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Rabeprazole Sodium (LY307640 sodium)

Alias: LY307640 sodium; LY-307640 sodium; LY 307640 sodium; Rabeprazole Sodium; Pariet; Aciphex; Rabeprazole sodium salt; Rebeprazole sodium;3810, E; Aciphex; dexrabeprazole; E 3810; E3810; LY 307640; LY-307640; LY307640;
Cat No.:V4894 Purity: ≥98%
Rabeprazole sodium (LY-307640 sodium) is a novel, potent and 2nd-generation proton pump inhibitor (PPI) that is used as an antiulcer drug.
Rabeprazole Sodium (LY307640 sodium)
Rabeprazole Sodium (LY307640 sodium) Chemical Structure CAS No.: 117976-90-6
Product category: Proton Pump
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
50mg
100mg
250mg
500mg
1g
Other Sizes

Other Forms of Rabeprazole Sodium (LY307640 sodium):

  • Rabeprazole (LY307640)
  • Rabeprazole-d4 (LY307640-d4)
  • Rabeprazole Sulfide (Standard)
  • Rabeprazole Sulfide
  • Rabeprazole-d3 sodium (LY307640-d3 sodium)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Rabeprazole sodium (LY-307640 sodium) is a novel, potent and 2nd-generation proton pump inhibitor (PPI) that is used as an antiulcer drug. It irreversibly inactivates gastric H+/K+-ATPase and induces apoptosis. Rabeprazole acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC50 of 0.3 μM. Rabeprazole can be used for the research of gastric ulcerations and gastroesophageal reflux. It is a partially reversible gastric proton pump inhibitor and also an inhibitor of ATP4.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
After 0.2 mM treatment for 16 hours, rabeprazole eliminated the viability of human cells [2]. In MKN-28 cells, rabeprazole totally suppressed ERK1/2 phosphorylation. MKN-28 cell line ERK 1/2 phosphorylation was significantly suppressed when the cell line was cultured in toxin media (pH 5.4) for two hours and then attenuated with rabeprazole (0.2 mM) for two hours [2].
ln Vivo
In female mice, rabeprazole sodium (10 mg/kg; lateral every 48 hours for 18 weeks) significantly reduces serum calcium levels, causes a decrease in bone mineral density (BMD), and results in secondary hyperparathyroidism [3].
Cell Assay
Cell Viability Assay[2]
Cell Types: Three gastric cancer cell lines KATO III, MKN-28 and MKN-45
Tested Concentrations: 0.2 mM
Incubation Duration: 16 hrs (hours)
Experimental Results: Treatment resulted in diminished viability of all tested cancer cell lines, comparable to KATO III Compared with MKN-28 cells, the cell viability was Dramatically diminished compared with MKN-45 cells.

Western Blot Analysis[2]
Cell Types: Three gastric cancer cell lines (KATO III, MKN-28 and MKN-45)[2]
Tested Concentrations: 0.2 mM
Incubation Duration: 2 hrs (hours) pretreatment
Experimental Results: Result in strong inhibition of ERK 1/2 Phosphorylated in MKN-28 cells, but no similar effect was observed in KATO III and MKN-45 cells.
Animal Protocol
Animal/Disease Models: Female Swiss albino mice (body weight 18-26 g) [3]
Doses: 10 mg/kg
Route of Administration: Oral; every 48 hrs (hrs (hours)) for 18 weeks
Experimental Results: Serum calcium levels compared with vehicle-treated group Dramatically lower (5.5±2.07 vs. 9.68±2.77).
References

[1]. Identification of Proton-Pump Inhibitor Drugs That Inhibit Trichomonas Vaginalis Uridine Nucleoside Ribohydrolase. Bioorg Med Chem Lett. 2014 Feb 15;24(4):1080-4.

[2]. Rabeprazole Exhibits Antiproliferative Effects on Human Gastric Cancer Cell Lines. Oncol Lett. 2014 Oct;8(4):1739-1744.

