2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. Potassium Channel TSPO
  4. Kv7.2/Kv7.3 activator-3

Kv7.2/Kv7.3 activator-3 (GRT-X) is an orally active Kv7.2/Kv7.3 and TSPO activator. Kv7.2/Kv7.3 activator-3 activates Kv7.2/Kv7.3, Kv7.4, and Kv7.5 with EC50 values of 0.37, 2.06, and 0.75 μM, respectively, and binds to TSPO with Ki values of 0.07 μM (rat membrane) and 4.60 μM (human U-118 MG cells). Kv7.2/Kv7.3 activator-3 prevents motor neuron degeneration in mice and humans conditioned by ALS/FTD astrocytes. Kv7.2/Kv7.3 activator-3 stimulates dorsal root ganglion axonal growth through TSPO and Kv7.2/3 activation. Kv7.2/Kv7.3 activator-3 has anti-epileptic effects in epileptic seizure models. Kv7.2/Kv7.3 activator-3 reduces pain hypersensitivity in patients with diabetic neuropathy, promotes neuronal survival and regeneration after cervical neuropathy in rats, and accelerates the recovery of normal function of sensory and motor neurons.

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Kv7.2/Kv7.3 activator-3

Kv7.2/Kv7.3 activator-3 Chemical Structure

CAS No. : 1361107-81-4

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Kv7.2/Kv7.3 activator-3 Related Antibodies

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Description

Kv7.2/Kv7.3 activator-3 (GRT-X) is an orally active Kv7.2/Kv7.3 and TSPO activator. Kv7.2/Kv7.3 activator-3 activates Kv7.2/Kv7.3, Kv7.4, and Kv7.5 with EC50 values of 0.37, 2.06, and 0.75 μM, respectively, and binds to TSPO with Ki values of 0.07 μM (rat membrane) and 4.60 μM (human U-118 MG cells). Kv7.2/Kv7.3 activator-3 prevents motor neuron degeneration in mice and humans conditioned by ALS/FTD astrocytes. Kv7.2/Kv7.3 activator-3 stimulates dorsal root ganglion axonal growth through TSPO and Kv7.2/3 activation. Kv7.2/Kv7.3 activator-3 has anti-epileptic effects in epileptic seizure models. Kv7.2/Kv7.3 activator-3 reduces pain hypersensitivity in patients with diabetic neuropathy, promotes neuronal survival and regeneration after cervical neuropathy in rats, and accelerates the recovery of normal function of sensory and motor neurons[1][2][3][4].

IC50 & Target[1][2][3][4]

KV7.2

0.37 μM (EC50)

KV7.4

2.06 μM (EC50)

KV7.5

0.75 μM (EC50)

In Vitro

Kv7.2/Kv7.3 activator-3 (6.25-25 μM, 20 days) shows reduction in motoneurons (MNs) death in SCOCs[1].
Kv7.2/Kv7.3 activator-3 (0.1-10 μM, 4 days) does not reduce MNs survival up to 2.5 μM in rat primary spinal cord cultures (VSCNs)[1].
Kv7.2/Kv7.3 activator-3 (6.25-25 μM, 4 days) preserves MNs viability in SCOCs treated with human SOD1G93A-ACM/SOD1D90A-ACM/TDP43A90V-ACM[1].
Kv7.2/Kv7.3 activator-3 (1-2.5 μM, 4 days) rescues MNs death, reduces DCF counts in VSCNs treated with human SOD1G93A-ACM/SOD1D90A-ACM/TDP43A90V-ACM[1].
Kv7.2/Kv7.3 activator-3 (10 μM, 4 days) enhances the length and density of the neurite network, with a marked increase in AUC in embryonic C57BL6/J DRG[2].
Kv7.2/Kv7.3 activator-3 (10 μM, 8 days) maintains positive effect on axonal growth, increases AUCs in E13.5 DRG explants[2].
Kv7.2/Kv7.3 activator-3 (10 μM, 4 days) induces increased expression of genes involved in myelination, Schwann cell and neuronal development and differentiation, and axonal structure in E13.5 DRG explants [2].
Kv7.2/Kv7.3 activator-3 (10 μM, 4 days) has no effect on neurite outgrowth, but increases expression of genes associated with myelination and Schwann cell and neuronal development, but not genes involved in axonal structure in DIV4 embryonic TSPO-KO DRG explants[2].
Kv7.2/Kv7.3 activator-3 activates neuronal hKv7.2/3, hKv7.4, and hKv7.5 channels with a higher potency than retigabine in CHO-K1 cells[3].
Kv7.2/Kv7.3 activator-3 (10 μM) leads a potent and efficient hyperpolarization of the resting membrane potential (EC50 = 0.201 μM, maximal hyperpolarization: 13.2 mV) in cultured rat DRG neurons[4].
Kv7.2/Kv7.3 activator-3 (10 μM) binds to rat heart membranes with high and to human U-118 MG glioblastoma cells with moderate affinity in TSPO binding assays, enhances pregnenolone synthesis by cultured rat C6 glioma cells in TSPO functional assay[4].

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

Kv7.2/Kv7.3 activator-3 Related Antibodies

Immunofluorescence[1]

Cell Line: SCOCs treated with SOD1G93A-ACM/SOD1D90A-ACM
Concentration: 6.25 μM, 12.5 μM,25 μM
Incubation Time: 4 days
Result: Preserved MN viability.

