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MedKoo Cat#: 318681 | Name: Roxatidine Acetate HCl
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Description:

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

Roxatidine acetate HCl is a histamine H2-receptor antagonist used in ulcer treatment. This compound has been found to inhibit platelet function.

Chemical Structure

Roxatidine Acetate HCl
Roxatidine Acetate HCl
CAS#93793-83-0 (Acetate Hydrochloride)

Theoretical Analysis

MedKoo Cat#: 318681

Name: Roxatidine Acetate HCl

CAS#: 93793-83-0 (Acetate Hydrochloride)

Chemical Formula: C19H29ClN2O4

Exact Mass:

Molecular Weight: 384.90

Elemental Analysis: C, 59.29; H, 7.59; Cl, 9.21; N, 7.28; O, 16.63

Price and Availability

Size Price Availability Quantity
100mg USD 450.00
200mg USD 650.00
500mg USD 1,000.00
1g USD 1,400.00
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Related CAS #
78273-80-0 (free base) 93793-83-0 (Acetate Hydrochloride) 78628-28-1 (roxatidine acetate)
Synonym
Roxatidine Acetate Hydrochloride; ROXATIDINE ACETATE HCl; Gastralgin; Altat; Roxit; HOE 760; HOE-760; N-(3-(3-(N(1)-piperidinylmethyl)phenoxy)propyl)acetoxyacetamide; TZU 0460; TZU-0460;
IUPAC/Chemical Name
[2-oxo-2-[3-[3-(piperidin-1-ylmethyl)phenoxy]propylamino]ethyl] acetate;hydrochloride
InChi Key
FEWCTJHCXOHWNL-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H28N2O4.ClH/c1-16(22)25-15-19(23)20-9-6-12-24-18-8-5-7-17(13-18)14-21-10-3-2-4-11-21;/h5,7-8,13H,2-4,6,9-12,14-15H2,1H3,(H,20,23);1H
SMILES Code
CC(=O)OCC(=O)NCCCOC1=CC=CC(=C1)CN2CCCCC2.Cl
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
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Roxatidine acetate hydrochloride is a specific and competitive histamin H2-receptor antagonist, with IC50 of 3.2 μM. It inhibits gastric acid secretion and ulcer formation.
In vitro activity:
Results indicate that roxatidine ameliorated TNF-α- induced the phosphorylations of IKK, IκBα, and NF-κB p65 as well as nuclear translocation of NF-κB p65 and the transcriptional activity of NF-κB, suggesting that roxatidine abolished the activation of NF-κB signaling pathway. Roxatidine attenuated TNF-α- induced degradation of type II collagen by suppressing the expression of MMP-3 and MMP-13 in human chondrosarcoma cell line SW1353 cells. Reference: Biomed Pharmacother. 2017 Nov;95:1156-1160. https://pubmed.ncbi.nlm.nih.gov/28926925/
In vivo activity:
Roxatidine acetate chloride (RXA) may be a potential anti-atopic dermatitis (AD) candidate. RXA treatment significantly alleviated Dfb-induced AD skin symptoms by decreasing immunoglobulin E, histamine, and inflammatory cytokines levels. RXA effectively inhibited the expression of adhesive molecules and recovered the filaggrin expression in Dfb-induced AD skin lesions and TNF-α/IFN-γ-stimulated HaCaT keratinocytes. RXA upregulated the expression of aryl hydrocarbon receptor and sirtuin1. Reference: Front Pharmacol. 2021 Dec 24;12:797086. https://pubmed.ncbi.nlm.nih.gov/35002730/
Solvent mg/mL mM
Solubility
DMSO 77.0 200.05
Ethanol 12.0 31.18
Water 77.0 200.05
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 384.90 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.

