2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel Calcium Channel
  4. A-425619

A-425619 is an orally active and selective transient receptor potential type V1 (TRPV1) antagonist. A-425619 blocks Capsaicin (HY-10448)- and N-arachidonoyl-dopamine (NADA)-induced Ca2+ influx in dorsal root ganglia and trigeminal ganglia. A-425619 relieves pathophysiological pain associated with inflammation and tissue injury in rats. A-425619 can be used for the study of pain related to inflammation and tissue injury.

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A-425619

A-425619 Chemical Structure

CAS No. : 581809-67-8

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Based on 1 publication(s) in Google Scholar

A-425619 Related Antibodies

Top Publications Citing Use of Products

View All TRP Channel Isoform Specific Products:

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TRPC TRPM TRPV TRPA TRPML

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

  • Biological Activity

  • Purity & Documentation

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Description

A-425619 is an orally active and selective transient receptor potential type V1 (TRPV1) antagonist. A-425619 blocks Capsaicin (HY-10448)- and N-arachidonoyl-dopamine (NADA)-induced Ca2+ influx in dorsal root ganglia and trigeminal ganglia. A-425619 relieves pathophysiological pain associated with inflammation and tissue injury in rats. A-425619 can be used for the study of pain related to inflammation and tissue injury[1][2][3].

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
2 nM
Compound: 7
Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of acid-induced receptor activation by FLIPR assay
Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of acid-induced receptor activation by FLIPR assay
[PMID: 17489570]
HEK293 IC50
5 nM
Compound: 7
Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay
Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay
[PMID: 17489570]
HEK293 IC50
9 nM
Compound: 7
Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay
Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as blockade of capsaicin-induced receptor activation by FLIPR assay
[PMID: 17489570]
In Vitro

A-425619 (10 μM) blocks 500 nM Capsaicin (HY-10448)-induced Ca2+ influx in dorsal root ganglia (IC50 = 78 nM) and trigeminal ganglia (IC50 = 115 nM), and inhibits 3 μM N-arachidonoyl-dopamine (NADA)-induced Ca2+ influx in dorsal root ganglia (IC50 = 36 nM) and trigeminal ganglia (IC50 = 37 nM)[1].
A-425619 (100 nM) can completely inhibit TRPV1-mediated acid-activated currents in dorsal root ganglia and trigeminal ganglion neurons[1].
A-425619 (0.01-1 μM) can significantly block 300 nM Capsaicin- and 3 μM NADA-evoked calcitonin gene-related peptide (CGRP) release in dorsal root ganglia[1].
A-425619 (3-100 nM) potently blocks the activation of native TRPV1 channels in rat dorsal root ganglion neurons(IC50 = 9 nM)[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

