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Catalog No.
Product Name
Application
Product Information
Citations
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MDR1/BCRP Inhibitor
CP-100356 is a dual inhibitor of MDR1 (P-glycoprotein) and BCRP, exhibiting IC50 values of 0.5 µM and 1.5 µM, respectively, for the inhibition of MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport. Additionally, CP-100356 shows weak inhibition of the OATP1B1 transporter, with an IC50 of approximately 66 µM, while demonstrating minimal inhibition against MRP2 and major human P450 enzymes (IC50 > 15 µM). This compound is valuable for research applications targeting drug resistance mechanisms and transport protein interactions in pharmacology and toxicology studies. -
BCRP/ABCG2 Inhibitor
Butein tetramethyl ether is a selective inhibitor of the breast cancer resistance protein (BCRP/ABCG2) that demonstrates potent biological activity. It has been shown to inhibit BCRP in MCF-7 MX and MDCK cell lines, with IC50 values of 2.2 μM and 1.03 μM, respectively. This compound is a valuable tool for research investigating the mechanisms of cancer resistance and could provide insights into therapeutic strategies for overcoming drug resistance in cancer treatments. -
ABCG2 (BCRP) Inhibitor
UR-MB108 is a selective inhibitor of ABCG2 (BCRP) with an IC50 value of 79 nM. This compound demonstrates high potency in inhibiting the efflux activity of the ABCG2 transporter. UR-MB108's stability in blood plasma enhances its potential for various biological applications, including studies on drug absorption and resistance in cancer research. -
P-gp/BCRP Inhibitor
P-gp/BCRP-IN-1 is a potent inhibitor targeting P-glycoprotein (P-gp) and Breast Cancer Resistance Protein (BCRP). This compound is designed to reverse drug resistance by inhibiting the efflux activities of these pivotal transporters. P-gp/BCRP-IN-1 enhances the oral bioavailability of chemotherapeutic agents, such as Paclitaxel (PTX), making it a valuable tool in cancer research and therapeutic development. Its efficacy and oral activity suggest a promising utility in overcoming drug resistance in various cancer models. -
BCRP Inhibitor
BCRP-IN-2 is a potent inhibitor of Breast Cancer Resistance Protein (BCRP), demonstrating enhanced inhibitory activity upon ultraviolet light activation. This compound serves as an effective probe for investigating the interactions of quinazolinamine derivatives with BCRP, facilitating ATP hydrolysis of the transport protein. BCRP-IN-2 significantly increases the accumulation of mitoxantrone in H460/MX20 cells, which exhibit BCRP overexpression, making it valuable for studies on multidrug resistance mechanisms in cancer research. -
BCRP/ABCG2 Inhibitor
3,7,2',4'-Tetramethoxy-5-hydroxyflavone is a potent inhibitor of the breast cancer resistance protein (BCRP/ABCG2), exhibiting an IC50 value of 5.98 μM. This compound is significant for research into multidrug resistance mechanisms in breast cancer, providing insights into potential therapeutic strategies to overcome treatment resistance. Its ability to modulate BCRP activity makes it a valuable tool in cancer pharmacology studies. -
BCRP Inhibitor
BCRP-IN-1 is a potent inhibitor of breast cancer resistance protein (BCRP), exhibiting IC50 values of 2.92 μM in the Hoechst 33342 assay and 2.46 μM in the Pheophorbide A assay. This compound is valuable for research applications targeting multidrug resistance in cancer cells, facilitating the study of therapeutic efficacy and drug transport mechanisms. Its selective inhibition of BCRP makes it an essential tool for understanding resistance pathways in oncology. -
L-type Calcium Chanel Inhibitor
Diltiazem is an orally active L-type calcium channel blocker that exerts antihypertensive and antiarrhythmic effects. It is utilized in research related to cardiac arrhythmias, hypertension, and angina pectoris, making it valuable for studies focused on cardiovascular health. Its mechanism of action contributes to the modulation of calcium influx, which is critical in various cardiac and vascular functions. -
NMDA Receptor Inhibitor
Bupivacaine is an NMDA receptor inhibitor that modulates neuronal excitability by blocking sodium, L-calcium, and potassium channels. It exhibits potent inhibition of SCN5A channels, with an IC50 of 69.5 μM. This compound is primarily utilized in research focused on chronic pain mechanisms and therapeutic interventions. -
Calcium Channel Inhibitor
Tetracaine hydrochloride is a calcium channel inhibitor that effectively blocks the voltage-sensitive release of Ca2+ from the sarcoplasmic reticulum. This compound exhibits significant biological activity and is primarily utilized in topical applications within ophthalmology, as well as serving as an antipruritic agent. Its mechanism of action makes it valuable for research in pain relief and modulation of calcium signaling pathways. -
