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BI-749327

Cat. No. M14277
BI-749327 Structure
Size Price Availability
5mg USD 350  USD350 1-2 Weeks
10mg USD 550  USD550 1-2 Weeks
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 442.43
CAS Number 2361241-23-6
Solubility (25°C) DMSO 31.25 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] David C Hutchings, et al. Interaction of background Ca 2+ influx, sarcoplasmic reticulum threshold and heart failure in determining propensity for Ca 2+ waves in sheep heart

[2] Tong Lu, et al. TRPC6 N338S is a gain-of-function mutant identified in patient with doxorubicin-induced cardiotoxicity

[3] Zhihuang Zheng, et al. Role of TRPC6 in kidney damage after acute ischemic kidney injury

[4] Pritesh P Jain, et al. TRPC6, a therapeutic target for pulmonary hypertension

[5] Brian Leei Lin, et al. In vivo selective inhibition of TRPC6 by antagonist BI 749327 ameliorates fibrosis and dysfunction in cardiac and renal disease

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