RT-PCR[1]

Cell Line: E13.5 DRG explants
Concentration: 10 μM
Incubation Time: 4 days
Result: Induced a significant increase in the mRNA expression of TSPO, Kv7.2, Kv7.3, myelin-related genes (Mpz, Mbp and Plp), Dhh, Krox20 and CNPase, and increased the total mRNA expression levels of Tfap2α, Stmn2, Peripherin, Cad19, and Nfh genes.

RT-PCR[1]

Cell Line: SPO-KO DRG explants
Concentration: 10 μM
Incubation Time: 4 days
Result: Increased Kv7.2, Kv7.3, Mpz, Mbp, Plp, Dhh, CNPase Tfap2α, and Cad19 mRNA levels, and decreased Stmn2 expression.
In Vivo

Kv7.2/Kv7.3 activator-3 (10 mg/kg, p.o., once) increases brain levels of neurosteroids and steroid in SD rat model[3].
Kv7.2/Kv7.3 activator-3 (0-10 mg/kg, p.o., once) prevents the occurrence of tonic epileptic seizures in Maximal electroshock seizure (MES) seizure male Wistar rats model[3].
Kv7.2/Kv7.3 activator-3 (0-3 mg/kg, p.o., once) increases seizure threshold in Electroconvulsive seizure (ECS) seizure male Wistar rats model[3].
Kv7.2/Kv7.3 activator-3 (0-100 mg/kg, p.o., once) increases latency to clonic seizures, decreases the incidence of tonic seizures in pentylenetetrazol (PTZ) seizure male Wistar rats model[3].
Kv7.2/Kv7.3 activator-3 (0-100 mg/kg, p.o., once) reduces incidence of tonic convulsions in PTZ seizure male SD rats model[3].
Kv7.2/Kv7.3 activator-3 (0-10 mg/kg, p.o., once) reduces the incidence of wild-running and clonic seizures, and prevents tonic seizures and mortality in male Rj:DBA/2 mice model[3].
Kv7.2/Kv7.3 activator-3 (0-100 mg/kg, p.o., once) prevents 6-Hz seizures in male NMRI mice model[3].
Kv7.2/Kv7.3 activator-3 (0.316-10 mg/kg, p.o., once) reduces hyperalgesia in Streptozotocin (STZ) (HY-13753)-induced chronic neuropathic pain (CNP) SD rats model[4].
Kv7.2/Kv7.3 activator-3 (5-10 mg/kg, p.o., once) promotes the survival and regeneration of neurons, accelerating the recovery of normal functions of sensory neurons and motor neuronsin severe cervical spinal nerve compression injury SD rats model[4].

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

Animal Model: Male SD rat (200-230 g) model[3]
Dosage: 10 mg/kg
Administration: p.o., once
Result: Increased brain levels of neurosteroids, including 3α,5α-THP and 3α,5α-THDOC, increased 627% (pregnenolone), 107% (progesterone), 116% (5-α-dihydroprogesterone), 132% (3α,5α-THP), 4911% (deoxycorticosterone), 1333% (5α-deoxycorticosterone), and 1040% (3α,5α-THDOC), respectively in brain steroid levels.
Animal Model: MES seizure male Wistar rats (200-230 g) model[3]
Dosage: 0 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg
Administration: p.o., once
Result: Prevented the occurrence of tonic epileptic seizures, with an ED50 of 3.7 mg/kg.
Animal Model: ECS seizure male Wistar rats (200-230 g) model[3]
Dosage: 0 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg
Administration: p.o., once
Result: Increased seizure threshold.
Animal Model: PTZ seizure male Wistar rats (200-230 g) model[3]
Dosage: 0 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg
Administration: p.o., once
Result: Increased latency to clonic seizures, decreased the incidence of PTZ-induced tonic seizures with ED50 of 37 mg/kg.
Animal Model: PTZ seizure male SD rats (200-230 g) model[3]
Dosage: 0 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg
Administration: p.o., once
Result: Reduced incidence of tonic convulsions.
Animal Model: Male Rj:DBA/2 mice (12-15 g) model[3]
Dosage: 0 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg
Administration: p.o., once
Result: Reduced the incidence of wild-running and clonic seizures, and prevented tonic seizures and mortality.
Animal Model: Male NMRI mice (21-25 g) model[3]
Dosage: 0 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg
Administration: p.o., once
Result: Prevented 6-Hz seizures with an ED50 of 13 mg/kg.
Animal Model: STZ-induced (75 mg/kg) CNP SD rats[4]
Dosage: 0.316, 1.0, 10 mg/kg
Administration: p.o., once
Result: Reduced mechanical hyperalgesia.
Animal Model: SD rats model[4]
Dosage: 10 mg/kg
Administration: p.o., once
Result: Increased the synthesis of anti-hyperalgesic neurosteroids.
Animal Model: Severe cervical spinal nerve compression injury SD rats model[4]
Dosage: 5 mg/kg, 10 mg/kg
Administration: p.o., once
Result: Had neuroprotective and regenerative effects, accelerated and improved functional recovery after traumatic peripheral nerve injury.
Molecular Weight

436.40

Formula

C22H20F4N2O3
CAS No.
SMILES

O=C(C1=C(C)C2=C(N(CCOC)C1=O)C=C(C(F)(F)F)C=C2)NCC3=CC=CC(F)=C3
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Please store the product under the recommended conditions in the Certificate of Analysis.
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References
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Kv7.2/Kv7.3 activator-3 Related Classifications

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Keywords:

Kv7.2/Kv7.3 activator-31361107-81-4Potassium ChannelTSPOKcsATranslocator ProteinActivatorMES seizureWistar ratsRj:DBA/2 miceNMRI miceCNPVSCNsSCOCsembryonic C57BL6/J DRGInhibitorinhibitorinhibit

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