N-type calcium channel Inhibitor
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TROX-1
0 ImagesTROX-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.
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NP118809
0 ImagesSynonyms: 39-1B4NP118809 is a potent N-type calcium channel blocker, with an IC50 of 0.11 μM; also less potently inhibits L-type calcium channel with an IC50 of 12.2 μM.
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Cav 2.2 blocker 2
0 ImagesCav 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.
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MONIRO-1
0 ImagesMONIRO-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 hCav2.2, hCav3.1, hCav3.2 and hCav3.3, respectively. MONIRO-1 has low activity against L-type calcium channels. MONIRO-1 can be used for the study of pain and epilepsy.
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PD0176078
0 ImagesPD0176078 is a newly found N-type Calcium channel blocker.
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PAM-2
0 ImagesCat. No.: HY-180400CAS No.: 1426293-61-9PAM-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 CaV2.2 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.
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Cav 2.2/3.2 blocker 1
0 ImagesCat. No.: HY-147639CAS No.: 2987640-67-3Cav 2.2/3.2 blocker 1 (Compound 9e) is a neuronal calcium channel blocker with IC50 values of 78 μM and 80 μM against Cav2.2 and Cav3.2, respectively. Cav 2.2/3.2 blocker 1 can penetrate the CNS.
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COX-2/CaV2.2-IN-1
0 ImagesCat. No.: HY-181612COX-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.
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NNC 09-0026
0 ImagesCat. No.: HY-187014CAS No.: 141360-03-4NNC 09-0026 is a neuronal calcium channel inhibitor. NNC 09-0026 exhibits IC50 values of 10 μM and 13 μM against neuronal L-type voltage-gated calcium channels, and an IC50 value of 13 μM against rat neuronal N-type voltage-gated calcium channels, with higher selectivity for neuronal L-type channels over peripheral L-type channels. NNC 09-0026 inhibits voltage-dependent Ca2+ channel currents, blocks Ca2+ influx through neuronal L-type and N-type voltage-gated calcium channels, and reduces potassium-stimulated calcium uptake in rat cerebral cortex synaptosomes. NNC 09-0026 inhibits TTX-sensitive Na+ channel currents in rat cerebellar Purkinje neurons. NNC 09-0026 attenuates ischemia-induced neuronal death, infarct volume and neurological deficits in rat models of cerebral ischemia. NNC 09-0026 can be used for studies on global cerebral ischemia, focal ischemia and cerebral ischemia-related research.
