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  3. Saviprazole

Saviprazole (HOE-731) is a H+,K+-ATPase inhibitor. Saviprazole inhibits gastric acid secretion. Saviprazole inhibits histamine- and dbcAMP-stimulated [14C]aminopyrine uptake, dbcAMP-induced oxygen consumption. Saviprazole can be used in research related to gastrointestinal diseases, such as gastric ulcers and acid reflux.

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

Saviprazole

Saviprazole Chemical Structure

CAS No. : 121617-11-6

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Based on 1 publication(s) in Google Scholar

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Description

Saviprazole (HOE-731) is a H+,K+-ATPase inhibitor. Saviprazole inhibits gastric acid secretion. Saviprazole inhibits histamine- and dbcAMP-stimulated [14C]aminopyrine uptake, dbcAMP-induced oxygen consumption. Saviprazole can be used in research related to gastrointestinal diseases, such as gastric ulcers and acid reflux[1][2].

In Vitro

Saviprazole (0.1-30 μM; 20 min pre-stimulation) non-competitively inhibits histamine- and dbcAMP-stimulated [14C] aminopyrine uptake in isolated rabbit gastric glands with IC50 values of 0.8 μM and 1.3 μM, respectively, and this inhibition is reversible with Dithioerythritol (HY-15916)[1].
Saviprazole (100 μM; 45 min) inhibits dbcAMP-stimulated oxygen consumption in isolated rabbit gastric glands down to basal levels, and this effect is dependent on an acidic parietal cell compartment, as it is fully prevented by 10 mM Imidazole (HY-114481)[1].
Saviprazole potently inhibits gastric H+,K+-ATPase and proton transport in gastric vesicles[2].

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

In Vivo

Saviprazole (0.03-1 mg/kg; i.v., i.d.; single dose) causes dose-dependent, state-of-stimulation-dependent inhibition of histamine-stimulated gastric acid secretion in Heidenhain pouch dogs, with an ID50 of 0.16 mg/kg i.v. and 0.31 mg/kg i.d.[2].
Saviprazole (0.1-30 mg/kg; i.d.; single dose) causes dose-dependent inhibition of basal and secretagogue-stimulated gastric acid secretion in pylorus-ligated rats, with ID50 values ranging from 0.9 to 2.5 mg/kg[2].
Saviprazole (0.1-1 mg/kg; i.v.; single dose) causes dose-dependent inhibition of receptor- and postreceptor-stimulated gastric acid secretion in anesthetized stomach-lumen-perfused rats, with 0.5 mg/kg reducing IBMX (HY-12318) + Forskolin (HY-15371)-stimulated secretion by ~70%[2].

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

Animal Model: Heidenhain pouch dogs[2]
Dosage: 0.03 mg/kg; 0.1 mg/kg; 0.3 mg/kg; 1.0 mg/kg
Administration: i.v.; single dose; i.d.; single dose
Result: Caused dose-dependent inhibition of histamine-stimulated gastric acid secretion, with ID50 values of 0.16 mg/kg (i.v.) and 0.31 mg/kg (i.d.).
Caused an immediate 80% drop in acid output after administration of 0.3 mg/kg i.v. during stimulated secretion; acid output was about half maximal on day 2 and approached control values on day 3.
Showed no inhibitory effect when 0.3 mg/kg i.v. was administered 3 hours prior to histamine stimulation.
Caused immediate complete inhibition of acid output at 1 mg/kg i.v., which lasted only 30 minutes, after which acid output rose to ~10% of maximally stimulated levels.
Molecular Weight

461.38

Formula

C15H10F7N3O2S2

CAS No.
Appearance

Solid

Color

Brown to black

SMILES

O=S(CC1=NC=CC(OCC(F)(C(F)(C(F)(F)F)F)F)=C1)C2=NC3=CSC=C3N2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (216.74 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 2.1674 mL 10.8371 mL 21.6741 mL
5 mM 0.4335 mL 2.1674 mL 4.3348 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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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 2.1674 mL 10.8371 mL 21.6741 mL 54.1853 mL
5 mM 0.4335 mL 2.1674 mL 4.3348 mL 10.8371 mL
10 mM 0.2167 mL 1.0837 mL 2.1674 mL 5.4185 mL
15 mM 0.1445 mL 0.7225 mL 1.4449 mL 3.6124 mL
20 mM 0.1084 mL 0.5419 mL 1.0837 mL 2.7093 mL
25 mM 0.0867 mL 0.4335 mL 0.8670 mL 2.1674 mL
30 mM 0.0722 mL 0.3612 mL 0.7225 mL 1.8062 mL
40 mM 0.0542 mL 0.2709 mL 0.5419 mL 1.3546 mL
50 mM 0.0433 mL 0.2167 mL 0.4335 mL 1.0837 mL
60 mM 0.0361 mL 0.1806 mL 0.3612 mL 0.9031 mL
80 mM 0.0271 mL 0.1355 mL 0.2709 mL 0.6773 mL
100 mM 0.0217 mL 0.1084 mL 0.2167 mL 0.5419 mL
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Product Name:
Saviprazole
Cat. No.:
HY-101646
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