A-425619 Related Antibodies
In Vivo

A-425619 (10.3-103 μg/rats (30-300 nmol/rats), intraplantar, 15 min before Capsaicin, single dose or 10.3-35 mg/kg (30-100 μmol/kg), p.o., 60 min before Capsaicin, single dose) dose-dependently blocks Capsaicin-induced mechanical hyperalgesia in rats[3].
A-425619 (3.5-35 mg/kg (10-100 μmol/kg), i.p., 30 min before testing, single dose or 3.5-103 mg/kg (10-300 μmol/kg), p.o., 60 min before testing, single dose) dose-dependently relieves CFA-induced chronic inflammatory thermal hyperalgesia in rats[3].
A-425619 (103 μg/rats (300 nmol/rats), intraplantar into inflamed paw, 30 min before testing, single dose) reduces CFA-induced thermal hyperalgesia in rats[3].
A-425619 (3.5-35 mg/kg (10-100 μmol/kg), i.p., 90 min after Carrageenan (HY-125474), single dose) dose-dependently relieves Carrageenan-induced acute inflammatory thermal hyperalgesia in rats[3].
A-425619 (35 mg/kg (100 μmol/kg), p.o., twice daily for 5 days) maintains efficacy in relieving skin incision-induced mechanical allodynia in rats[3].
A-425619 (35-103 mg/kg (100-300 μmol/kg), i.p., 30 min before testing, single dose) reduces MIA-induced osteoarthritic pain in rats[3].
A-425619 (35 mg/kg (100 μmol/kg), i.p., 30 min before testing, single dose) reduces mechanical allodynia in L5/L6 spinal nerve ligation model and in sciatic nerve ligation model of neuropathic pain in rats[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Capsaicin-induced mechanical hyperalgesia model in rats: 2 μg/10 μL of capsaicin solution was subcutaneously injected into the plantar aspect of the right hind paw of rats[3]
Dosage: 10.3-103 μg/rats (30-300 nmol/rats)
Administration: intraplantar 15 min before Capsaicin for a single dose
Result: Showed dose-dependent blocking effects on capsaicin-induced mechanical hyperalgesia.
Showed no effect on the paw withdrawal threshold of the capsaicin-injected paw when 300 nmol/rat was injected into the contralateral paw.
Animal Model: Capsaicin-induced mechanical hyperalgesia model in rats: 2 μg/10 μL of capsaicin solution was subcutaneously injected into the plantar aspect of the right hind paw of rats[3]
Dosage: 10.3-35 mg/kg (30-100 μmol/kg)
Administration: p.o. 60 min before Capsaicin for a single dose
Result: Showed dose-dependent preventive effects on capsaicin-induced mechanical hyperalgesia.
Achieved full efficacy at 35 mg/kg (100 μmol/kg), with an ED50 of 45 μmol/kg.
Significantly increased the paw withdrawal threshold compared with vehicle-treated rats that received Capsaicin.
Animal Model: Complete Freund’s adjuvant (CFA)-induced chronic inflammatory pain model in rats: 150 μL of 50% CFA solution was injected into the plantar surface of the right hind paw of rats[3]
Dosage: 3.5-35 mg/kg (10-100 μmol/kg) or 3.5-103 mg/kg (10-300 μmol/kg)
Administration: i.p. 30 min before testing for a single dose or p.o. 60 min before testing for a single dose
Result: Relieved CFA-induced thermal hyperalgesia, with an ED50 of 51 μmol/kg administered intraperitoneally.
Relieved CFA-induced thermal hyperalgesia, with an ED50 of 40 μmol/kg administered orally.
Animal Model: Complete Freund’s adjuvant (CFA)-induced chronic inflammatory pain model in rats: 150 μL of 50% CFA solution was injected into the plantar surface of the right hind paw of rats[3]
Dosage: 103 mg/rats (300 nmol/rats)
Administration: intraplantar into inflamed paw 30 min before testing for a single dose
Result: Produced a 56.2% reduction in CFA-induced thermal hyperalgesia.
Animal Model: Carrageenan-induced acute inflammatory pain model in rats: 100 μL of 1% λ-carrageenan solution was injected into the plantar surface of the right hind paw of rats[3]
Dosage: 3.5-35 mg/kg (10-100 μmol/kg)
Administration: i.p. 90 min after Carrageenan (HY-125474) for a single dose
Result: Relieved carrageenan-induced thermal hyperalgesia, with an ED50 of 50 μmol/kg.
Animal Model: Skin incision postoperative pain model in rats: a 1-cm longitudinal incision was made on the plantar surface (starting 0.5 cm from the proximal edge of the heel and extending toward the toes), the plantaris muscle was elevated and incised longitudinally (with origin and insertion intact), the skin was closed with two 5-0 nylon sutures[3]
Dosage: 35 mg/kg (100 μmol/kg)
Administration: p.o. twice daily for 5 days
Result: Produced a 42.6% reduction in mechanical allodynia when tested at 24 hours after surgery (day 2), and still exerted a 37.6% analgesic effect on day 5 after surgery.
Animal Model: Monoiodoacetate (MIA)-induced osteoarthritic pain model in rats: under light halothane anesthesia, a single intra-articular injection of 3 mg MIA (dissolved in 0.05 ml sterile isotonic saline) was administered into the knee joint cavity of rats[3]
Dosage: 35-103 mg/kg (100-300 μmol/kg)
Administration: i.p. 30 min before testing for a single dose
Result: Reduced MIA-induced increase in weight-bearing difference between the injured and non-injured hind limbs.
Animal Model: Spinal nerve (L5/L6) ligation neuropathic pain model in rats: a 1.5-cm incision was made dorsal to the lumbosacral plexus, the left L5 and L6 spinal nerves were isolated and tightly ligated with 3-0 silk threads[3]
Dosage: 35 mg/kg (100 μmol/kg)
Administration: i.p. 30 min before testing for a single dose
Result: Reduced mechanical allodynia induced by spinal nerve injury.
Molecular Weight

345.32

Formula

C18H14F3N3O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC(F)(F)C(C=C1)=CC=C1CNC(NC2=CC=CC3=C2C=CN=C3)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (289.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8959 mL 14.4793 mL 28.9586 mL
5 mM 0.5792 mL 2.8959 mL 5.7917 mL
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* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8959 mL 14.4793 mL 28.9586 mL 72.3966 mL
5 mM 0.5792 mL 2.8959 mL 5.7917 mL 14.4793 mL
10 mM 0.2896 mL 1.4479 mL 2.8959 mL 7.2397 mL
15 mM 0.1931 mL 0.9653 mL 1.9306 mL 4.8264 mL
20 mM 0.1448 mL 0.7240 mL 1.4479 mL 3.6198 mL
25 mM 0.1158 mL 0.5792 mL 1.1583 mL 2.8959 mL
30 mM 0.0965 mL 0.4826 mL 0.9653 mL 2.4132 mL
40 mM 0.0724 mL 0.3620 mL 0.7240 mL 1.8099 mL
50 mM 0.0579 mL 0.2896 mL 0.5792 mL 1.4479 mL
60 mM 0.0483 mL 0.2413 mL 0.4826 mL 1.2066 mL
80 mM 0.0362 mL 0.1810 mL 0.3620 mL 0.9050 mL
100 mM 0.0290 mL 0.1448 mL 0.2896 mL 0.7240 mL
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A-425619 Related Classifications

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  • 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:

A-425619581809-67-8A425619A 425619TRP ChannelCalcium ChannelTransient receptor potential channelsCa2+ channelsCa channelsinflammationtissue injuryTRPV1Inhibitorinhibitorinhibit

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