[CAS NO. 1422252-46-7] BI-9627hydrochloride

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PRODUCTS SPECIFICATIONS [1422252-46-7]

Catalog

HY-18071A

Brand

MCE

CAS

1422252-46-7

DESCRIPTION [1422252-46-7]

Overview

MDL	-
Molecular Weight	392.80
Molecular Formula	C16H20ClF3N4O2
SMILES	NC(NC(C1=CC=C(C2CCN(C(C)=O)CC2)C(C(F)(F)F)=C1)=O)=N.Cl

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

Summary

BI-9627 hydrochloride is potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor, with IC50s of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. BI-9627 hydrochloride displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 hydrochloride shows low DDI (drug-drug interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury ^[1] .

IC50 & Target

IC50: 6 nM (NHE1 in intracellular pH recovery assay), 31 nM (NHE1 in human platelet swelling assay) ^[1]

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 254.58 mM ; Need ultrasonic)

H ₂ O : 4.17 mg/mL ( 10.62 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5458 mL	12.7291 mL	25.4583 mL
5 mM	0.5092 mL	2.5458 mL	5.0916 mL
10 mM	0.2546 mL	1.2729 mL	2.5458 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

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

Solubility: ≥ 2.5 mg/mL (6.36 mM); Clear solution
2.

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

Solubility: ≥ 2.5 mg/mL (6.36 mM); Clear solution
3.

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

Solubility: ≥ 2.5 mg/mL (6.36 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Huber JD, 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. 2