Search Result

Results for "

CAV2 Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (1) Calcium Channel (12) COX (1) Drug Isomer (1) Epigenetic Reader Domain (1) GABA Receptor (1) Histone Acetyltransferase (1) IKZF Family (1) Interleukin Related (1) MDM-2/p53 (1) nAChR (1) Notch (1) TNF Receptor (1)
By Research Areas:	Cancer (1) Cardiovascular Disease (1) Endocrinology (1) Inflammation/Immunology (3) Neurological Disease (11)

Inhibitors & Agonists

Peptides

Natural
Products

Targets Recommended: Serpin

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-120751

TROX-1	Calcium Channel	Neurological Disease
TROX-1 is a selective, orally active and brain-penetrant N-type calcium channel (Cav2.2) inhibitor with an IC₅₀ value of 0.11 μM. TROX-1 exerts state-dependent and use-dependent inhibition, preferentially targets open/inactivated channels, blocks depolarization-associated calcium influx, and fully blocks calcium influx in rat dorsal root ganglion neurons. TROX-1 reverses inflammatory-induced hyperalgesia, nerve injury-induced allodynia. TROX-1 can be used for the research of pain .

HY-P1080

ω-Agatoxin IVA 1 Publications Verification	Calcium Channel	Cardiovascular Disease Neurological Disease
ω-Agatoxin IVA is a potent, selective P/Q type Ca ²⁺ (Cav2.1) channel blocker with IC₅₀ values of 2 nM and 90 nM. ω-Agatoxin IVA inhibits glutamate exocytosis and calcium influx elicited by high potassium. ω-Agatoxin IVA inhibits Capsaicin (HY-10448)-induced CGRP release and vasodilation. ω-Agatoxin IVA can be used for the research of neurological and cardiovascular disease .

HY-P1080A

ω-Agatoxin IVA TFA 1 Publications Verification	Calcium Channel	Neurological Disease
ω-Agatoxin IVA TFA is a potent, selective P/Q type Ca ²⁺ (Cav2.1) channel blocker with IC₅₀ values of 2 nM and 90 nM. ω-Agatoxin IVA TFA inhibits glutamate exocytosis and calcium influx elicited by high potassium. ω-Agatoxin IVA TFA inhibits Capsaicin (HY-10448)-induced CGRP release and vasodilation. ω-Agatoxin IVA TFA can be used for the research of neurological and cardiovascular disease .

HY-148866

Cavα2δ1&NET-IN-3	Calcium Channel	Neurological Disease Endocrinology
Cavα2δ1&NET-IN-3 (example 216) is an inhibitor of the subunit α2δ of voltage-gated calcium channels (VGCC) and noradrenaline transporter (NET). Cavα2δ1&NET-IN-3 has K_is of 100-500 nM for human α2δ-1 subunit of Ca_v2.2 calcium channel and NET, respectively .

HY-P10898

GeX-2	nAChR Calcium Channel GABA Receptor	Neurological Disease
GeX-2 is a truncated analogue of αO-conotoxin. GeX-2 activates GABA_B receptor. GeX-2 inhibits α9α10 nAChR and *Ca_V2.2* channels. GeX-2 alleviates pain in the rat model of chronic constriction injury .

HY-169845

Calcium Channel antagonist 6	Calcium Channel	Neurological Disease
Calcium Channel antagonist 6 (Compound 328) is a highly selective antagonist of voltage-gated calcium channel CaV2.2 with an IC₅₀ value of 0.37 μM. Calcium Channel antagonist 6 inhibits of neuron depolarization-induced Ca ²⁺ influx. Calcium Channel antagonist 6 is promising for research of neuropathic pain .

HY-P5874

Myr-TAT-CBD3	Calcium Channel	Inflammation/Immunology
Myr-TAT-CBD3 is *CRMP2-CaV2.2* interaction inhibitor. Myr-tat-CBD3 can significantly attenuate carrageenan-induced thermal hypersensitivity and reverse thermal hypersensitivity induced in a rat model of postoperative pain. Myr-TAT-CBD3 can be used to study inflammation and postoperative pain .

