DRAinh-A250
DRAinh-A250 is an orally active inhibitor of mouse and human SLC26A3 (DRA). DRAinh-A250 inhibits SLC26A3-mediated anion transport, blocks colonic fluid absorption, reduces luminal fluid alkalization in the distal colonic loops of mice, and alleviates Loperamide (HY-156131)-induced constipation in wild-type and cystic fibrosis mice. DRAinh-A250 can be used in the research of constipation and cystic fibrosis-related constipation.
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- CAS No.: 858747-13-4
- Formule: C20H17BrO5
- Masse moléculaire:417.26
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
0.25 μM
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Inhibition of human SLC26A3-mediated Cl-/I- exchange in HEK cells using YFP halide sensor.
Inhibition of human SLC26A3-mediated Cl-/I- exchange in HEK cells using YFP halide sensor.
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30046015 |
DRAinh-A250 (compound 4ba) (0.001-1 μM) potently inhibits slc26a3-mediated chloride/iodide exchange in Fischer rat thyroid cells expressing mouse slc26a3 and halide-sensitive yellow fluorescent protein, with an IC50 of 0.15 μM[1].
DRAinh-A250 (0.02-12.5 μM) potently inhibits mouse slc26a3-mediated Cl−/HCO3− exchange in FRT cells, with an IC50 of approximately 0.1 μM[2].
DRAinh-A250 (0.01-3 μM) inhibits Cl−/SCN− exchange mediated by mouse slc26a3 in FRT cells, with an IC50 of approximately 0.3 μM[2].
DRAinh-A250 (1 μM; 0-5 min for inhibition kinetics, 10 min for reversibility washout) rapidly inhibits mouse slc26a3-mediated Cl−/I− exchange in FRT-YFP-slc26a3 cells[2].
DRAinh-A250 (0.156-1.25 μM) potently inhibits human SLC26A3-mediated Cl−/I− exchange in HEK cells, with an IC50 of approximately 0.25 μM[2].
DRAinh-A250 (10 μM; 24 h) shows no cytotoxicity to T84 cells after 24-hour incubation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:T84 cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Did not cause toxicity in T84 cells.
DRAinh-A250 (5 mg/kg; p.o.; single dose) partially reverses loperamide-induced constipation in wild-type mice and significantly alleviates loperamide-induced constipation in cystic fibrosis mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:wild-type; cystic fibrosis mice with loss of functional CFTR[2]
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Dosage:5 mg/kg
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Administration:p.o.; single dose
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Result:Partially prevented Loperamide-induced reductions in stool weight, pellet number, and stool water content in wild-type mice.
Significantly increased stool weight, pellet number, and stool water content compared to Loperamide-only treated cystic fibrosis mice, reducing Loperamide-induced constipation.
Demonstrated fully reversible anticonstipation effect, with Loperamide-induced constipation remaining intact when administered 24 hours after treatment.
Chemical Information
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CAS No. 858747-13-4
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Masse moléculaire 417.26
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Formule C20H17BrO5
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SMILES
O=C1OC2=C(C=CC(OCC=3C=CC=C(Br)C3)=C2C)C(=C1CC(=O)O)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DRAinh-A250 Related Classifications
HY-124706 Related Classifications
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