- Cat. No.
- A19551
DS88790512
DS88790512 is a potent, selective, and orally bioavailable TRPC6 inhibitor with an IC50 of 11 nM.
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Transient receptor potential (TRP) channel modulators act on cation channels that sense heat, cold and irritants. The mammalian family has six subfamilies, including vanilloid (TRPV), ankyrin (TRPA), canonical (TRPC) and melastatin (TRPM) channels. TRP channels respond to temperature, touch, osmotic changes and plant-derived compounds, so they are often described as cellular sensors. Cloning of the capsaicin receptor TRPV1 in 1997 identified it as a heat-activated ion channel in pain-sensing neurons. AMG517 and SB-705498 are TRPV1 antagonists, while A 967079 blocks TRPA1 and optovin activates TRPA1 when exposed to light. Pyr10 inhibits TRPC3, and Pico145 inhibits channels formed by TRPC1, TRPC4 and TRPC5. The spider toxin peptide GsMTx4, an inhibitor of mechanosensitive channels, is also listed under Piezo Channel.
DS88790512 is a potent, selective, and orally bioavailable TRPC6 inhibitor with an IC50 of 11 nM.
AMG9810 is a selective and competitive vanilloid receptor 1 (TRPV1) antagonist with IC50 values of 24.5 and 85.6 nM for human and rat TRPV1, repectively.
TRPA1 Antagonist 1 is a methylene phosphate prodrug which converts to its active parent drug, a TRPA1 antagonist with an IC50 of 8 nM.
TC-I 2014 (compound 5) is a potent and orally active Benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonist, with IC50 values of 0.8 nM, 3.0 nM and 4.4 nM for canine, human and rat channels respectively.
GSK3395879 is a selective and orally bioavailable transient receptor potential vanilloid-4 (TRPV4) antagonist with an IC50 of 1 nM for hTRPV4.
Pyr3 is a selective inhibitor of transient receptor potential canonical channel 3 (TRPC3), with an IC50 of 700 nM for TRPC3-mediated Ca2+ influx.
Synonyms: SC 0030
JYL 1421 is a TRPV1 receptor antagonist, with an IC50 of 8 nM.
HC-067047 is a potent and selective TRPV4 antagonist and reversibly inhibits currents through the human, rat, and mouse TRPV4 orthologs with IC50 values of 48 nM, 133 nM, and 17 nM, respectively.
RN-1747 is a selective transient receptor potential cation channel subfamily V member 4 (TRPV4) agonist, with EC50 values are 0.77 μM, 4.0 μM and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4 respectively. RN-1747 also antagonizes TRPM8, with an IC50 of 4 μM.
RN-1734 is selective antagonist of the TRPV4 channel, completely antagonizes 4αPDD-mediated activation of TRPV4 with comparable, low micromolar IC50s for all three species (hTRPV4: 2.3 μM, mTRPV4: 5.9 μM, rTRPV4: 3.2 μM).
BCTC is a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells.
GSK2798745 is a first-in-class, highly potent, selective, orally active transient receptor potential vanilloid 4 (TRPV4) ion channel blocker with IC50s of 1.8 and 1.6 nM for hTRPV4 and rTRPV4, respectively.
SAR7334 is a potent and specific TRPC6 inhibitor, inhibiting TRPC6 currents with IC50 of 7.9 nM.
SN 2 is a novel and potent activator of TRPML3 ion channel with EC50 of 1.8±0.13 μM.
D-3263 is an agonist of transient receptor potential melastatin member 8 (TRPM8) with potential antineoplastic activity.
Capsazepine is a synthetic analogue of the sensory neurone excitotoxin, and an antagonist of TRPV1 receptor with an IC50 of 562 nM.
Synonyms: L593754 hydrochloride; L 593754; MH 12-43 hydrochloride; MH-12-43
EIPA hydrochloride (L593754 hydrochloride) is a TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA also inhibits Na+/H+-exchanger (NHE) and macropinocytosis.
A-1165442 is a potent, competitive and orally available TRPV1 antagonist with an IC50 of 9 nM for human TRPV1.
Pyr6 is a selective inhibitor of TRPC3 with IC50 of 0.49 uM(Ca2+ influx inhibition in thapsigargin depleted native RBL-2H3 cells).
A-784168 is a potent and selective antagonist of Vanilloid receptor type 1 (TRPV1).
AC1903 is a specific and selective inhibitor of TRPC5 and has podocyte-protective properties.
M8-B is an antagonist of transient receptor potential melastatin 8 (TRPM8) that blocks activation by cold, icilin (Item No. 10137), or menthol in vitro (IC50s = 7.8, 26.9, and 64.3 nM, respectively).
LASSBio-1135 is a dual TRPV1 antagonist and TNF-alpha production inhibitor.
TC-I 2000 is a TRPM8 channel blocker that inhibits icilin-induced TRPM8 channel activation in rTRPM8-expressing CHO cells