TRPV4/TRPA1-IN-1
TRPV4/TRPA1-IN-1 is a TRPV4/TRPA1 inhibitor that suppresses TRPV4/TRPA1-mediated calcium influx. TRPV4/TRPA1-IN-1 alleviates pain behaviors in a mouse trigeminal stimulation pain model and inhibits inflammation and pain-related behaviors in a mouse acute pancreatitis model. TRPV4/TRPA1-IN-1 can be used in research on acute pancreatitis.
For research use only. We do not sell to patients.
- CAS No.: 1532515-60-8
- Formula: C25H25N3S
- Molecular Weight:399.56
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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rTRPV4 0.45 μM (IC50) |
mTRPA 0.43 μM (IC50) |
TRPV4-IN-4 (0-10 μM) inhibits TRPV4-mediated Ca2+ influx in N2a cells overexpressing TRPV4, primary porcine articular chondrocytes, and primary rat astrocytes (IC50 = 0.45 μM in N2a cells)[1].
TRPV4-IN-4 (5 μM; 5 min) effectively inhibits TRPV4-mediated transmembrane currents in TRPV4-GFP+ N2a cells[1].
TRPV4-IN-4 inhibits TRPA1 activity in N2a cells overexpressing TRPA1 (IC50 = 0.43 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:N2a cells
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Concentration:0-80 μM
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Incubation Time:2 days
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Result:Showed first evidence of toxicity at 20 μM over 2 days, with more pronounced effects at 40 μM.
TRPV4-IN-4 (10 mg/kg, intraperitoneal injection, single dose) alleviates inflammation and pain associated with Caerulein (HY-A0190)-induced acute pancreatitis in mouse models, including the reduction of pancreatic edema and pain-related behaviors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (8-12 week old, wild-type); Trpv4⁻/⁻ (backcrossed to C57BL/6J background)[1]
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Dosage:10 mg/kg
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Administration:i.p.; single dose
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Result:Significantly attenuated late-phase nocifensive behavior by >50% in wild-type mice. Virtually eliminated immediate-phase pain behavior and strikingly reduced late-phase pain behavior in Trpv4⁻/⁻ mice, with potency equivalent to A967079 (HY-108463) (25 mg/kg) in reducing late-phase pain.
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Animal Model:C57BL/6J (8-10 week old, male)[1]
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Dosage:10 mg/kg
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Administration:i.p.; single dose
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Result:Virtually eliminated pancreatic edema. Significantly reduced serum amylase levels. Significantly decreased pancreatic MPO content. Significantly lowered histopathological inflammation score. Virtually eliminated Caerulein-induced nocifensive pain behavior.
Chemical Information
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CAS No. 1532515-60-8
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Molecular Weight 399.56
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Formula C25H25N3S
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SMILES
N1=C(SC=C1C=2C=CC=CC2)NC3=CC=C(C=C3)CCN(C)CC=4C=CC=CC4
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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)
TRPV4/TRPA1-IN-1 Related Classifications
HY-122692 Related Classifications
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