2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation Apoptosis NF-κB MAPK/ERK Pathway
  3. Histamine Receptor Caspase NF-κB p38 MAPK
  4. Roxatidine

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.

Roxatidine Chemical Structure

Roxatidine Chemical Structure

CAS No. : 78273-80-0

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Roxatidine:

Roxatidine Related Antibodies

Top Publications Citing Use of Products

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H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3].

IC50 & Target

H2 Receptor

 

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.

Roxatidine Related Antibodies

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
Molecular Weight

306.41

Formula

C17H26N2O3
CAS No.
Appearance

Oil

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2636 mL 16.3182 mL 32.6364 mL
5 mM 0.6527 mL 3.2636 mL 6.5273 mL
View the Complete Stock Solution Preparation Table

* 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.

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Roxatidine78273-80-0Histamine ReceptorCaspaseNF-κBp38 MAPKNuclear factor-κBNuclear factor-kappaBactive metabolitehistamineinflammatory cytokinesanaphylactic miceInhibitorinhibitorinhibit

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