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MedKoo Cat#: 464281 | Name: BI-749327
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

BI-749327 is a novel potent and selective orally bioavailable TRPC6 antagonist with 85- and 42-fold selectivity over the most closely related channels, TRPC3 and TRPC7.

Chemical Structure

BI-749327
BI-749327
CAS#2361241-23-6

Theoretical Analysis

MedKoo Cat#: 464281

Name: BI-749327

CAS#: 2361241-23-6

Chemical Formula: C23H21F3N4O2

Exact Mass: 442.1617

Molecular Weight: 442.44

Elemental Analysis: C, 62.44; H, 4.78; F, 12.88; N, 12.66; O, 7.23

Price and Availability

Size Price Availability Quantity
5mg USD 450.00 2 Weeks
25mg USD 1,250.00 2 Weeks
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Related CAS #
No Data
Synonym
BI-749327; BI749327; BI 749327;
IUPAC/Chemical Name
(4-(6-aminopyridazin-3-yl)piperidin-1-yl)(4-(4-(trifluoromethyl)phenoxy)phenyl)methanone
InChi Key
RGYMFGHHIDRCBN-UHFFFAOYSA-N
InChi Code
InChI=1S/C23H21F3N4O2/c24-23(25,26)17-3-7-19(8-4-17)32-18-5-1-16(2-6-18)22(31)30-13-11-15(12-14-30)20-9-10-21(27)29-28-20/h1-10,15H,11-14H2,(H2,27,29)
SMILES Code
NC1=NN=C(C=C1)C2CCN(CC2)C(C3=CC=C(C=C3)OC4=CC=C(C=C4)C(F)(F)F)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
BI-749327 is a TRPC6 antagonist with IC50s of 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6, respectively.
In vitro activity:
In vitro, BI 749327 suppressed NFAT activation in HEK293T cells expressing wild-type or gain-of-function TRPC6 mutants (P112Q, M132T, R175Q, R895C, and R895L) and blocked associated signaling and expression of prohypertrophic genes in isolated myocytes. Reference: Proc Natl Acad Sci U S A. 2019 May 14;116(20):10156-10161. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6525474/
In vivo activity:
To test the efficacy of BI 749327 against cardiac disease in vivo, C57BL/6J mice were subjected to transaortic constriction (TAC) surgery to induce pressure overload or to sham surgery. BI 749327 (30 mg/kg/day, yielding unbound trough plasma concentration ∼180 nM) improved left heart function, reduced volume/mass ratio, and blunted expression of profibrotic genes and interstitial fibrosis in mice subjected to sustained pressure overload. Additionally, BI 749327 dose dependently reduced renal fibrosis and associated gene expression in mice with unilateral ureteral obstruction. Reference: Proc Natl Acad Sci U S A. 2019 May 14;116(20):10156-10161. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6525474/
Solvent mg/mL mM comments
Solubility
DMSO 31.3 70.63
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 442.44 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Lin BL, Matera D, Doerner JF, Zheng N, Del Camino D, Mishra S, Bian H, Zeveleva S, Zhen X, Blair NT, Chong JA, Hessler DP, Bedja D, Zhu G, Muller GK, Ranek MJ, Pantages L, McFarland M, Netherton MR, Berry A, Wong D, Rast G, Qian HS, Weldon SM, Kuo JJ, Sauer A, Sarko C, Moran MM, Kass DA, Pullen SS. In vivo selective inhibition of TRPC6 by antagonist BI 749327 ameliorates fibrosis and dysfunction in cardiac and renal disease. Proc Natl Acad Sci U S A. 2019 May 14;116(20):10156-10161. doi: 10.1073/pnas.1815354116. Epub 2019 Apr 26. PMID: 31028142; PMCID: PMC6525474.
In vitro protocol:
1. Lin BL, Matera D, Doerner JF, Zheng N, Del Camino D, Mishra S, Bian H, Zeveleva S, Zhen X, Blair NT, Chong JA, Hessler DP, Bedja D, Zhu G, Muller GK, Ranek MJ, Pantages L, McFarland M, Netherton MR, Berry A, Wong D, Rast G, Qian HS, Weldon SM, Kuo JJ, Sauer A, Sarko C, Moran MM, Kass DA, Pullen SS. In vivo selective inhibition of TRPC6 by antagonist BI 749327 ameliorates fibrosis and dysfunction in cardiac and renal disease. Proc Natl Acad Sci U S A. 2019 May 14;116(20):10156-10161. doi: 10.1073/pnas.1815354116. Epub 2019 Apr 26. PMID: 31028142; PMCID: PMC6525474.
In vivo protocol:
1. Lin BL, Matera D, Doerner JF, Zheng N, Del Camino D, Mishra S, Bian H, Zeveleva S, Zhen X, Blair NT, Chong JA, Hessler DP, Bedja D, Zhu G, Muller GK, Ranek MJ, Pantages L, McFarland M, Netherton MR, Berry A, Wong D, Rast G, Qian HS, Weldon SM, Kuo JJ, Sauer A, Sarko C, Moran MM, Kass DA, Pullen SS. In vivo selective inhibition of TRPC6 by antagonist BI 749327 ameliorates fibrosis and dysfunction in cardiac and renal disease. Proc Natl Acad Sci U S A. 2019 May 14;116(20):10156-10161. doi: 10.1073/pnas.1815354116. Epub 2019 Apr 26. PMID: 31028142; PMCID: PMC6525474.