Ca2+-ATPase Inhibitor
IPrAuCl is a gold compound that functions as a selective inhibitor of sarcoplasmic reticulum Ca2+-ATPase, demonstrating an IC50 value of 16.3 µM. Its primary mechanism involves hindering calcium ion transport, making it a valuable tool for researching calcium homeostasis and muscle contraction dynamics. IPrAuCl may also be useful in studies investigating the role of Ca2+-ATPase in various cellular processes and diseases. -
NMDA Receptor Inhibitor
Bupivacaine-d9 is a deuterium-labeled analog of Bupivacaine, primarily targeting NMDA receptors. This compound exhibits inhibitory effects on sodium, L-calcium, and potassium channels, with a notable potency against SCN5A channels, characterized by an IC50 value of 69.5 μM. Bupivacaine-d9 is utilized in research related to chronic pain mechanisms and the modulation of excitatory neurotransmission, offering valuable insights into therapeutic applications in pain management. -
Calcium Channel Inhibitor
Lidoflazine is a potent inhibitor of calcium channels, specifically known for its high affinity blockade of the HERG potassium channel. This compound exhibits antianginal properties, making it relevant in studies related to cardiac function and arrhythmias. Notably, Lidoflazine is associated with a risk of QT interval prolongation and ventricular arrhythmia, which underscores its importance in pharmacological research aiming to understand cardiovascular safety profiles. -
Calcium Channel Inhibitor
Pranidipine is a potent, long-acting 1,4-dihydropyridine calcium channel inhibitor, specifically designed to modulate calcium influx in vascular smooth muscle cells. Its primary biological activity involves the reduction of blood pressure, making it an effective antihypertensive agent. This compound is widely used in cardiovascular research to investigate mechanisms underlying hypertension and to evaluate therapeutic strategies for managing elevated blood pressure. -
Calcium Influx Inhibitor
Carboxyamidotriazole Orotate is an orotate salt of Carboxyamidotriazole, a potent inhibitor of calcium influx. It acts primarily as a cytostatic agent targeting nonvoltage-operated calcium channels and disrupting calcium-mediated signaling pathways. This compound demonstrates notable anti-tumor, anti-inflammatory, and antiangiogenic properties, making it valuable in cancer research and the study of inflammatory diseases. -
Calcium Channel Inhibitor
Nothofagin is a dihydrochalcone that acts as a calcium channel inhibitor. By blocking calcium influx, it downregulates NF-κB translocation, providing a mechanism to modulate inflammatory responses. This compound exhibits antioxidant properties and has potential applications in research related to septic responses and vascular inflammation. -
SERCA Inhibitor
CAD204520 dihydrochloride is a selective SERCA inhibitor with an IC50 of 0.34 μM. This compound specifically targets mutated NOTCH1 proteins, demonstrating significant relevance in the study of T-cell acute lymphoblastic leukemia (T-ALL) and mantle cell lymphoma (MCL). It is a valuable tool for research investigating the therapeutic potential and mechanisms of these cancers. -
SERCA Inhibitor
CAD204520 is a selective inhibitor of the Sarcoplasmic Reticulum Calcium ATPase (SERCA), demonstrating an IC50 value of 0.34 μM. This compound specifically targets mutated NOTCH1 proteins more effectively than wild-type, making it a valuable tool for studying T-cell acute lymphoblastic leukemia (T-ALL) and mantle cell lymphoma (MCL). CAD204520 is suitable for research aimed at understanding the molecular mechanisms and therapeutic strategies in these malignancies. -
Calcium Channel Inhibitor
Heteroclitin D is a lignan derived from Kadsura medicinal plants, functioning primarily as a calcium channel inhibitor. It exhibits significant biological activity by inhibiting L-type calcium channels, which are critical in various physiological processes. This compound is suitable for research applications focusing on calcium signaling, neuroprotection, and studies related to oxidative stress and lipid peroxidation. -
Calcium Channel Inhibitor
Yangambin is a furofuran lignan that functions as a calcium channel inhibitor, targeting voltage-gated Ca2+ channels. This compound effectively reduces intracellular calcium levels in vascular smooth muscle cells, promoting peripheral vasodilation. Additionally, Yangambin demonstrates antiallergic activity by inhibiting β-hexosaminidase release with an IC50 of 33.8 μM and exhibits anti-inflammatory properties with an IC50 of 37.4 μM, making it valuable for research in vascular biology and inflammation. -
