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TRPC6-IN-3

Cat No.:V70129 Purity: ≥98%
TRPC6-IN-3 (compound 17) is an orally bioavailable transient receptor potential C6 ion channel (TRPC6) inhibitor.
TRPC6-IN-3
TRPC6-IN-3 Chemical Structure CAS No.: 2311863-36-0
Product category: TRP Channel
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
Other Sizes
Official Supplier of:
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Product Description
TRPC6-IN-3 (compound 17) is an orally bioavailable transient receptor potential C6 ion channel (TRPC6) inhibitor. TRPC6-IN-3 not only regulates intracellular calcium concentration but also modulates membrane potential by modulating cation fluxes including calcium and sodium ions. TRPC6-IN-3 may be utilized in respiratory system research.
Biological Activity I Assay Protocols (From Reference)
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].
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.
References

[1]. Inhibitors of TRPC6 for treating respiratory conditions. WO2021209510.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C22H22FN5O3
Molecular Weight
423.440187931061
Exact Mass
423.17
CAS #
2311863-36-0
PubChem CID
138674835
Appearance
White to off-white solid powder
LogP
2.1
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
8
Rotatable Bond Count
5
Heavy Atom Count
31
Complexity
584
Defined Atom Stereocenter Count
0
SMILES
C(N1CCC(C2=NN=C(N)C=C2)CC1)(C1=NC=C(OC2=CC=C(F)C=C2)C(OC)=C1)=O
InChi Key
JUALOUHZJJERQT-UHFFFAOYSA-N
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)
Chemical Name
[4-(6-aminopyridazin-3-yl)piperidin-1-yl]-[5-(4-fluorophenoxy)-4-methoxypyridin-2-yl]methanone
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO: 125 mg/mL (295.20 mM)
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.

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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.
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 corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Clinical Trial Information
Title:A Study to Find Out if BI 764198 Helps Adults and Adolescents With a Kidney Condition Called Focal Segmental Glomerulosclerosis (FSGS)
Status:Recruiting
updateDate:2026-04-29
Ctid:NCT07220083

Link: https://clinicaltrials.gov/ct2/show/NCT07220083

Conditions:Focal Segmental Glomerulosclerosis
Interventions:Placebo
Phase:Phase 3
Title:PODOMOUNT-Basket, a Study to Test Whether BI 764198 Helps Adults and Adolescents With Different Types of Kidney Disease
Status:Recruiting
updateDate:2026-04-28
Ctid:NCT07355296

Link: https://clinicaltrials.gov/ct2/show/NCT07355296

Conditions:Proteinuric Kidney Diseases
Interventions:Placebo matching BI 764198
Phase:Phase 2
Title:A Study in Healthy Men to Test How Itraconazole Influences the Amount of BI 764198 in the Blood
Status:Completed
updateDate:2026-04-15
Ctid:NCT07308652

Link: https://clinicaltrials.gov/ct2/show/NCT07308652

Conditions:Healthy
Interventions:Itraconazole
Phase:Phase 1
View More

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:Healthy
Interventions:BI 764198
Phase:Phase 1
Title:A Study to Test BI 764198 in People With a Type of Kidney Disease Called Focal Segmental Glomerulosclerosis
Status:Completed
updateDate:2026-01-12
Ctid:NCT05213624

Link: https://clinicaltrials.gov/ct2/show/NCT05213624

Conditions:Kidney Disease, Chronic
Interventions:Placebo
Phase:Phase 2
Title:ACTION ON COVID-19: A Study to Test Whether BI 764198 Helps Lung Health of People Hospitalised With COVID-19
Status:Terminated
updateDate:2022-04-11
Ctid:NCT04604184

Link: https://clinicaltrials.gov/ct2/show/NCT04604184

Conditions:COVID-19
Interventions:Placebo
Phase:Phase 2
Title:A Study in Healthy Men Tests How Different Doses of BI 764198 Are Taken up in the Body and How Well They Are Tolerated.
Status:Completed
updateDate:2021-11-08
Ctid:NCT03854552

Link: https://clinicaltrials.gov/ct2/show/NCT03854552

Conditions:Healthy
Interventions:Placebo
Phase:Phase 1
Title:A Study in Healthy Japanese Men to Test How Well Different Doses of BI 764198 Are Tolerated
Status:Completed
updateDate:2021-11-01
Ctid:NCT04665700

Link: https://clinicaltrials.gov/ct2/show/NCT04665700

Conditions:Healthy
Interventions:Placebo
Phase:Phase 1
Title:A Study in People With Normal Kidney Function and People With Reduced Kidney Function to Test How BI 764198 is Processed in the Body
Status:Completed
updateDate:2020-12-19
Ctid:NCT04176536

Link: https://clinicaltrials.gov/ct2/show/NCT04176536

Conditions:Healthy|Chronic Kidney Disease
Interventions:BI 764198
Phase:Phase 1
Title:A Study to Test How Well Healthy Men Tolerate Different Doses of BI 764198
Status:Completed
updateDate:2020-11-04
Ctid:NCT04102462

Link: https://clinicaltrials.gov/ct2/show/NCT04102462

Conditions:Healthy
Interventions:Matching placebo
Phase:Phase 1

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