2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. 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.

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TRPV4/TRPA1-IN-1

TRPV4/TRPA1-IN-1 Chemical Structure

CAS No. : 1532515-60-8

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TRPV4/TRPA1-IN-1 Related Antibodies

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Description

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[1].

IC50 & Target[1]

rTRPV4

0.45 μM (IC50)

mTRPA

0.43 μM (IC50)

In Vitro

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.

TRPV4/TRPA1-IN-1 Related Antibodies

Cell Viability Assay[1]

Cell Line: N2a cells
Concentration: 0-80 μM
Incubation Time: 2 days
Result: Showed first evidence of toxicity at 20 μM over 2 days, with more pronounced effects at 40 μM.
In Vivo

TRPV4-IN-4 (10 mg/kg; i.p.; single dose) alleviates trigeminal inflammatory pain mediated by TRPV4 and TRPA1 in a mouse model of pain[1].
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.

Animal Model: C57BL/6J (8-12 week old, wild-type); Trpv4⁻/⁻ (backcrossed to C57BL/6J background)[1]
Dosage: 10 mg/kg
Administration: i.p.; single dose
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.
Animal Model: C57BL/6J (8-10 week old, male)[1]
Dosage: 10 mg/kg
Administration: i.p.; single dose
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.
Molecular Weight

399.56

Formula

C25H25N3S
CAS No.
SMILES

N1=C(SC=C1C=2C=CC=CC2)NC3=CC=C(C=C3)CCN(C)CC=4C=CC=CC4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TRPV4/TRPA1-IN-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TRPV4/TRPA1-IN-11532515-60-8TRP ChannelTransient receptor potential channelsN2a cellsacute pancreatitis modelcalcium influxTRPA1TRPV4GSK205trigeminal irritant pain modelInhibitorinhibitorinhibit

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