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α-Spinasterol
α-Spinasterol is a TRPV1 antagonist (IC50 = 1.4 μM), which reduces capsaicin-mediated Ca2+ influx in vitro; displays antinociceptive and antiedematogenic effects in multiple mouse models of pain. Learn MoreStarting at: $89.00
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NS 1643
NS 1643 is a human ether-a-go-go related gene (hERG) KV11.1 channel activator (EC50 = 10.5 μM), which exhibits different molecular mechanisms of action at KV11.1 (hERG1) and KV11.2 (hERG2) channels. Learn MoreStarting at: $90.00
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JW 67
JW 67 is an inhibitor of canonical Wnt pathway signaling (IC50 = 1.17 μM); targets the β-catenin destruction complex (GSK-3β/AXIN/APC) to induce β-catenin degradation. Learn MoreStarting at: $109.00
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NDT 9513727
NDT 9513727 is a potent C5a receptor (C5aR) competitive antagonist (IC50 = 11.6 nM); selective for human C5aR (IC50 values for rat and mouse C5aR are > 10 μM), which exhibits inverse agonist pharmacokinetics. Learn MoreStarting at: $189.00
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DPO-1
DPO-1 is a blocker of IKur ultrarapid delayed rectifier potassium current and KV1.5 channels (IC50 = 0.31 μM for rKV1.5), which displays selectivity for inhibition of IKur over Ito (8-fold), IK1, IKr and IKs (20-fold) in native myocytes and selectivity for rat recombinant KV1.5 over KV3.1 (~ 15-fold). Learn MoreStarting at: $105.00
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NS 5806
NS 5806 is a KV4.3 channel activator; mediates the transient outward K+ current (Ito), which increases IKv4.3 peak current amplitude in CHO-K1 cells expressing KV4.3 and KChIP2 (EC50 = 5.3 μM), and inhibits KV1.4-mediated currents independently of KChIP2. Learn MoreStarting at: $149.00
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SN-6
SN-6 is a selective Na+/Ca2+-exchange (NCX) inhibitor which displays some selectivity for NCX1. IC50 values are 2.9, 16 and 8.6 μM for inhibition of intracellular Na+-dependent 45Ca2+ uptake by cells expressing NCX1, NCX2 and NCX3 respectively. Learn MoreStarting at: $115.00
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SB 590885
SB 590885 is a potent B-Raf inhibitor (Kd = 0.3 nM), which is elective for B-Raf against 46 other kinases (Ki app values are 0.16 and 1.72 nM for B-Raf and c-Raf respectively), and decreases anchorage-independent growth of melanoma cell lines. It also inhibits ERK phosphorylation and proliferation in tumor cells expressing B-RafV600E. Learn MoreStarting at: $159.00
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HEMADO
HEMADO is an high affinity and selective adenosine A3 receptor agonist (Ki values are 1.1, 327, 1230 and > 30,000 nM for human A3, A1, A2A and A2B receptors respectively). Learn MoreStarting at: $139.00
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BVT 948
BVT 948 is a non-competitive, cell-permeable inhibitor of protein tyrosine phosphatases (PTPs) (IC50 = 0.09 - 1.7 μM); displays irreversible inhibition through catalysis of the hydrogen peroxide-dependent oxidation of PTP. Learn MoreStarting at: $95.00
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BRD 7389
BRD 7389 is a p90 ribosomal S6 kinase (RSK) inhibitor (IC50 values are 1.2, 1.5 and 2.4 μM for RSK3, RSK1 and RSK2 respectively), which upregulates insulin expression in terminally differentiated pancreatic α-cells. Learn MoreStarting at: $139.00
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MRS 2279
MRS 2279 is a selective, high affinity competitive antagonist of the P2Y1 receptor (Ki = 2.5 nM; IC50 = 51.6 nM). Learn MoreStarting at: $259.00
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2-ThioUTP tetrasodium salt
2-ThioUTP tetrasodium salt is a potent and selective P2Y2 agonist (EC50 values are 0.035, 0.35 and 1.5 μM for hP2Y2, hP2Y4 and hP2Y6 receptors respectively). Learn MoreStarting at: $269.00
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NS 6180
NS 6180 is a potent KCa3.1 channel blocker (IC50 values are 9, 14 and 15 nM for rat, human and mouse erythrocyte KCa3.1 channels respectively), which exhibits ~ 50% inhibition of KCa1.1, KV1.3, and KV11.1 channels, noradrenaline and dopamine transporters, L-type Ca2+ channels and melatonin receptors at a concentration of 10 μM. Learn MoreStarting at: $99.00
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LY 487379 hydrochloride
LY 487379 hydrochloride is a positive allosteric modulator selective for mGlu2 receptors, which potentiates glutamate-stimulated [35S]GTPγS binding (EC50 values are 1.7 and > 10 μM for mGlu2 and mGlu3 receptors respectively). Learn MoreStarting at: $110.00
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TCS 2510
TCS 2510 is a highly selective EP4 agonist (EC50 = 2.5 nM; Ki = 1.2 nM), which displays no significant binding at other prostaglandin receptors at concentrations up to 14 μM. Learn MoreStarting at: $139.00
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SSR 69071
SSR 69071 is a high affinity, potent inhibitor of human leukocyte elastase (HLE) (IC50 = 3.9 nM), which displays species-selectivity (Ki values are 0.017, 1.70, 3.01, 58 and > 100 nM for human, mouse, rat, rabbit and porcine elastase respectively) and inhibits HLE-induced lung hemorrhage in mice (ID50 = 2.8 mg/kg) and reduces infarct size in an in vivo acute model of coronary ischemia-reperfusion injury. Orally active. Learn MoreStarting at: $139.00
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NS 3623
NS 3623 is a human ether-a-go-go (hERG) KV11.1 potassium channel activator, which activates the IKr current and displays antiarrhythmic activity and exhibits potential dual mode of action at the hERG inhibitory site; may also act as a partial blocker of KV11.1 (hERG) channels. Learn MoreStarting at: $145.00
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6'-Iodoresiniferatoxin
6'-Iodoresiniferatoxin is a high affinity TRPV1 (VR1) vanilloid receptor partial agonist (Ki = 0.71 nM; EC50 = 130 nM at human VR1), which displays partial agonism at human VR1 and full agonism at rat VR1. Learn MoreStarting at: $159.00
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Spermidine trihydrochloride
Spermidine trihydrochloride binds to the polyamine modulatory site of the NMDA receptor and has been described as an agonist based on its ability to enhance the binding of [3H]-MK801. Learn MoreStarting at: $65.00
