Rifabutin-vonoprazan conjugate 1
Rifabutin-vonoprazan conjugate 1 is an orally active acid-responsive bifunctional molecule. Rifabutin-vonoprazan conjugate 1 exhibits anti-Helicobacter pylori activity (MIC ≤ 0.125 μg/mL) and acid-suppressive effects (acid inhibition rate > 85% at a dose of 2 mg/kg). Rifabutin-vonoprazan conjugate 1 also demonstrates anti-ulcer activity. Rifabutin-vonoprazan conjugate 1 can be used in research related to Helicobacter pylori infection and gastric ulcer.
For research use only. We do not sell to patients.
- Formula: C104H139FN10O21SSi2
- Molecular Weight:1972.51
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
Rifabutin-vonoprazan conjugate 1 (Compound 10) (0.125-64 μg/mL; 48 h) inhibits H. pylori ATCC 700392, demonstrating activity comparable to rifabutin (HY-17025)[1].
Rifabutin-vonoprazan conjugate 1 (1 μM; 50 min) exhibitS a 9.66% inhibition rate against porcine gastric H+/K+-ATPase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Rifabutin-vonoprazan conjugate 1 (0.3-3 mg/kg; oral gavage; single dose) exhibits dose-dependent anti-ulcer activity in mice [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (SD) (male, 250-280 g)[1]
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Dosage:2 mg/kg
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Administration:i.g.; single dose
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Result:Achieved 34.24% inhibition rate in basal gastric acid secretion model.
Achieved 64.97% inhibition rate in 2-Deoxy-D-glucose (HY-13966)-stimulated gastric acid secretion model.
Achieved 87.17% inhibition rate in Histamine (HY-B1204)-stimulated gastric acid secretion model.
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Animal Model:Mice treated water-immersion
restraint stress[1] -
Dosage:0.3, 0.75, 1.5, and 3 mg/kg
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Administration:i.g.; single dose
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Result:Induced dose-dependent reduction in ulcer area between 0.3 and 1.5 mg/kg.
Showed most pronounced effect at 1.5 mg/kg, with antiulcer efficacy comparable to Vonoprazan (HY-100007) at 3 mg/kg.
Exacerbated ulcers at 3 mg/kg.
Chemical Information
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Molecular Weight 1972.51
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Formula C104H139FN10O21SSi2
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SMILES
CC(C)[Si](C(C)C)(OCCCCCC1=CN(CCCCCCO[Si](C(C)C)(OC2=CC=C(COC(N(C)CC3=CN(S(=O)(C4=CC=CN=C4)=O)C(C5=CC=CC=C5F)=C3)=O)C=C2)C(C)C)N=N1)OC6=CC=C(COC(N7C8(CCN(CC(C)C)CC8)N=C(C7=C(NC(/C(C)=C\C=C\[C@H](C)[C@@H]([C@@H](C)[C@@H](O)[C@@H](C)[C@@H]([C@H](C)[C@@H](OC)/C=C/O9)OC(C)=O)O)=O)C%10=O)C%11=C%10C(O)=C(C)C(O[C@@]%129C)=C%11C%12=O)=O)C=C6
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Rifabutin-vonoprazan conjugate 1 Related Classifications
HY-181038 Related Classifications
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