2. Membrane Transporter/Ion Channel
  3. CFTR
  4. I1421

I1421 is an activator of the cystic fibrosis transmembrane conductance regulator (CFTR) with an EC50 of 64 nM for WT CFTR currents. I1421 also allosterically activates multiple mutants causing cystic fibrosis (CF) with good in vivo potency, with an oral bioavailability of 60% in mice corresponding to a half-life of 75 min. I1421 synergizes with Elexacaftor (HY-111772) to enhance CFTR currents.

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I1421 Chemical Structure

I1421 Chemical Structure

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Based on 1 publication(s) in Google Scholar

I1421 Related Antibodies

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Description

I1421 is an activator of the cystic fibrosis transmembrane conductance regulator (CFTR) with an EC50 of 64 nM for WT CFTR currents. I1421 also allosterically activates multiple mutants causing cystic fibrosis (CF) with good in vivo potency, with an oral bioavailability of 60% in mice corresponding to a half-life of 75 min. I1421 synergizes with Elexacaftor (HY-111772) to enhance CFTR currents[1].

IC50 & Target

EC50: 64 nM (WT CFTR)[1]
In Vivo

I1421 (10 mg/kg; ip, po, sc; single dose) is rapidly absorbed in C57BL/6 mice. After three different administration routes, the maximum plasma concentrations (Cmax) observed 15 min after intraperitoneal and oral administration of 7.4 μM and 3.4 μM, respectively. The plasma level after intraperitoneal administration is higher than that after the other two administration routes[1].
I1421 (3 mg/kg; iv, po; single dose) has a bioavailability of 60% in mice after oral and intravenous injection, but the oral T1/2 is shorter (75 min)[1].

Pharmacokinetic Analysis in C57BL/6 Mice[1]

Route Dose (mg/kg) Tmax (h) Cmax (ng/mL) AUClast (ng·h/mL) T1/2 (h) CL (mL/min/kg) Vss (1/kg) F (%)
IP 10 0.25 2617 2145 2.16 - - -
PO 10 0.25 1181 1211 1.24 - - 60
SC 10 0.50 625 1512 1.36 - - -
IV 3 - 2354 610 1.78 81.51 2.49 -

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

343.35

Formula

C18H18FN3O3
SMILES

O=C(N1N=C(N)C2=C1C=C(CO)C=C2)[C@@H](C)COC3=CC=C(F)C=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Animal Administration

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
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I1421 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

I1421I 1421I-1421CFTRCystic fibrosis transmembrane conductance regulatorABC transporteranion channelinhibitorslarge-scale dockingligand discoverypotentiatorsInhibitorinhibitorinhibit

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