Calcium Channel Inhibitor
PD0176078 is a selective N-type calcium channel inhibitor, primarily targeting voltage-gated calcium channels. It exhibits significant biological activity by effectively blocking calcium influx, which modulates neurotransmitter release and can influence pain signaling pathways. This compound is valuable for research applications focused on neuropharmacology and the investigation of pain mechanisms. -
Cav3.1/Cav3.2/Cav3.3 Inhibitor
ML218 hydrochloride is a selective inhibitor of T-type calcium channels, specifically Cav3.1, Cav3.2, and Cav3.3, exhibiting IC50 values of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. This compound effectively inhibits burst activity in subthalamic nucleus neurons and demonstrates minimal interference with L- or N-type calcium channels, KATP channels, or hERG potassium channels. Additionally, ML218 hydrochloride has the capability to penetrate the blood-brain barrier, making it a valuable tool for neurological research applications. -
Calcium Channel Inhibitor
Etripamil hydrochloride is a potent L-type calcium channel inhibitor primarily used in the research of paroxysmal supraventricular tachycardia (PSVT). By blocking calcium influx through slow calcium channels, it effectively slows down atrioventricular node conduction and extends the refractory period of the atrioventricular node. This compound is valuable for studying cardiac electrophysiology and the mechanisms underlying arrhythmias. -
CaVAb Inhibitor
UK-59811 hydrochloride is a Br-dihydropyridine derivative that functions as a potent inhibitor of the bacterial homotetrameric voltage-gated calcium channel, CaVAb, with an IC50 value of 194 nM. It serves as a valuable tool for studying calcium ion transport and its physiological implications in bacterial systems. Its specific action on CaVAb makes it suitable for research applications focused on calcium signaling and channel modulation. -
T-type Calcium Channel Inhibitor
IAA65 is a potent inhibitor of T-type calcium channels, exhibiting an IC50 value of 18.9 µM. This compound is primarily utilized in research related to epilepsy, aiding in the investigation of calcium channel modulation and its effects on neuronal excitability. IAA65 may facilitate the exploration of therapeutic strategies targeting T-type calcium channels for seizure management. -
T-type Calcium Channel Inhibitor
IAB15 is a potent inhibitor of T-type calcium channels, which play a crucial role in regulating neuronal excitability and neurotransmitter release. This compound demonstrates significant activity in modulating calcium ion influx, making it a valuable tool in epilepsy research. Its ability to selectively target these channels positions IAB15 as an important reagent for studying calcium signaling pathways and their implications in seizure disorders. -
Potassium/Sodium Channel Inhibitor
Huwentoxin I is a peptide toxin that specifically inhibits voltage-gated sodium channels and N-type calcium channels. This compound has demonstrated significant inhibitory effects on sodium channels in both rat hippocampus and cockroach dorsal unpaired median (DUM) neurons, with IC50 values of 66.1 nM and 4.80 nM, respectively. Huwentoxin I is valuable for studies focused on neuronal excitability and channelopathy-related research applications. -
Cav 3.2 Inhibitor
Cav 3.2 inhibitor 1 is a selective inhibitor of the Cav 3.2 T-type calcium channel, exhibiting minimal interaction with dopamine D2 receptors. This compound is valuable for studying mechanisms underlying somatic and visceral pain, making it a significant tool in pain research and potential therapeutic development. -
Cav 3.2 Inhibitor
Cav 3.2 Inhibitor 4 is a selective inhibitor targeting the Cav 3.2 T-type calcium channel, exhibiting an IC50 of 0.6 μM. This compound is primarily researched for its potential in investigating atrial fibrillation and related cardiac conditions. Its peripheral restriction enhances its utility in studying physiological processes influenced by Cav 3.2 activity in diverse experimental settings. -
Calcium Channel Inhibitor
Calcicludine is a potent inhibitor of high-voltage-activated calcium channels, with a particular affinity for L-type calcium channels. Derived from the venom of the green mamba, this protein toxin plays a critical role in studies investigating calcium signaling and neurotransmitter release. Its unique mechanism makes Calcicludine a valuable tool for researchers exploring neuronal excitability and muscle contraction pathways. -
Calcium Channel Blocker, Cholesterol Acyltransferase Inhibitor
