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Pathways Recommended:	Membrane Transporter/Ion Channel

Results for "

CaV2.2 channel

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Calcium Channel (14) Drug Isomer (1) GABA Receptor (1) nAChR (2)
By Research Areas:	Cardiovascular Disease (1) Endocrinology (1) Neurological Disease (13)

Inhibitors & Agonists

Peptides

Targets Recommended: Calcium Channel CRAC Channel Na+/Ca2+ Exchanger CaSR Calmodulin CaMK

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-119373

Cav 2.2 blocker 1 1 Publications Verification	Calcium Channel	Neurological Disease
Cav 2.2 blocker 1 (compound 9) is a *N-type calcium channel* (Cav 2.2) blocker for the treatment of pain, with an IC₅₀** of 1 nM .

HY-115597

BTT-266	Calcium Channel	Neurological Disease
BTT-266 is an antagonist forcalcium channel, through suppression of the Ca_Vα_1-AID-Ca_Vβ₃ interaction, with a K_i of 1.4 μM. BTT-266 modulates the activation of voltage-dependent Ca_V2.2. BTT-266 exhibits analgesic efficacy against neuropathic pain in rats model .

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].

HY-147638

MONIRO-1	Calcium Channel	Neurological Disease
MONIRO-1 is a T-type and N-type calcium channel blocker with IC₅₀ values of 34, 3.3, 1.7 and 7.2 µM against hCa_v2.2, hCa_v3.1, hCa_v3.2 and hCa_v3.3, respectively. MONIRO-1 has low activity against L-type calcium channels. MONIRO-1 can be used for the study of pain and epilepsy .

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-132268

Cav 2.2 blocker 2	Calcium Channel	Neurological Disease
Cav 2.2 blocker 2 is a **Cav2.2 calcium channel** blocker extracted from patent WO2017046581A1, compound 1. Cav 2.2 blocker 2 can reverses hyperalgesia associated with an injury or inflammation in conjunction with the opioid .

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-147639

Cav 2.2/3.2 blocker 1	Calcium Channel	Neurological Disease
Cav 2.2/3.2 blocker 1 (Compound 9e) is a neuronal calcium channel blocker with IC₅₀ values of 78 μM and 80 μM against *Ca_v2.2* and *Ca_v3.2, respectively. Cav 2.2*/3.2 blocker 1 can penetrate the CNS .

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-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-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 .

HY-180400

PAM-2	nAChR Calcium Channel	Neurological Disease
PAM-2 is a potent, orally active, CNS-penetrant selective α7 nAChR positive allosteric modulator (human α7 nAChR EC₅₀: 39 μM, rat α7 nAChR EC₅₀: 12 μM) with anti-nociceptive and anti-inflammatory activity. PAM-2 exhibits selectivity over α9α10 nAChR (IC₅₀ = 174 μM) and *Ca_V2.2* channel (IC₅₀ = 89 μM). PAM-2 decreases Streptozotocin (STZ) (HY-13753)- and Oxaliplatin (HY-17371)-inducned nuroparhic pain in mice by α7 nAChR potentiation. PAM-2 can be used for the research of neuropathic 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 .

Cat. No.	Product Name	Target	Research Area

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].

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-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 .

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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

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