HY-P5813

Cd1a β-TRTX-cd1a; β-Theraphotoxin-cd1a	Calcium Channel	Neurological Disease
Cd1a is a β-toxin derived from the African spider Ceratogyrus darlingi. Cd1a can regulate calcium ion channels. Cd1a inhibits human calcium ion channels (Ca_v2.2)(IC₅₀2.6 μM) and mouse sodium ion channels (Na_v1.7). Cd1a can be used in the development of peripheral pain treatment drugs .

HY-181612

COX-2/CaV2.2-IN-1	COX Calcium Channel Interleukin Related TNF Receptor	Neurological Disease Inflammation/Immunology
COX-2/CaV2.2-IN-1 is an orally active and selective dual *COX-2/CaV2.2* inhibitor, exhibiting a COX-2 IC₅₀ of 0.26 μM and a *CaV2.2* IC₅₀ of 0.29 μM. COX-2/CaV2.2-IN-1 suppresses inflammatory responses and inflammatory mediator (IL-6, TNF-α, NO) production. COX-2/CaV2.2-IN-1 produces pronounced analgesic effects in diverse models of inflammatory, neuropathic, and visceral pain. COX-2/CaV2.2-IN-1 can be used for the research of chronic pain .

HY-115596

BTT-369	Calcium Channel	Neurological Disease
BTT-369 is a Ca_Vα₁·Ca_Vβ₃ protein-protein complex antagonist with a K_i of 2.0 μM. BTT-369 inhibits *Ca_V2.2* currents, with an apparent IC₅₀ value of 31 μM. BTT-369 disrupts the interaction between Ca_Vα₁ and Ca_Vβ₃ subunits. BTT-369 reduces the current density of *Ca_V2.2, and shifts the voltage dependence of steady-state inactivation and activation of Ca_V2.2* to more positive potentials. BTT-369 alleviates mechanical hyperalgesia in a rat model of tibial nerve injury. BTT-369 can be used for the study of neuropathic pain .

HY-N12768

Rhodojaponin VI	MDM-2/p53 Notch Calcium Channel	Neurological Disease Inflammation/Immunology
Rhodojaponin VI is an orally active diterpenoid compound found in hododendron molle G. Don (Ericaceae) (RM). Rhodojaponin VI binds rat N-Ethylmaleimide-sensitive fusion (NSF) with a Kd of 1.03 μM. Rhodojaponin VI blocks the MDM2-Notch1 signalling pathway by reducing MDM2 and Notch1 expression. Rhodojaponin VI indirectly reduces *Cav_2.2* current intensity by inhibiting NSF-mediated Cav2.2 trafficking. Rhodojaponin VI alleviates glomerulonephritis progression and podocyte injury in passive heymann nephritis rats. Rhodojaponin VI also has antinociceptive effects. Rhodojaponin VI can be used for the researches of heymann nephritis and pain .

HY-181957

KB528	Epigenetic Reader Domain Histone Acetyltransferase Apoptosis IKZF Family	Cancer
KB528 is a p300/CBP histone acetyltransferase (KAT) inhibitor with low nM IC₅₀ values against human p300 and CBP, and exhibits selectivity over other KAT family members. KB528 modulates the IRF4 transcriptional network, downregulates the expression of IRF4, MYC, *CAV2* and IGLL5, and reduces the protein level of IKZF3. KB528 potently induces apoptosis in multiple myeloma cells. KB528 is applicable to research related to multiple myeloma .

HY-120751A

(S)-TROX-1	Drug Isomer Calcium Channel	Neurological Disease
(S)-TROX-1 is the S-enantiomer of TROX-1 (HY-120751). TROX-1 is a selective, orally active and brain-penetrant N-type calcium channel (Cav2.2) inhibitor with an IC₅₀ value of 0.11 μM. TROX-1 exerts state-dependent and use-dependent inhibition, preferentially targets open/inactivated channels, blocks depolarization-associated calcium influx, and fully blocks calcium influx in rat dorsal root ganglion neurons. TROX-1 reverses inflammatory-induced hyperalgesia, nerve injury-induced allodynia. TROX-1 can be used for the research of pain .

