Cat. No.: HY-137941

Roxatidine

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Roxatidine is an active metabolite of Roxatidine acetate hydrochloride, is an orally active histamine H2-receptor antagonist. Roxatidine, an anti-ulcer agent, suppresses histamine release (thus inhibiting proton secretion) and inhibits the production of VEGF-1, an important marker of inflammation and angiogenesis. Anti-allergic inflammatory effect. Roxatidine is promising for research of gastric and duodenal ulcers.

For research use only. We do not sell to patients.

Purity: 98.25%
CAS No.: 78273-80-0
Formula: C₁₇H₂₆N₂O₃
Molecular Weight:306.41

Storage:

Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Roxatidine Chemical Structure

CAS No.: 78273-80-0

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Sample (0.1mg)

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(In Japan)

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

H₂ Receptor

All Histamine Receptor Isoforms :

All Caspase Isoforms :

All NF-κB Isoforms :

All p38 MAPK Isoforms :

In Vitro

Roxatidine (6.25-25 μM, 6 h 30 min) suppresses the PMACI-induced production of pro-inflammatory cytokines, NF-κB and caspase-1 activation, activation of p38 MAPK in HMC-1^[1].
Roxatidine (40-120 μM, 1 h) inhibits the production of PGE2, NO, and histamine induced by LPS, as well as the expression of COX-2, iNOS, and HDC in RAW 264.7 cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Real Time qPCR^[1]

Cell Line:

HMC-1 cells
Concentration:

6.25-25 μM
Incubation Time:

6 h 30 min
Result:

Down-regulated the PMACI-induced TNF-α, IL-6, and IL-1β production and their mRNA expression in a dose-dependent manner.

Western Blot Analysis^[1]

Cell Line:

HMC-1 cells
Concentration:

6.25-25 μM
Incubation Time:

60 min
Result:

Suppressed the PMACI-stimulated nuclear translocations of p65 subunit of NF-κB, phosphorylation and degradation of IκB-α, the PMACI-induced activation of p38 MAPK in HMC-1.

In Vivo

Roxatidine (20 mg/kg, p.o., a single dose for 1h before Compound 48/80 injection) ameliorates Compound 48/80 (HY-115768) (8mg/kg, i.p., a single dose for 1h)-induced allergic hypersensitivity and suppresses Compound 48/80-induced allergic inflammation in anaphylactic animal model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Compound 48/80-induced anaphylactic shock mouse model^[1]
Dosage:

20 mg/kg
Administration:

p.o., a single dose for 1h before Compound 48/80 injection
Result:

Increased the survival rate to 20% at 60 min after compound 48/80 injection.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 78273-80-0
Appearance Oil
Molecular Weight 306.41
Formula C₁₇H₂₆N₂O₃
Color Colorless to light yellow
SMILES

O=C(NCCCOC1=CC=CC(CN2CCCCC2)=C1)CO
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (326.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.2636 mL

16.3182 mL

32.6364 mL

5 mM

0.6527 mL

3.2636 mL

6.5273 mL

10 mM

0.3264 mL

1.6318 mL

3.2636 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Lee M, et al. Roxatidine attenuates mast cell-mediated allergic inflammation via inhibition of NF-κB and p38 MAPK activation. Sci Rep. 2017;7:41721. Published 2017 Jan 31. [Content Brief]

[2]. Collins JD, et al. Pharmacokinetics of roxatidine in healthy volunteers. Drugs. 1988;35 Suppl 3:41-7. [Content Brief]

[3]. Cho EJ, et al. 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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.2636 mL	16.3182 mL	32.6364 mL	81.5911 mL
	5 mM	0.6527 mL	3.2636 mL	6.5273 mL	16.3182 mL
	10 mM	0.3264 mL	1.6318 mL	3.2636 mL	8.1591 mL
	15 mM	0.2176 mL	1.0879 mL	2.1758 mL	5.4394 mL
	20 mM	0.1632 mL	0.8159 mL	1.6318 mL	4.0796 mL
	25 mM	0.1305 mL	0.6527 mL	1.3055 mL	3.2636 mL
	30 mM	0.1088 mL	0.5439 mL	1.0879 mL	2.7197 mL
	40 mM	0.0816 mL	0.4080 mL	0.8159 mL	2.0398 mL
	50 mM	0.0653 mL	0.3264 mL	0.6527 mL	1.6318 mL
	60 mM	0.0544 mL	0.2720 mL	0.5439 mL	1.3599 mL
	80 mM	0.0408 mL	0.2040 mL	0.4080 mL	1.0199 mL
	100 mM	0.0326 mL	0.1632 mL	0.3264 mL	0.8159 mL

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Roxatidine

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All Histamine Receptor Isoforms

All Caspase Isoforms

All NF-κB Isoforms

All p38 MAPK Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Roxatidine Related Classifications

Cat. No.: HY-137941