An NHE1 inhibitor
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BI-9627

Item No. 27640

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(1-acetyl-4-piperidinyl)-N-(aminoiminomethyl)-3-(trifluoromethyl)-benzamide
CAS Number
1204329-34-9
Molecular Formula
C16H19F3N4O2
Formula Weight
356.3
Purity
≥95% (mixture of tautomers)
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 10mg/mLDMSO: 20mg/mLDMSO:PBS (pH 7.2) (1:7): 0.12mg/mL
λmax
244 nm
SMILES
CC(N(CC1)CCC1C2=CC=C(C(NC(N)=N)=O)C=C2C(F)(F)F)=O
InChi Code
InChI=1S/C16H19F3N4O2/c1-9(24)23-6-4-10(5-7-23)12-3-2-11(14(25)22-15(20)21)8-13(12)16(17,18)19/h2-3,8,10H,4-7H2,1H3,(H4,20,21,22,25)
InChi Key
QMHRLXNEGYTSRV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $128

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    10 mg

    $215

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    Product Description

    BI-9627 is an inhibitor of sodium-hydrogen exchanger isoform 1 (NHE1), with IC50 values of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively.1 It is greater than 30-fold selective for NHE1 over NHE2 and is inactive at NHE3 up to 16 μM in a pHi assay. BI-9627 inhibits phenylephrine-induced hypertrophy in neonatal rat cardiomyocytes.2 It increases recovery of left ventricular developed pressure and inhibits increases in left ventricular end-diastolic pressure (LVEDP) in a Langendorff isolated perfused rat heart model of ischemia-reperfusion injury when used at a concentration of 100 nM.1 BI-9627 (45 and 150 ppm in the diet) also attenuates decreases in left ventricular end-systolic pressure and increases in LVEDP in coronary artery-ligated rats.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Huber, J.D., Bentzien, J., Boyer, S.J., et al. Identification of a potent sodium hydrogen exchanger isoform 1 (NHE1) inhibitor with a suitable profile for chronic dosing and demonstrated cardioprotective effects in a preclinical model of myocardial infarction in the rat. J. Med. Chem. 55(16), 7114-7140 (2012).

    2. Kilić, A., Huang, C.X., Rajapurohitam, V., et al. Early and transient sodium-hydrogen exchanger isoform 1 inhibition attenuates subsequent cardiac hypertrophy and heart failure following coronary artery ligation. J. Pharmacol. Exp. Ther. 351(3), 492-499 (2014).