1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. TRP Channel
  3. BI-749327

BI-749327 

Cat. No.: HY-111925 Purity: 99.53%
Handling Instructions

BI-749327 is a potent, high selectivity and orally bioavailable TRPC6 antagonist, with IC50s of 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6, respectively. BI-749327 is 85-fold more selective for mouse TRPC6 than TRPC3 and 42-fold versus TRPC7.

For research use only. We do not sell to patients.

BI-749327 Chemical Structure

BI-749327 Chemical Structure

CAS No. : 2361241-23-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2650 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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Description

BI-749327 is a potent, high selectivity and orally bioavailable TRPC6 antagonist, with IC50s of 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6, respectively. BI-749327 is 85-fold more selective for mouse TRPC6 than TRPC3 and 42-fold versus TRPC7[1].

IC50 & Target

IC50: 13 nM (mouse TRPC6), 19 nM (human TRPC6), 15 nM (guinea pig TRPC6)[1]

In Vitro

BI-749327 suppresses NFAT activation in HEK293T cells expressing wild-type or gain-of-function TRPC6 mutants and blocks associated signaling and expression of prohypertrophic genes in isolated myocytes[1].

In Vivo

BI-749327 (30 mg/kg/day; i.g.) improves left heart function, reduces volume/mass ratio, and blunts expression of profibrotic genes and interstitial fibrosis in mice subjected to sustained pressure overload[1].
BI-749327 dose dependently reduces renal fibrosis and associated gene expression in mice with unilateral ureteral obstruction[1].
BI-749327 has long terminal half-life (t1/2 8.5-13.5 hours) for mice (3-30 mg/kg; p.o.)[1].

Animal Model: C57BL/6J mice[1]
Dosage: 30 mg/kg/day
Administration: Oral gavage
Result: Improved left heart function, reduced volume/mass ratio, and blunted expression of profibrotic genes and interstitial fibrosis in mice subjected to sustained pressure overload.
Animal Model: CD-1 mice[1]
Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg
Administration: Oral administration
Result: t1/2 8.5-13.5 hours
Molecular Weight

442.43

Formula

C₂₃H₂₁F₃N₄O₂

CAS No.

2361241-23-6

SMILES

NC1=NN=C(C2CCN(C(C3=CC=C(OC4=CC=C(C(F)(F)F)C=C4)C=C3)=O)CC2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 31.25 mg/mL (70.63 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2602 mL 11.3012 mL 22.6024 mL
5 mM 0.4520 mL 2.2602 mL 4.5205 mL
10 mM 0.2260 mL 1.1301 mL 2.2602 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  0.5% CMC-Na/saline water

    Solubility: 1 mg/mL (2.26 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.70 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.70 mM); Clear solution

  • 4.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.70 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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BI-749327
Cat. No.:
HY-111925
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