ChemicalBook > CAS DataBase List > BI-749327

BI-749327

Product Name
BI-749327
CAS No.
2361241-23-6
Chemical Name
BI-749327
Synonyms
BI-749327;BI-749327, 10 mM in DMSO;(4-(6-aminopyridazin-3-yl)piperidin-1-yl)(4-(4-(trifluoromethyl)phenoxy)phenyl)methanone;Methanone, [4-(6-amino-3-pyridazinyl)-1-piperidinyl][4-[4-(trifluoromethyl)phenoxy]phenyl]-;BI749327,Inhibitor,BI-749327,inhibit,Transient receptor potential channels,BI 749327,TRP Channel
CBNumber
CB95419686
Molecular Formula
C23H21F3N4O2
Formula Weight
442.43
MOL File
2361241-23-6.mol
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BI-749327 Property

Boiling point:
637.5±55.0 °C(Predicted)
Density 
1.334±0.06 g/cm3(Predicted)
storage temp. 
-20°C
solubility 
Soluble in DMSO (25 mg/ml)
pka
5.26±0.10(Predicted)
form 
solid
color 
White
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene
Product number
CS-0094062
Product name
BI-749327
Purity
99.53%
Packaging
5mg
Price
$350
Updated
2021/12/16
ChemScene
Product number
CS-0094062
Product name
BI-749327
Purity
99.53%
Packaging
10mg
Price
$550
Updated
2021/12/16
ChemScene
Product number
CS-0094062
Product name
BI-749327
Purity
99.53%
Packaging
50mg
Price
$1650
Updated
2021/12/16
ChemScene
Product number
CS-0094062
Product name
BI-749327
Purity
99.53%
Packaging
100mg
Price
$2650
Updated
2021/12/16
DC Chemicals
Product number
DC42750
Product name
BI-749327
Purity
>98%
Packaging
1g
Price
$2400
Updated
2021/12/16
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BI-749327 Chemical Properties,Usage,Production

Description

BI 749327 (2361241-23-6) is a potent (IC50 = 13 nM mouse TRPC6, 19 nM human TRPC6) and selective (85-fold over TRPC3, 42-fold over TRC7) orally available blocker of TRPC6.1 It suppressed interstitial fibrosis and associated molecular signaling in mouse heart and kidney disease models.? BI 749327 reversed established pulmonary hypertension by 50% via regression of pulmonary remodeling in a mouse model.2

Uses

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].

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

References

[1] BRIAN LEEI LIN. In vivo selective inhibition of TRPC6 by antagonist BI 749327 ameliorates fibrosis and dysfunction in cardiac and renal disease.[J]. ACS Catalysis , 2019: 10156-10161. DOI:10.1073/pnas.1815354116
[2] PRITESH P JAIN. TRPC6, a therapeutic target for pulmonary hypertension.[J]. ACS Applied Electronic Materials, 2021: L1161-L1182. DOI:10.1152/ajplung.00159.2021

BI-749327 Preparation Products And Raw materials

Raw materials

Preparation Products

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BI-749327 Suppliers

China 48 United States 7 Global 55
Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070 13913916777;
Fax
+86-25-83453306
Email
info@chemlin.com.cn
Country
China
ProdList
15778
Advantage
64
BOC Sciences
Tel
1-631-485-4226; 16314854226
Email
info@bocsci.com
Country
United States
ProdList
12952
Advantage
65
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4796
Advantage
55
Shanghai Beckham Medical Technology Co., Ltd
Tel
13816613772
Fax
QQ: 12922499
Email
huahero21@sina.com
Country
China
ProdList
2495
Advantage
55
Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Fax
021-65675885
Email
info@efebio.com
Country
China
ProdList
9803
Advantage
58
ShangHai Biochempartner Co.,Ltd
Tel
177-54423994 17754423994
Fax
QQ:2853530913
Email
2853530910@QQ.com
Country
China
ProdList
7999
Advantage
62
Shanghai Chaolan Chemical Technology Center
Tel
021-QQ：65489617 15618227136
Fax
21-5161 9052
Email
Sales@ATKchemical.com
Country
China
ProdList
9497
Advantage
58
Shanghai Yu Ben Biotechnology Co., Ltd.
Tel
021-61350663 15502154572
Fax
-
Email
1639466865@qq.com
Country
China
ProdList
499
Advantage
58
Fan De(Beijing) Biotechnology Co., Ltd.
Tel
15911056312
Email
liming@bio-fount.com
Country
China
ProdList
9729
Advantage
58
TargetMol Chemicals Inc.
Tel
+1-781-999-5354; +17819995354
Email
marketing@targetmol.com
Country
United States
ProdList
32470
Advantage
58

2361241-23-6, BI-749327Related Search:

METHOPRENE ACID Levetiracetam Pomalidomide Imiquimod

  • BI-749327
  • Methanone, [4-(6-amino-3-pyridazinyl)-1-piperidinyl][4-[4-(trifluoromethyl)phenoxy]phenyl]-
  • BI749327,Inhibitor,BI-749327,inhibit,Transient receptor potential channels,BI 749327,TRP Channel
  • (4-(6-aminopyridazin-3-yl)piperidin-1-yl)(4-(4-(trifluoromethyl)phenoxy)phenyl)methanone
  • BI-749327, 10 mM in DMSO
  • 2361241-23-6