Cat. No.	Product Name	Target	Research Area

HY-P1080

ω-Agatoxin IVA 1 Publications Verification	Calcium Channel	Cardiovascular Disease Neurological Disease
ω-Agatoxin IVA is a potent, selective P/Q type Ca ²⁺ (Cav2.1) channel blocker with IC₅₀ values of 2 nM and 90 nM. ω-Agatoxin IVA inhibits glutamate exocytosis and calcium influx elicited by high potassium. ω-Agatoxin IVA inhibits Capsaicin (HY-10448)-induced CGRP release and vasodilation. ω-Agatoxin IVA can be used for the research of neurological and cardiovascular disease .

HY-P1080A

ω-Agatoxin IVA TFA 1 Publications Verification	Calcium Channel	Neurological Disease
ω-Agatoxin IVA TFA is a potent, selective P/Q type Ca ²⁺ (Cav2.1) channel blocker with IC₅₀ values of 2 nM and 90 nM. ω-Agatoxin IVA TFA inhibits glutamate exocytosis and calcium influx elicited by high potassium. ω-Agatoxin IVA TFA inhibits Capsaicin (HY-10448)-induced CGRP release and vasodilation. ω-Agatoxin IVA TFA can be used for the research of neurological and cardiovascular disease .

HY-P10898

GeX-2	nAChR Calcium Channel GABA Receptor	Neurological Disease
GeX-2 is a truncated analogue of αO-conotoxin. GeX-2 activates GABA_B receptor. GeX-2 inhibits α9α10 nAChR and *Ca_V2.2* channels. GeX-2 alleviates pain in the rat model of chronic constriction injury .

HY-P5874

Myr-TAT-CBD3	Calcium Channel	Inflammation/Immunology
Myr-TAT-CBD3 is *CRMP2-CaV2.2* interaction inhibitor. Myr-tat-CBD3 can significantly attenuate carrageenan-induced thermal hypersensitivity and reverse thermal hypersensitivity induced in a rat model of postoperative pain. Myr-TAT-CBD3 can be used to study inflammation and postoperative pain .

HY-P5813

Cd1a β-TRTX-cd1a; β-Theraphotoxin-cd1a	Calcium Channel	Neurological Disease
Cd1a is a β-toxin derived from the African spider Ceratogyrus darlingi. Cd1a can regulate calcium ion channels. Cd1a inhibits human calcium ion channels (Ca_v2.2)(IC₅₀2.6 μM) and mouse sodium ion channels (Na_v1.7). Cd1a can be used in the development of peripheral pain treatment drugs .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N12768

Rhodojaponin VI	Structural Classification Terpenoids Diterpenoids Pieris japonica (Thunb.) D. Don ex G. Don Ericaceae Plants Source Classification	MDM-2/p53 Notch Calcium Channel
Rhodojaponin VI is an orally active diterpenoid compound found in hododendron molle G. Don (Ericaceae) (RM). Rhodojaponin VI binds rat N-Ethylmaleimide-sensitive fusion (NSF) with a Kd of 1.03 μM. Rhodojaponin VI blocks the MDM2-Notch1 signalling pathway by reducing MDM2 and Notch1 expression. Rhodojaponin VI indirectly reduces *Cav_2.2* current intensity by inhibiting NSF-mediated Cav2.2 trafficking. Rhodojaponin VI alleviates glomerulonephritis progression and podocyte injury in passive heymann nephritis rats. Rhodojaponin VI also has antinociceptive effects. Rhodojaponin VI can be used for the researches of heymann nephritis and pain .

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

We use cookies

MedChemExpress values your privacy and your trust is important to us. We use cookies to enhance your website experience. Some cookies are necessary to run the website. Privacy and Cookie Policy

Name
Email *

	Sorry, but the email address you supplied was invalid.

CAV2 Inhibitors

Inhibitors & Agonists

Peptides

NaturalProducts

Natural
Products