Recalculate based on batch purity %
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. Ze R, Wang S, Xie M, Zhang B, Tang X, Li J. Roxatidine Attenuates Degradation of Extracellular Matrix. Biomed Pharmacother. 2017 Nov;95:1156-1160. doi: 10.1016/j.biopha.2017.08.130. Epub 2017 Sep 15. PMID: 28926925. 2. Cho EJ, An HJ, Shin JS, Choi HE, Ko J, Cho YW, Kim HM, Choi JH, Lee KT. Roxatidine suppresses inflammatory responses via inhibition of NF-κB and p38 MAPK activation in LPS-induced RAW 264.7 macrophages. J Cell Biochem. 2011 Dec;112(12):3648-59. doi: 10.1002/jcb.23294. PMID: 21809375. 3. Kang YM, Lee M, An HJ. New Potential of Roxatidine Acetate Hydrochloride on Atopic Dermatitis Mouse Model, Human Keratinocytes, and Human Skin Equivalent Model. Front Pharmacol. 2021 Dec 24;12:797086. doi: 10.3389/fphar.2021.797086. PMID: 35002730; PMCID: PMC8740129. 4. Ji L, Wang T, Tian L, Song H, Gao M. Roxatidine inhibits fibrosis by inhibiting NF‑κB and MAPK signaling in macrophages sensing breast implant surface materials. Mol Med Rep. 2020 Jan;21(1):161-172. doi: 10.3892/mmr.2019.10815. Epub 2019 Nov 12. PMID: 31746427; PMCID: PMC6896367.
In vitro protocol:
1. Ze R, Wang S, Xie M, Zhang B, Tang X, Li J. Roxatidine Attenuates Degradation of Extracellular Matrix. Biomed Pharmacother. 2017 Nov;95:1156-1160. doi: 10.1016/j.biopha.2017.08.130. Epub 2017 Sep 15. PMID: 28926925. 2. Cho EJ, An HJ, Shin JS, Choi HE, Ko J, Cho YW, Kim HM, Choi JH, Lee KT. Roxatidine suppresses inflammatory responses via inhibition of NF-κB and p38 MAPK activation in LPS-induced RAW 264.7 macrophages. J Cell Biochem. 2011 Dec;112(12):3648-59. doi: 10.1002/jcb.23294. PMID: 21809375.
In vivo protocol:
1. Kang YM, Lee M, An HJ. New Potential of Roxatidine Acetate Hydrochloride on Atopic Dermatitis Mouse Model, Human Keratinocytes, and Human Skin Equivalent Model. Front Pharmacol. 2021 Dec 24;12:797086. doi: 10.3389/fphar.2021.797086. PMID: 35002730; PMCID: PMC8740129. 2. Ji L, Wang T, Tian L, Song H, Gao M. Roxatidine inhibits fibrosis by inhibiting NF‑κB and MAPK signaling in macrophages sensing breast implant surface materials. Mol Med Rep. 2020 Jan;21(1):161-172. doi: 10.3892/mmr.2019.10815. Epub 2019 Nov 12. PMID: 31746427; PMCID: PMC6896367.
1: Nakamura H, Kawashima H, Azuma R, Sato I, Nagao K, Miyazawa K. Pharmacokinetics of the H(2) blocker roxatidine acetate hydrochloride in pediatric patients, in comparison with healthy adult volunteers. Drug Metab Pharmacokinet. 2012;27(4):422-9. Epub 2012 Jan 31. PubMed PMID: 22293541. 2: Maheshwari A, Sharma M, Sharma D. Investigation of the binding of roxatidine acetate hydrochloride with cyclomaltoheptaose (β-cyclodextrin) using IR and NMR spectroscopy. Carbohydr Res. 2011 Sep 27;346(13):1809-13. doi: 10.1016/j.carres.2011.07.003. Epub 2011 Jul 18. PubMed PMID: 21816394. 3: Ali SM, Maheshwari A, Asmat F. Complexation of roxatidine acetate hydrochloride with beta-cyclodextrin: NMR spectroscopic study. Pharmazie. 2004 Aug;59(8):653-5. PubMed PMID: 15378861. 4: Yasutake K, Amano M, Mizokami Y, Kubota S, Fukumoto H, Imamura Y, Yokoya H, Irie K. Effects of changing the type of H2-blocker in the treatment of H2-blocker-resistant ulcers: comparison of roxatidine acetate hydrochloride and other H2-blockers. J Int Med Res. 1998 Jan-Feb;26(1):25-36. PubMed PMID: 9513074. 5: Yoshimura N, Takeuchi H, Ogata H, Ishioka T, Aoi R. Effects of roxatidine acetate hydrochloride and cimetidine on the pharmacokinetics of theophylline in healthy subjects. Int J Clin Pharmacol Ther Toxicol. 1989 Jun;27(6):308-12. PubMed PMID: 2737801. 6: Morita K, Konishi H, Ono T, Shimakawa H. A comparison of the inhibitory effects of roxatidine acetate hydrochloride and cimetidine on cytochrome P-450-mediated drug-metabolism in mouse hepatic microsomes and in man in vivo. J Pharmacobiodyn. 1987 Jul;10(7):287-95. PubMed PMID: 2891811. 7: Iwamura S, Shibata K, Kawabe Y, Tsukamoto K, Honma S. The metabolism of roxatidine acetate hydrochloride in rat and dog liver homogenates. J Pharmacobiodyn. 1987 Jun;10(6):229-35. PubMed PMID: 2889823. 8: Igawa K, Matsunaga T, Yokozeki H, Nishioka K. Erythrodermic drug eruption due to roxatidine acetate hydrochloride. Clin Exp Dermatol. 2005 May;30(3):304-5. PubMed PMID: 15807703. 9: Nagai N, Furuhata M, Ogata H. Drug interactions between theophylline and H2-antagonists, roxatidine acetate hydrochloride and cimetidine: pharmacokinetic analysis in rats in vivo. Biol Pharm Bull. 1995 Nov;18(11):1610-3. PubMed PMID: 8593491. 10: Kawanishi M, Enomoto A, Shimada Y, Kurokawa Y. [Clinical evaluation of roxatidine acetate hydrochloride injection as preanesthetic medication]. Masui. 1991 Sep;40(9):1364-70. Japanese. PubMed PMID: 1682516. 11: Kojima A, Andoh K, Shima T, Koga Y, Hashimoto Y. [The effect of oral administration of roxatidine acetate hydrochloride 3 hours prior to the operation on pH and volume of gastric juice]. Masui. 1991 Mar;40(3):451-3. Japanese. PubMed PMID: 1677048. 12: Tanioka H, Terahara A, Sasaki Y. Radiographic assessment of nocturnal gastric juice secretion after administration of roxatidine acetate hydrochloride. Clin Ther. 1991 Jan-Feb;13(1):22-4. PubMed PMID: 1674230. 13: Honma S, Iwamura S, Kobayashi R, Kawabe Y, Shibata K. The metabolism of roxatidine acetate hydrochloride. Liberation of deuterium from the piperidine ring during hydroxylation. Drug Metab Dispos. 1987 Jul-Aug;15(4):551-9. PubMed PMID: 2888630.