Voltage-gated potassium channel Inhibitor

Voltage-gated potassium channel Inhibitors (28):

Cat. No.	Product Name	Effect	Purity

HY-18063

ML252	Inhibitor	99.9%
ML252 is a selective inhibitor of KCNQ2 (Kv7.2) channel with an IC₅₀s of 69 nM, 2.92 μM, 0.12 μM and 0.20 μM for KCNQ2, KCNQ1 (Kv7.1), KCNQ2/Q3 and KCNQ4, respectively. ML252 also inhibits Cytochrome P450 with IC₅₀s of 6.1 nM (CYP1A2), 18.9 nM (CYP2C9), 3.9 nM (CYP3A4), 19.9 nM (CYP2D6), respectively. ML252 shows highly brain penetrant .

HY-P3055A

Dendrotoxin-I TFA	Inhibitor	99.85%
Dendrotoxin-I (DTX-I) TFA is a potent K⁺ channel blocker with IC₅₀s of 0.13-50 nM for voltage-gated potassium channel subunits K_V1.1, K_V1.2 and K_V1.6. Dendrotoxin-I TFA, a neurotoxin, has the potential for cancer research.

HY-186059

HCN2 modulator-4	Inhibitor
HCN2 modulator-4 is a HCN2 ion channel inhibitor. HCN2 modulator-4 inhibits HCN2 ion channel activity. HCN2 modulator-4 can be used for the research of pain, inflammatory pain, neuropathic pain, tinnitus, central nervous system disorders, psychiatric disorders, mood disorders.

HY-186061A

HCN2 modulator-8	Inhibitor
HCN2 modulator-8 is a pyrazolopyridine derivative and selective HCN2 inhibitor. HCN2 modulator-8 can be used for the research of pain, tinnitus, central nervous system disorders, psychiatric disorders, mood disorders.

HY-P1427A

Guangxitoxin 1E TFA	Inhibitor
Guangxitoxin 1E TFA is the TFA salt form of Guangxitoxin 1E (HY-P1427). Guangxitoxin 1E TFA is a peptide toxin and a selective inhibitor for voltage-gated potassium channel K_V2.1 and K_V2.2 with IC₅₀ of 1-3 nM. Guangxitoxin 1E TFA enhances glucose-stimulated intracellular calcium ion oscillations and increases insulin secretion in a glucose-dependent manner.

HY-108574

CP 339818 hydrochloride	Inhibitor	99.61%
CP 339818 hydrochloride is a non-peptide Kv1.3 channel (IC₅₀ = 200 nM) and Kv1.4 channel blocker. CP 339818 hydrochloride inhibits HCN channel with IC₅₀s of 18.9 μM and 43.4 μM against HCN1 and HCN4 (high Cl^-). CP 339818 hydrochloride has significantly weaker blocking effects on Kv1.1, Kv1.2, Kv1.5, Kv1.6, Kv3.1-4, and Kv4.2 channels. CP 339818 hydrochloride selectively blocked Kv1.3, thereby inhibiting the activation process of human T cells. CP 339818 hydrochloride can be used to study the physiological functions of HCN and Kv channels.

HY-172930

PVTX-405	Inhibitor
PVTX-405 is a selective and oral active IKZF2 molecular glue degrader with a DC₅₀ of 0.7 nM and a D_max of 91%. PVTX-405 enhances degradation efficiency, significantly reduces off-target degradation, and alleviates hERG inhibition with IC₅₀ of 48 µM. PVTX-405 significantly inhibits the growth of MC38 tumors, with greater synergistic anti-cancer efficacy in combination with immune checkpoint therapies (ICTs) (anti-PD1 or anti-LAG3) in the MC38 mouse tumor xenograft model using Crbn^391V C57BL/6 mice.

HY-172374A

KV1.3-IN-2 hydrochloride	Inhibitor
KV1.3-IN-2 hydrochloride is a kv1.3 potassium channel inhibitor without affecting hERG channel activity. KV1.3-IN-2 hydrochloride can be used in research of immune-related diseases such as psoriasis, rheumatoid arthritis, and systemic lupus erythematosus.

HY-P1073

ProTx-I	Inhibitor
ProTx-I is a toxin derived from Thrixopelma pruriens and a peptide inhibitor targeting TTX-resistant sodium channels. ProTx-I interacts with voltage sensors of multiple domains such as NaV1.7, reduces neuronal excitability through allosteric modulation of channel gating and alteration of voltage dependence. The IC₅₀ values of ProTx-I against human NaV1.7, NaV1.2, NaV1.6, and NaV1.5 are 95 nM, 104 nM, 21 nM, and 358 nM, respectively; ProTx-I also potently inhibits Ba²⁺ currents of hCav3.1, while its inhibitory potency against hCav3.2 is approximately 160-fold lower. ProTx-I is applicable to the research of chronic pain.

