Am J Vet Res. 2011 Dec;72(12):1576-9. doi: 10.2460/ajvr.72.12.1576. PubMed PMID: 22126683.
6: Alvillar BM, Boscan P, Mama KR, Ferreira TH, Congdon J, Twedt DC. Effect of epidural and intravenous use of the neurokinin-1 (NK-1) receptor antagonist maropitant on the sevoflurane minimum alveolar concentration (MAC) in dogs. Vet Anaesth Analg. 2012 Mar;39(2):201-5. doi: 10.1111/j.1467-2995.2011.00670.x. Epub 2011 Nov 22. PubMed PMID: 22103569.
7: Mathis A, Lee K, Alibhai HI. The use of maropitant to prevent vomiting induced by epidural administration of preservative free morphine through an epidural catheter in a dog. Vet Anaesth Analg. 2011 Sep;38(5):516-7. doi: 10.1111/j.1467-2995.2011.00645.x. PubMed PMID: 21831059.
8: Williams-Fritze MJ, Carlson Scholz JA, Zeiss C, Deng Y, Wilson SR, Franklin R, Smith PC. Maropitant citrate for treatment of ulcerative dermatitis in mice with a C57BL/6 background. J Am Assoc Lab Anim Sci. 2011 Mar;50(2):221-6. PubMed PMID: 21439216; PubMed Central PMCID: PMC3061423.
9: Rau SE, Barber LG, Burgess KE. Efficacy of maropitant in the prevention of delayed vomiting associated with administration of doxorubicin to dogs. J Vet Intern Med. 2010 Nov-Dec;24(6):1452-7. doi: 10.1111/j.1939-1676.2010.0611.x. Epub 2010 Oct 12. PubMed PMID: 21039869.
10: Narishetty ST, Galvan B, Coscarelli E, Aleo M, Fleck T, Humphrey W, McCall RB. Effect of refrigeration of the antiemetic Cerenia (maropitant) on pain on injection. Vet Ther. 2009 Fall;10(3):93-102. PubMed PMID: 20037963.
