trpc

TRPC6-IN-1 is an inhibitor of the Transient Receptor Potential Canonical 6 Channel (TRPC6) (EC50: 4.66 μM).

IA-Alkyne (Iodoacetamide-alkyne) is a TRP channel (TRPC) agonist. IA-Alkyne can be used to develop an isotopically tagged probe for quantitative cysteine-reactivity profiling. It also has the potential for the study of respiratory infection.

TRPC antagonist1 (compound 15g) is a potent TRP channel (TRPC) antagonist with IC50 values of 2.4 μM, 12.2 μM, 7.6 μM, 2.9 μM, and 3.4 μM for TRPC3, TRPC4, TRPC5, TRPC6, and TRPC7, respectively. It demonstrates significant anti-glioblastoma efficacy in vitro against the U87 cell line.

TRPC6-IN-2 is a TRPC protein inhibitor, specifically inhibiting TRPC6 protein.

TRPC5-IN-4, a potent and safe TRPC inhibitor, exhibits IC50 values of 14.07 nM and 65 nM for TRPC5 and TRPC4, respectively, indicating high efficacy. It does not cause damage to liver and kidney cellular components, making it suitable for chronic kidney disease (CKD) research [1].

TRPC5-IN-5 (Compound ph8) is a TRPC5 inhibitor with an IC50 value of 1.28 μM. It is applicable in research related to neurological and kidney diseases.

TRPC4/5-IN-3 (Compound 32) is an orally active inhibitor of transient receptor potential canonical channels 4 and 5 (TRPC4/5), with IC50 values of 3.6 nM and 5.5 nM, respectively. It inhibits the hERG channel with an IC50 of 6.5 µM. This compound demonstrates good metabolic stability in human, rat, and mouse liver microsomes. In mouse models, TRPC4/5-IN-3 exhibits antidepressant and anxiolytic effects and displays favorable pharmacokinetic properties, with an oral bioavailability of 87%.

TRPC6 antagonist-1 (X26) is a TRPC6 inhibitor with IC50 values of 0.97 μM for TRPC6, 3.93 μM for TRPC3, 5.77 μM for TRPC5, and 4.37 μM for TRPC7. Additionally, TRPC6 antagonist-1 hinders TGF-β1-induced myofibroblast differentiation, thereby mitigating renal fibrosis.

TRPC4/5-IN-2 (Compound 12) is an orally active transient receptor potential (TRPC5) inhibitor with an IC50 value of 81 nM. This compound exhibits good biosafety and low hepatic and renal toxicity, making it a promising candidate for the treatment of chronic kidney disease (CKD).

TRPC6-PAM-C20 is a selective TRPC6 positive allosteric modulator that induces a transient increase in intracellular Ca2+ with an EC50 of 2.37 μM in HEK cells expressing TRPC6 and enhances OAG-induced platelet aggregation.

TRPC5-IN-1 is a TRPC5 inhibitor active in various animal models of chronic kidney disease.

TRPC4/5-IN-1 can be used for the research of skin inflammatory diseases and proteinuric kidney diseases. TRPC4/5-IN-1 is a potent inhibitor of TRP channel 5/4 (TRPC5/4) with IC50 values of 0.54 μM and 2.06 μM, respectively. [1].

TRPC3/6-IN-1 is a highly potent and selective inhibitor that blocks the activity of canonical transient receptor channels TRPC3 and TRPC6, showing significant potency against human isoforms hTRPC3 and hTRPC6 with IC50 values of 1260 nM and 500 nM, respectively. This compound is valuable for research on chronic models of heart failure [1].

TRPC5-IN-3 is a potent TRPC5 inhibitor with an IC50 of 10.75 nM.

TRPC5-IN-2 is a potent inhibitor of TRPC5.

TRPC5 modulator-1 (Compound 9) is a TRPC5 modulator with an IC50 of less than 1 nM, suitable for studying neuropsychiatric disorders.

TRPC6-IN-3 (compound 17) is an orally active inhibitor of the transient receptor potential C6 ion channel (TRPC6), which regulates intracellular calcium concentration and modulates the flux of cations, including calcium and sodium ions, thereby affecting membrane potential.

TRPC3/6-IN-2 is a potent inhibitor of TRPC3 and TRPC6, with IC50 values of 16 nM and 29.8 nM, respectively [1].

Rosiglitazone (BRL49653) is a PPARγ agonist, TRPC5 activator, and TRPM3 inhibitor with oral activity. Rosiglitazone is also a hypoglycemic agent and a thiazolidinedione insulin sensitizer.

Mavatrep (JNJ-39439335) is a selective antagonist of TRPV1 with Ki of 6.5 nM and can be used for studies about inflammatory pain.

D-GsMTx4 TFA, a selective spider venom peptide, is a TRPC1/6 and Piezo2 inhibitor that inhibits cation-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families, blocks cation-selective stretch-activated channels (SACs), and attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglia reactivity. toxicity and microglia reactivity.D-GsMTx4 TFA prevented myocardial infarction in a mouse model of ischemia/reperfusion and can be used to characterize the role of excitatory MSCs in normal physiology and pathology.

Diphenyleneiodonium chloride (DPI)(DPI) is an irreversible inhibitor of iNOS and eNOS (IC50 values of 50 nM and 0.3 μM, respectively),and displays broad-spectrum bactericidal activity.

D-3263 hydrochloride (D3263 HCl salt) is enteric-coated, orally bioavailable transient receptor potential melatonin member 8 (TRPM8) agonist.

OMDM-6 is a dual agonist of TRPV1(EC50 = 75 nM) and CB1 (Ki = 3.2 μM). OMDM-6 inhibits anandamide cellular uptake with a Ki of 7.0 μM.