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Pathways Recommended: Membrane Transporter/Ion Channel
Results for "

Cav3.1 channels

" in MedChemExpress (MCE) Product Catalog:

17

Inhibitors & Agonists

3

Peptides

1

Isotope-Labeled Compounds

Cat. No. Nombre del producto Target Áreas de investigación Chemical Structure
  • HY-111828
    TTA-A2
    1 Publications Verification

    		 Calcium Channel Neurological Disease
    TTA-A2 is a potent, selective and orally active t-type voltage gated calcium channel antagonist with reduced pregnane X receptor (PXR) activation. TTA-A2 is equally potent against the Cav3.1 (a1G) and Cav3.2 (a1H) channels with IC50 values of 89 nM and 92 nM, respectively, at -80 and -100 mV holding potentials. TTA-A2 can be used for the research of a variety of human neurological diseases, including sleep disorders and epilepsy .
    TTA-A2
  • HY-103309
    ML218
    2 Publications Verification

    		 Calcium Channel Neurological Disease
    ML218 is a potent, selective and orally active T-type Ca 2+ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor with IC50s of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. ML218 inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 has no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. ML218 can penetrate the blood-brain barrier .
    ML218
  • HY-132184
    5,6-Epoxyeicosatrienoic acid

    5,6-EET; (±)5,6-EpETrE

    		 Adrenergic Receptor Calcium Channel Endocrinology
    5,6-Epoxyeicosatrienoic acid (5,6-EET; (±)5,6-EpETrE) is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5,6-Epoxyeicosatrienoic acid degrades into 5,6-DiHET and 5,6-δ-lactone, which can be converted to 5,6-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5,6-Epoxyeicosatrienoic acid has been implicated in the mobilization of calcium and hormone secretion. 5,6-Epoxyeicosatrienoic acid is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC50=0.54 μM), and Cav3. and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2.
    5,6-Epoxyeicosatrienoic acid
  • HY-120597
    SAK3

    		Calcium Channel Neurological Disease
    SAK3 is a potent T-type voltage-gated Ca 2+ channels (T-VGCCs) enhancer. SAK3 enhances Cav3.1 and Cav3.3 T-type Ca 2+ channel currents. Acute SAK3 administration improves memory deficits in olfactory-bulbectomized mice . SAK3 inhibits amyloid β plaque formation in APP-KI mice by activating the proteasome activity .
    SAK3
  • HY-P3269
    Calciseptine

    		Calcium Channel Cardiovascular Disease
    Calciseptine is a natural polypeptide toxin found in the venom of the black mamba snake (Dendroaspis p. polylepis). Calciseptine is a highly effective and selective blocker of the L-type channel of the Cav1.2 subtype, with an IC50 value of 92 nM. Calciseptine has no effect on Cav3.1, Cav2.2, Cav2.1, Cav1.1, voltage-sensitive sodium channels and potassium channels. Calciseptine exhibits negative inotropic and negative relaxant effects on mice, and does not affect heart rate or the action potential of sinoatrial node pacemaker cells. Calciseptine can be used for research on cardiovascular diseases[1].
    Calciseptine
  • HY-50707
    (Rac)-TTA-P2

    (Rac)-T-Type calcium channel inhibitor

    		 Calcium Channel Drug Isomer Neurological Disease
    (Rac)-TTA-P2 is the isomer of TTA-P2 (HY-10035), and can be used as an experimental control. TTA-P2 (T-Type calcium channel inhibitor) is a potent inhibitor of T-Type calcium channel. TTA-P2 penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. TTA-P2 has the potential for the research of neurology disease .
    (Rac)-TTA-P2
  • HY-177955
    α-Obscurine derivative-1

    		Calcium Channel Drug Derivative Neurological Disease
    α-Obscurine derivative-1 (Compound 7) is a α-Obscurine (HY-134036) derivative. α-Obscurine derivative-1 inhibits CaV3.1 ion channel current with an IC50 of 0.19 μM. α-Obscurine derivative-1 can be used in the research of neurological disorders .
    α-Obscurine derivative-1
  • HY-10035A
    (R)-TTA-P2