HY-P1409A

ADWX 1 TFA	Inhibitor	98.37%
ADWX 1 TFA is a new peptide inhibitor that is potent and selective for Kv1.3 with an IC₅₀ value of 1.89 pM. ADWX 1 inhibits Kv1.3 channel activity specifically to inhibit both the initial calcium signaling and NF-κB activation. ADWX 1 TFA ameliorates the disease in rats of experimental autoimmune encephalomyelitis (EAE) models. ADWX 1 TFA can be used to study T cell-mediated autoimmune diseases.

HY-P5917A

Vm24-toxin TFA	Inhibitor
Vm24-toxin (Vaejovis mexicanus peptide 24) TFA, a 36-residue peptide, is a potent and selective Kv1.3 blocker with a K_d of ~3 pM in lymphocytes. Vm24-toxin TFA shows >1500-fold affinity for Kv1.3 over other assayed potassium channels. Vm24-toxin TFA folds into a distorted cystine-stabilized α/β motif consisting of a single-turn α-helix and a three-stranded antiparallel β-sheet, stabilized by four disulfide bridges. Vm24-toxin TFA attenuates the CD4⁺ effector memory T cell response to T cell receptor (TCR) stimulation.

HY-P5931

Spinoxin	Inhibitor	98.0%
Spinoxin isolated from the venom of scorpion Heterometrus spinifer, is a 34-residue peptide neurotoxin cross-linked by four disulfide bridges. Spinoxin is a potent inhibitor of Kv1.3 potassium channel (IC₅₀ = 63 nM), considering to be valid molecular targets in the diagnostics and therapy of various autoimmune disorders and cancers.

HY-18063A

ML252 hydrochloride	Inhibitor	98.5%
ML252 hydrochloride is a selective inhibitor of KCNQ2 (Kv7.2) channel with IC₅₀s of 69 nM, 2.92 μM, 0.12 μM and 0.20 μM for KCNQ2, KCNQ1 (Kv7.1), KCNQ2/Q3 and KCNQ4, respectively. ML252 hydrochloride also inhibits Cytochrome P450 with IC₅₀s of 6.1 nM (CYP1A2), 18.9 nM (CYP2C9), 3.9 nM (CYP3A4), 19.9 nM (CYP2D6), respectively. ML252 hydrochloride shows highly brain penetrant.

HY-172374

KV1.3-IN-2	Inhibitor
KV1.3-IN-2 is a kv1.3 potassium channel inhibitor without affecting hERG channel activity. KV1.3-IN-2 can be used in research of immune-related diseases such as psoriasis, rheumatoid arthritis, and systemic lupus erythematosus.

HY-168214

Kv7.2/Kv7.3 agonist 1	Inhibitor
Kv7.2/Kv7.3 agonist 1 (Compound 16) is an orally active agonist for KV7.2/7.3 channel (KCNQ2/3) with an EC₅₀ of 1.03 μM. Kv7.2/Kv7.3 agonist 1 exhibits analgesic efficacy in mice chronic constriction injury (CCI) model and mice Streptozotocin (HY-13753)-induced diabetic peripheral neuropathic pain (DPNP) model, with ED₅₀ of 12.02 and 9.63 mg/kg.

HY-113964

UK-78282	Inhibitor
UK-78282 is a selective Kv1.3 voltage-gated potassium channel inhibitor with an IC₅₀ of 200 nM. UK-78282 also inhibit Kv1.4 potassium channel. UK-78282 can inhibit human T cell activation.

HY-P5917

Vm24-toxin	Inhibitor
Vm24-toxin (Vaejovis mexicanus peptide 24), a 36-residue peptide, is a potent and selective Kv1.3 blocker with a K_d of ~3 pM in lymphocytes. Vm24-toxin shows >1500-fold affinity for Kv1.3 over other assayed potassium channels. Vm24-toxin folds into a distorted cystine-stabilized α/β motif consisting of a single-turn α-helix and a three-stranded antiparallel β-sheet, stabilized by four disulfide bridges. Vm24-toxin attenuates the CD4⁺ effector memory T cell response to T cell receptor (TCR) stimulation.

HY-P2707

α-Dendrotoxin	Inhibitor
α-Dendrotoxin (α-DTX) is a voltage-gated K⁺ channel blocker and an acid-sensing ion channel (ASIC) inhibitor. α-Dendrotoxin blocks K_v1.1, K_v1.2, K_v1.6 and D-type (I_D) voltage-gated K⁺ channels, and reversibly inhibits slowly inactivating potassium currents. α-Dendrotoxin induces epilepsy-related behaviors in mice. α-Dendrotoxin can be used in studies related to tonic-clonic seizures.

HY-P3055

Dendrotoxin-I	Inhibitor
Dendrotoxin-I (DTX-I) is a potent K⁺ channels blocker with IC₅₀s of 0.13-50 nM for voltage-gated potassium channel subunits K_V1.1, K_V1.2 and K_V1.6, respectively. Dendrotoxin-I, a neurotoxin, has the potential for cancer research.

HY-P2949

Pandinotoxin Kα	Inhibitor
Pandinotoxin Kα, isolated from the venom of Pandinus imperator, is the inhibitor of A-type potassium channel.

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