Soraprazan (BYK61359) (Synonyms: BYK61359) |
Catalog No.GC30130
One-Click Copy Product Info
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Soraprazan (BYK61359) (BYK61359) es un inhibidor competitivo K reversible de la H,K-ATPasa (Ki=6,4 nM), con una IC50 de 0,19 μM en glÁndulas gÁstricas.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 261944-46-1
Sample solution is provided at 25 µL, 10mM.
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Soraprazan is a reversible, and fast-acting inhibitor of gastric H+/K+ ATPase.
Soraprazan is a potent inhibitor of gastric H,K-ATPase, with an IC50 of 0.1 μM when measured in ion-leaky vesicles in the presence of 1 mM potassium. Soraprazan also effectively inhibits dibutyryl cAMP-stimulated [14C]AP accumulation in isolated gastric glands with an IC50 of 0.19 μM (0.09-0.40 μM geometric mean from n=6 with 95% confidence limits). In ion-leaky vesicles, soraprazan is a potent k-competitive inhibitor of the H,K-ATPase, with Ki of 6.4 nM. Soraprazan binds to the H,K-ATPase in ion-leaky vesicles with a Kd of 26.4 nM and a Bmax of 2.89 nmol/mg[1].
[1]. Simon WA, et al. Soraprazan: setting new standards in inhibition of gastric acid secretion. J Pharmacol Exp Ther. 2007 Jun;321(3):866-74. Epub 2007 Mar 16.
Kinase experiment: | [3H]Soraprazan binding studies are carried out at 20°C. In saturation experiments to determine the Kd value, ion-leaky gastric vesicles (0.01-0.02 mg/mL) are resuspended in a buffer composed of 20 mM Tris-HCl, pH 7.0, 2 mM MgCl2, and 2 mM ATP (pH 7.0 by Tris) in the presence of increasing concentrations of [3H]soraprazan (0.1 nM-1 μM). Nonspecific binding is determined in the presence of a 100 fold excess of unlabeled soraprazan over the concentration range of [3H]soraprazan used. The enzyme suspension (1 mL) is incubated at 20°C for 30 min and rapidly filtered through a nitrocellulose membrane filter (0.45 μM) prewet with a solution composed of 20 mM Tris-HCl, pH 7.0, 10% polyethylene glycol 3350 that is placed on top of a glass fiber filter. The membrane is ished five times with 2.5 mL of a buffer composed of 20 mM Tris-HCl, pH 7.0, and 10% polyethylene glycol 3350 to remove unbound inhibitor. The membrane is put into a 20-mL scintillation vial, dimethylacetamide (0.5 mL) is added to dissolve the membrane, and 14 mL of scintillation solvent is added and counted. Binding of [3H]soraprazan is determined by subtracting the nonspecific binding of [3H]soraprazan, obtained in the presence of the 100-fold excess of nonradioactive soraprazan, from the amounts of [3H]soraprazan bound to the membrane in the absence of the cold inhibitor. |
References: [1]. Simon WA, et al. Soraprazan: setting new standards in inhibition of gastric acid secretion. J Pharmacol Exp Ther. 2007 Jun;321(3):866-74. Epub 2007 Mar 16. | |
| Cas No. | 261944-46-1 | SDF | |
| Sinónimos | BYK61359 | ||
| Canonical SMILES | O[C@@H]1[C@@H](C2=CC=CC=C2)NC3=C(C=CN4C3=NC(C)=C4C)[C@H]1OCCOC | ||
| Formula | C21H25N3O3 | M.Wt | 367.44 |
| Solubility | DMSO : ≥ 150 mg/mL (408.23 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7215 mL | 13.6077 mL | 27.2153 mL |
| 5 mM | 544.3 μL | 2.7215 mL | 5.4431 mL |
| 10 mM | 272.2 μL | 1.3608 mL | 2.7215 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)