    		Calcium Channel Neurological Disease
    (R)-TTA-P2 is the isomer of TTA-P2 (HY-10035), and can be used as an experimental control. TTA-P2 (T-Type calcium channel inhibitor) is a potent inhibitor of T-Type calcium channel. TTA-P2 penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. TTA-P2 has the potential for the research of neurology disease .
    (R)-TTA-P2
  • HY-156889
    Cav 3.1 blocker 1

    		Calcium Channel Neurological Disease
    Cav 3.1 blocker 1 (compound 12) is a T-type calcium channel blocker with an IC50value of 160 nM for Cav3.1. Cav 3.1 blocker 1 weakly inhibits Cav 3.2 (IC50 of 5000 nM), and shows no inhibition on Cav 3.3 and Cav 1.2 (IC50 of >10000 nM) .
    Cav 3.1 blocker 1
  • HY-P5793
    GTx1-15

    		Sodium Channel Calcium Channel Neurological Disease
    GTx1-15 is an inhibitor cystine knot (ICK) peptide that inhibits the voltage-dependent calcium channel Cav3.1 and the voltage-dependent sodium channels Nav1.3 and Nav1.7 .
    GTx1-15
  • HY-122201
    NSC156529

    		Calcium Channel Neurological Disease Cancer
    NSC156529 is a potent T-type calcium-channel antagonist. NSC156529 shows inhibits on Cav3.1 and Cav3.2 and o Cav3.3 without effect. NSC156529 has the potential for the research of neuropsychic and genital system diseases .
    NSC156529
  • HY-P5869
    Kurtoxin

    		Calcium Channel Sodium Channel Neurological Disease
    Kurtoxin is a selective Cav3 (T-type) voltage-gated Ca 2+ channel gating inhibitor with a Kd of 15 nM for Cav3.1 (α1G T-type) Ca 2+ channel. Kurtoxin can interact with high affinity with native neuronal high-threshold L-type, N-type, and P-type Ca 2+ channels in central and peripheral neurons. Kurtoxin also shows cross-reactivity with voltage-gated Na + channel .
    Kurtoxin
  • HY-103309A
    ML218 hydrochloride

    		Calcium Channel Neurological Disease
    ML218 hydrochloride is a potent, selective and orally active T-type Ca 2+ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor with IC50s of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. ML218 hydrochloride inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 hydrochloride has no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. ML218 hydrochloride can penetrate the blood-brain barrier .
    ML218 hydrochloride
  • HY-103309S
    ML218-d9

    		Calcium Channel Neurological Disease
    ML218-d9 is the deuterium labeled ML218. ML218 is a potent, selective and orally active T-type Ca2+ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor with IC50s of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. ML218 inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 has no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. ML218 can penetrate the blood-brain barrier .
    ML218-d9
  • HY-147708
    T-Type calcium channel inhibitor 2

    		Calcium Channel Cancer
    T-Type calcium channel inhibitor 2 (compound 6g) is a potent T-type calcium channel inhibitor with IC50s of 31.0, 83.1, 69.3 µM for Cav3.1 (α1G), Cav3.2 (α1H), Cav3.3 (α1I) (α1H), respectively. T-Type calcium channel inhibitor 2 shows cytotoxicity for A549, HCT-116 cells with IC50s of 5.0, 6.4 µM, respectively .
    T-Type calcium channel inhibitor 2
  • HY-118030
    RQ-00311651

    		Calcium Channel Neurological Disease
    RQ-00311651 is a T-type calcium channel blocker that specifically targets the Cav3.2 isoform with a role in neuropathic and visceral pain. RQ-00311651 significantly inhibits T currents in HEK293 cells expressing human Cav3.1 or Cav3.2. RQ-00311651 also inhibited high potassium-induced calcium signaling. RQ-00311651 also inhibits antiallergic properties in rats and mice with neuropathic pain induced by spinal nerve injury or Paclitaxel (HY-B0015). Oral and intraperitoneal injection (10-20 mg/kg) inhibits Cerulein (HY-A0190)-induced acute pancreatitis and cyclophosphamide-induced cystitis in mice .
    RQ-00311651
  • HY-103309R
    ML218 (Standard)

    		Reference Standards Calcium Channel Neurological Disease
    ML218 (Standard) is the analytical standard of ML218 (HY-103309). This product is intended for research and analytical applications. ML218 is a potent, selective and orally active T-type Ca2+ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor with IC50s of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. ML218 inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 has no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. ML218 can penetrate the blood-brain barrier .
    ML218 (Standard)

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