Belfosdil functions as a selective calcium channel blocker while also inhibiting acyl coenzyme A cholesterol acyltransferase (ACAT). This dual action contributes to its role in modulating calcium influx and lipid metabolism. Belfosdil is utilized in research focused on cardiovascular and metabolic diseases, exploring its potential for therapeutic applications. -
Cavα2δ1/NET Inhibitor
Cavα2δ1&NET-IN-2 is a dual inhibitor targeting the α2δ-1 subunit of voltage-gated calcium channels and the norepinephrine transporter (NET). It demonstrates effective inhibition of Cavα2δ-1 with a Ki of 454 nM and exhibits potent inhibition of NET with a Ki of 59 nM and an IC50 of 7 nM. This compound is valuable for research focused on pain mechanisms and the associated neurotransmitter systems. -
NMDA Receptor Inhibitor
Bupivacaine hydrochloride monohydrate is an NMDA receptor inhibitor that effectively modulates excitatory neurotransmission. It possesses the ability to block sodium, L-calcium, and potassium channels, with a notable potency in inhibiting SCN5A channels, exhibiting an IC50 value of 69.5 μM. This compound is primarily utilized in research focused on chronic pain mechanisms and the development of analgesic strategies. -
Calcium Channel Inhibitor
Levosemotiadil is a calcium channel inhibitor that demonstrates increased binding affinity to human serum albumin (HSA) compared to its R-isomer. Research utilizing high-performance frontal analysis (HPFA) indicates that levosemotiadil binds approximately three times more strongly to HSA than semotiadil, with specific interactions at the diazepam binding site. The binding affinity of both enantiomers is diminished in the presence of diazepam, while warfarin shows no effect. These properties underscore levosemotiadil's potential as a Ca- and Na-channel blocker, making it a valuable compound for exploring its pharmacokinetics and therapeutic applications. -
Calcium Channels Inhibitor
ω-Grammotoxin SIA is a selective inhibitor of P/Q and N-type voltage-gated calcium channels, derived from spider venom. This protein toxin is instrumental in studying calcium's role in neuronal and cardiovascular signaling pathways. Its unique mechanism allows researchers to explore its potential applications in understanding and treating various neurological and cardiovascular diseases. -
α2δ-1 Inhibitor
(rel)-Mirogabalin is an inhibitor of the α2δ-1 subunit of voltage-dependent calcium channels. It is primarily used in research focused on neuropathic pain modulation and may also play a role in studying anxiety disorders. Its ability to regulate calcium influx makes it a significant compound for investigating therapeutic potentials in calcium-related pathophysiologies. -
Calcium Channel Inhibitor
(S)-Lercanidipine is a calcium channel blocker that exhibits antihypertensive and neuroprotective activities. It effectively reduces oxidative stress and has been shown to protect auditory sensory hair cells from noise-induced damage. In vitro studies demonstrate that (S)-Lercanidipine enhances cell viability, particularly at lower concentrations, and significantly lowers the hearing threshold in mice following noise exposure. Its antioxidant properties are characterized by an increase in the expression of antioxidant enzyme genes and a decrease in oxidative enzyme gene expression, suggesting its potential for mitigating noise-induced hearing loss and preserving outer hair cell viability. -
Cavα2δ1/NET Inhibitor
Cavα2δ1&NET-IN-1 is a dual inhibitor targeting the α2δ-1 subunit of voltage-gated calcium channels and the norepinephrine transporter (NET). This compound demonstrates inhibition of Cavα2δ-1 with a Ki value of 112 nM, and inhibits NET with a Ki of 383 nM and an IC50 of 67 nM. Cavα2δ1&NET-IN-1 is suitable for research applications focused on pain mechanisms and related therapeutic pathways. -
Calcium Channel Inhibitor
Cav 3.2 inhibitor 2 is a selective inhibitor of Cav3.2 T-type Ca2+ channels, exhibiting an IC50 of 0.09339 μM under a -80 mV holding potential. This compound effectively reduces T-channel-dependent somatic and visceral pain in murine models, making it a valuable tool for investigating intractable pain mechanisms. Its ability to modulate calcium channel activity positions Cav 3.2 inhibitor 2 as a significant agent in pain research and therapeutic development. -
Calcium Channel Inhibitor
Pincainide is a calcium channel inhibitor that specifically targets voltage-gated calcium channels in smooth muscle. It effectively reduces calcium influx, leading to the inhibition of norepinephrine- and high potassium-induced contractile responses. Pincainide is relevant in the study of cardiovascular diseases, providing insights into mechanisms related to smooth muscle function and regulation. -