[3]. Supplement With Calcium or Alendronate Suppresses Osteopenia Due to Long Term Rabeprazole Treatment in Female Mice: Influence on Bone TRAP and Osteopontin Levels. Front Pharmacol. 2020 May 13;11:583.

Additional Infomation
Rabeprazole sodium is an organic sodium salt. It contains a rabeprazole(1-).
Rabeprazole Sodium is the sodium salt of the prodrug rabeprazole, a substituted benzimidazole proton pump inhibitor, with potential anti-ulcer activity. After protonation, accumulation, and transformation to the active sulfenamide within the acidic environment of gastric parietal cells, rabeprazole selectively and irreversibly binds to and inhibits the H+, K+ATPase (hydrogen-potassium adenosine triphosphatase) enzyme system located on the parietal cell secretory surface, inhibiting gastric acid secretion.
A 4-(3-methoxypropoxy)-3-methylpyridinyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS.
See also: Rabeprazole (has active moiety).
Drug Indication
Treatment of duodenal ulcer, Treatment of gastric ulcer, Treatment of gastro-oesophageal reflux disease, Treatment of Helicobacter pylori in patients with peptic ulcer disease, Treatment of Zollinger-Ellison syndrome
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C18H20N3NAO3S
Molecular Weight
381.4245
Exact Mass
381.112
CAS #
117976-90-6
Related CAS #
Rabeprazole;117976-89-3;Rabeprazole-d4 sodium;Rabeprazole-d4;934295-48-4;Rabeprazole Sulfide;117977-21-6;Rabeprazole-d3 sodium;1216494-11-9
PubChem CID
14720269
Appearance
White to off-white solid powder
Density
0.45~0.55 g/ml
Boiling Point
603.9ºC at 760 mmHg
Melting Point
140-141ºC dec.
Flash Point
319.1ºC
LogP
3.484
Hydrogen Bond Donor Count
0
Hydrogen Bond Acceptor Count
7
Rotatable Bond Count
8
Heavy Atom Count
26
Complexity
446
Defined Atom Stereocenter Count
0
InChi Key
KRCQSTCYZUOBHN-UHFFFAOYSA-N
InChi Code
InChI=1S/C18H20N3O3S.Na/c1-13-16(19-9-8-17(13)24-11-5-10-23-2)12-25(22)18-20-14-6-3-4-7-15(14)21-18;/h3-4,6-9H,5,10-12H2,1-2H3;/q-1;+1
Chemical Name
sodium;2-[[4-(3-methoxypropoxy)-3-methylpyridin-2-yl]methylsulfinyl]benzimidazol-1-ide
Synonyms
LY307640 sodium; LY-307640 sodium; LY 307640 sodium; Rabeprazole Sodium; Pariet; Aciphex; Rabeprazole sodium salt; Rebeprazole sodium;3810, E; Aciphex; dexrabeprazole; E 3810; E3810; LY 307640; LY-307640; LY307640;
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
H2O : ≥ 100 mg/mL (~262.18 mM)
DMSO : ≥ 48 mg/mL (~125.85 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.45 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.08 mg/mL (5.45 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.08 mg/mL (5.45 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.6218 mL 13.1089 mL 26.2178 mL
5 mM 0.5244 mL 2.6218 mL 5.2436 mL
10 mM 0.2622 mL 1.3109 mL 2.6218 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
A Study in Healthy Men to Compare Two Different Oral Formulations of BI 1810631 and to Test How Food or Rabeprazole Influence the Amount of BI 1810631 in the Blood
CTID: NCT05380947
Phase: Phase 1    Status: Completed
Date: 2024-10-16
Fasting Study of Rabeprazole Sodium Delayed-Release Tablets 20 mg to Aciphex® Delayed-Release Tablets 20 mg
CTID: NCT00648349
Phase: Phase 1    Status: Completed
Date: 2024-04-24
Food Study of Rabeprazole Sodium Delayed-Release Tablets 20 mg to Aciphex® Tablets 20 mg
CTID: NCT00649194
Phase: Phase 1    Status: Completed
Date: 2024-04-24
Fed Study of Rabeprazole Sodium Tablets 20 mg and Aciphex® Tablets 20 mg
CTID: NCT00649493
Phase: Phase 1    Status: Completed
Date: 2024-04-23
A Study to Compare the Safety, Pharmacokinetics and Pharmacodynamics of YPI 011 to Rabeprazole in Healthy Adult Subjects
CTID: NCT04703868
Phase: Phase 1    Status: Completed
Date: 2024-01-24
View More

