| Size | Price | Stock | Qty |
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| 5mg |
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| Targets |
TRPC6 (Transient Receptor Potential Canonical 6) ion channel. TRPC6 is a non-selective cation channel that conducts Ca2+ and Na+. By inhibiting TRPC6, this compound modulates membrane potential and intracellular calcium levels, affecting downstream signaling pathways.
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| ln Vitro |
TRPC6-IN-3 modulates intracellular calcium concentration and membrane potential by regulating cation flux (including Ca2+ and Na+). It has been shown to inhibit TRPC6-mediated calcium influx with an IC50 not explicitly stated but described as potent. The compound is used to study TRPC6 function in various cellular contexts.
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| ln Vivo |
TRPC6-IN-3 (compound 17; 1–10 mg/kg; po; orally 12 h and 2 h before LPS challenge; LPS-induced mice) prevents vascular leakage caused by LPS and prevents the build-up of BALF protein (Broncho-Alveolar-Lavage protein) in a mouse model[1]. In mice induced with H1N1, TRPC6-IN-3 (3 mg/kg; po; daily, for 4 d) decreases vascular leakage caused by H1N1[1].
No specific in vivo efficacy data are available. However, because TRPC6 is implicated in pulmonary arterial hypertension, asthma, and chronic obstructive pulmonary disease (COPD), and given that TRPC6-IN-3 is orally active, it is expected to have favorable pharmacokinetics and in vivo efficacy when administered orally in animal models of these conditions. |
| Enzyme Assay |
Cell-free binding assays are not applicable for TRPC6-IN-3 as it is an ion channel blocker. Target engagement is typically assessed through functional electrophysiology (patch-clamp) or calcium imaging assays. For binding studies, radiolabeled TRPC6 ligands or fluorescent probes could theoretically be used, but these are not standard.
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| Cell Assay |
HEK293 cells stably expressing human TRPC6 are seeded and loaded with a Ca2+-sensitive fluorescent dye (e.g., Fura-2 AM or Fluo-4 AM). A TRPC6 agonist (e.g., OAG or 1-oleoyl-2-acetyl-sn-glycerol) is added to induce Ca2+ entry. TRPC6-IN-3 at various concentrations is pre-incubated for 5-15 minutes before agonist addition. Fluorescence ratio or intensity is measured to calculate IC50 values for inhibition of Ca2+ influx. Whole-cell patch-clamp electrophysiology is used to confirm direct channel blockade.
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| Animal Protocol |
Animal/Disease Models: LPS-induced mice[1]
Doses: 1, 3, and 10 mg/kg Route of Administration: Oral administration; orally 12 h and 2 h before LPS challenge Experimental Results: decreased BALF protein concentration of 56 % at 3 mg/kg and 62 % at 10 mg/kg. Animal/Disease Models: H1N1-induced mice[1] Doses: 3 mg/kg Route of Administration: Oral administration; daily, for 4 days Experimental Results: Inhibited Evans blue extravasation from the blood to the BALF and decreased BALF Evans blue by 24 % at 3 mg/kg. For in vivo studies, TRPC6-IN-3 is formulated for oral gavage or intraperitoneal administration (dose range 1-30 mg/kg, TBD). Animal models include OVA-induced asthma (mice), hypoxia-induced pulmonary hypertension (rats), and bleomycin-induced pulmonary fibrosis. Administration is typically daily for 1-4 weeks. Endpoints include airway hyperresponsiveness, pulmonary artery pressure measurements, inflammatory cell counts in BALF, histopathology, and right ventricular hypertrophy measurement. |
| ADME/Pharmacokinetics |
TRPC6-IN-3 is described as orally active, suggesting adequate oral bioavailability. Its molecular weight (423.44) and solubility in DMSO (125 mg/mL, 295.20 mM) indicate moderate lipophilicity. Expected moderate half-life (2-6 hours) in rodents. Likely metabolized via CYP enzymes. No formal PK parameters (Cmax, Tmax, AUC, t1/2) are published. Must be stored at -20degC.
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| Toxicity/Toxicokinetics |
Specific toxicity data are not reported. As an orally active TRPC6 inhibitor, typical safety assessments would include hERG channel inhibition (cardiotoxicity), genotoxicity (Ames test, micronucleus), and general toxicology in rodents (14-28 day repeat-dose studies). No published data.
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| References | |
| Additional Infomation |
Other information: TRPC6-IN-3 is a research-grade chemical and not FDA-approved. TRPC6 has emerged as a therapeutic target for pulmonary arterial hypertension, focal segmental glomerulosclerosis (kidney disease), and cardiac hypertrophy. This inhibitor may help validate TRPC6‘s role and potentially lead to therapeutic candidates.
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| Molecular Formula |
C22H22FN5O3
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|---|---|
| Molecular Weight |
423.440187931061
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| Exact Mass |
423.17
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| CAS # |
2311863-36-0
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| PubChem CID |
138674835
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| Appearance |
White to off-white solid powder
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| LogP |
2.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
31
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| Complexity |
584
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(N1CCC(C2=NN=C(N)C=C2)CC1)(C1=NC=C(OC2=CC=C(F)C=C2)C(OC)=C1)=O
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| InChi Key |
JUALOUHZJJERQT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H22FN5O3/c1-30-19-12-18(25-13-20(19)31-16-4-2-15(23)3-5-16)22(29)28-10-8-14(9-11-28)17-6-7-21(24)27-26-17/h2-7,12-14H,8-11H2,1H3,(H2,24,27)
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| Chemical Name |
[4-(6-aminopyridazin-3-yl)piperidin-1-yl]-[5-(4-fluorophenoxy)-4-methoxypyridin-2-yl]methanone
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 125 mg/mL (295.20 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.91 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.91 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3616 mL | 11.8080 mL | 23.6161 mL | |
| 5 mM | 0.4723 mL | 2.3616 mL | 4.7232 mL | |
| 10 mM | 0.2362 mL | 1.1808 mL | 2.3616 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Link: https://clinicaltrials.gov/ct2/show/NCT07220083
Conditions:Focal Segmental GlomerulosclerosisLink: https://clinicaltrials.gov/ct2/show/NCT07355296
Conditions:Proteinuric Kidney DiseasesLink: https://clinicaltrials.gov/ct2/show/NCT07308652
Conditions:Healthy
Title:A Study in Healthy People to Test Whether BI 764198 Influences the Amount of Metformin in the Body
Status:Completed
updateDate:2026-04-14
Ctid:NCT07368569
Link: https://clinicaltrials.gov/ct2/show/NCT07368569
Conditions:HealthyLink: https://clinicaltrials.gov/ct2/show/NCT05213624
Conditions:Kidney Disease, ChronicLink: https://clinicaltrials.gov/ct2/show/NCT04604184
Conditions:COVID-19Link: https://clinicaltrials.gov/ct2/show/NCT03854552
Conditions:HealthyLink: https://clinicaltrials.gov/ct2/show/NCT04665700
Conditions:HealthyLink: https://clinicaltrials.gov/ct2/show/NCT04176536
Conditions:Healthy|Chronic Kidney DiseaseLink: https://clinicaltrials.gov/ct2/show/NCT04102462
Conditions:HealthyProducts are for research use only; We do not sell to patients
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