Cavα2δ1/NET Inhibitor
Cavα2δ1&NET-IN-3 is a selective inhibitor targeting the α2δ subunit of voltage-gated calcium channels (VGCC) and the noradrenaline transporter (NET). This compound exhibits inhibitory constants (Kis) in the range of 100-500 nM for the human α2δ-1 subunit of the Cav2.2 calcium channel and for NET. Cavα2δ1&NET-IN-3 is utilized in research applications focused on pain modulation and neurotransmitter regulation, contributing to the understanding of various neurological disorders. -
Calcium Channel inhibitor
Calcium Channel Antagonist 4 is a potent inhibitor of voltage-gated calcium channels, exhibiting an IC50 value within the range of 5-20 μM. This compound's ability to selectively block calcium influx makes it a valuable tool for studying calcium signaling pathways in various cellular processes. It is particularly useful in research applications related to neurology, cardiology, and muscle physiology. -
FTO Inhibitor
Meclofenamic acid sodium hydrate is a selective inhibitor of fat mass and obesity-associated enzyme (FTO). Its primary action involves competing with FTO for binding to m(6)A-containing nucleic acids, thereby influencing RNA metabolism. Additionally, it exhibits non-selective gap-junction blocking activity and inhibits potassium channels hKv2.1 and hKv1.1, with IC50 values of 56.0 μM and 155.9 μM, respectively. This compound is valuable in research focused on obesity, metabolic regulation, and the role of RNA modifications in cellular processes. -
Aliostericeffect for Myosin ATPase 13 Inhibitor
Diazobenzenesulfonic acid, also known as 4-Sulfobenzenediazonium, functions as an allosteric inhibitor of myosin ATPase 13. This compound has significant biological activity by modulating the enzyme's function, thereby influencing muscle contraction mechanisms. It is primarily utilized in research applications aimed at understanding myosin-related pathways and exploring potential therapeutic targets for muscle-related diseases. -
Cardiac Myofibrillar ATPase Inhibitor
DN-F01 is a potent inhibitor of cardiac myofibrillar ATPase, exhibiting a strong calcium-dependent activity with an IC50 value of 11 ± 4 nmol/L. This compound serves as a valuable tool in studying cardiac muscle contractility and ATPase regulation. Its ability to selectively inhibit cardiac myofibrillar ATPase makes it suitable for research in cardiovascular physiology and related pathologies. -
Myosin ATPase Inhibitor
Myosin-IN-2 is a potent Myosin ATPase inhibitor, demonstrating an IC50 of 1.06 μM. This compound plays a critical role in research focused on heart diseases, particularly hypertrophic cardiomyopathy (HCM). By selectively inhibiting Myosin ATPase activity, Myosin-IN-2 provides valuable insights into the mechanisms underlying cardiac function and related pathological conditions. -
SERCA Inhibitor
CXL 017 is a selective inhibitor of the sarco/endoplasmic reticulum Ca2+-ATPase (SERCA), functioning by competing with ATP for binding and thereby inhibiting ATPase activity. This compound demonstrates notable cytotoxicity specifically against multidrug-resistant acute myeloid leukemia cells, such as HL60/MX2. CXL 017 is valuable in research related to multidrug-resistant acute myeloid leukemia and offers insights into potential therapeutic approaches for overcoming drug resistance in cancer. -
Calcium Channel Inhibitor
A-1048400 is a selective calcium channel inhibitor that demonstrates potent activity against N-type and T-type calcium channels, with IC50 values of 1.4 μM and 1.2 μM, respectively. By inhibiting neurotransmitter release and reducing membrane hyperexcitability, A-1048400 exhibits significant analgesic properties. This compound is particularly valuable for investigating mechanisms and treatments related to neuropathic pain, such as that resulting from spinal nerve ligation and chronic constriction injury. -
Cav3.2 Inhibitor
Cav 3.2 inhibitor 3 is a selective inhibitor of the Cav3.2 T-type calcium channel, exhibiting an IC50 of 0.1534 μM. This compound demonstrates minimal binding affinity for D2 receptors, making it a valuable tool for studying the role of Cav3.2 channels in various physiological processes. Its use is particularly relevant in research areas focused on neuronal excitability and pain modulation. -
Calcium Channel Inhibitor
TTA-P1 is a potent inhibitor of human T-type calcium channels, exhibiting state-independent characteristics. This compound is crucial for studying various physiological processes such as neuronal burst firing, hormone secretion, and cell proliferation. TTA-P1 is particularly valuable for research related to absence epilepsy and other neurological disorders linked to calcium signaling.