Efficacy and Safety After Multiple Doses of TNP-2198 Capsules, Rabeprazole Sodium Enteric-coated Tablets and Amoxicillin Capsules in Helicobacter Pylori Infected-positive Participants
CTID: NCT06076694
Phase: Phase 2    Status: Completed
Date: 2023-12-12


A Study to Evaluate Preliminary Helicobacter Pylori Eradication After Multiple Doses of TNP-2198 Capsules Combined With Rabeprazole Sodium Enteric-
A Multicenter, Double-Blind, Parallel-Group Study to Evaluate Short-Term Safety and Efficacy and Long-Term Maintenance of Two Dose Levels of Rabeprazole Sodium Delayed-Release Pediatric Bead Formulation in 1-to-11-Year-Old Pediatric Subjects with Endoscopically Proven GERD
CTID: null
Phase: Phase 3    Status: Not Authorised, Ongoing, Completed
Date: 2009-03-05
A Randomized Double-Blind Parallel Study of Rabeprazole Extended-Release 50 mg Versus Esomeprazole 40 mg for Healing and Symptomatic Relief of Moderate to Severe Erosive gastroesophageal Reflux Disease (GERD)
CTID: null
Phase: Phase 3    Status: Completed
Date: 2008-08-01
A Randomized Double-Blind Parallel Study of Rabeprazole Extended-Release 50 mg Versus Esomeprazole 40 mg for Healing and Symptomatic Relief of Moderate to Severe Erosive gastroesophageal Reflux Disease (GERD)
CTID: null
Phase: Phase 3    Status: Completed
Date: 2008-08-01
A Pharmacokinetic, Pharmacodynamic and Safety Study of Single and Multiple Doses of Rabeprazole in Pediatric Subjects with GERD 1 to 11 Months old, Inclusive
CTID: null
Phase: Phase 1    Status: Completed
Date: 2008-05-16
A Pharmacokinetic and Safety Study of Single and Multiple Doses of Rabeprazole in Pediatric Subjects with GERD 1 to 11 Years old, inclusive
CTID: null
Phase: Phase 1    Status: Completed
Date: 2008-04-25
Adequate therapy against low-dose aspirin-induced ulcer: comparison of two acid-inhibitory drugs, rabeprazole and famotidine (Quality study)
CTID: UMIN000007639
Phase:    Status: Complete: follow-up complete
Date: 2012-04-02
The Esophageal Dysfunction Plays a Key Role in the Pathogenesis of PPI-resistant Globus sensation
CTID: UMIN000007417
Phase:    Status: Recruiting
Date: 2012-03-01
Efficacy of E3810 for the prevention of gastric or duodenal ulcer caused by low-dose aspirin
CTID: jRCT2080221499
Phase:    Status:
Date: 2011-06-29
Long-term administration study of E3810 for the prevention of gastric or duodenal ulcer caused by low-dose aspirin
CTID: jRCT2080221500
Phase:    Status:
Date: 2011-06-29
Prophylactic efficacy of Proton Pump Inhibitor on Recurrence of Peptic Ulcer in Patients continuously treated with Low-dose Aspirin-Randomized, Multi-center, single-blinded, parallel-group, comparative study-
CTID: UMIN000002901
Phase: Phase III    Status: Complete: follow-up complete
Date: 2009-12-15

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