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| Cas No.: | 1820787-94-7 |
| Chemical Name: | Irak4-IN-1 |
| Synonyms: | IRAK4-IN-1;4-[(4-morpholin-4-ylcyclohexyl)amino]quinazoline-6-carbonitrile;BCP32795;BDBM50242697 |
| SMILES: | O1C([H])([H])C([H])([H])N(C([H])([H])C1([H])[H])C1([H])C([H])([H])C([H])([H])C([H])(C([H])([H])C1([H])[H])N([H])C1C2C([H])=C(C#N)C([H])=C([H])C=2N=C([H])N=1 |
| Formula: | C19H23N5O |
| M.Wt: | 337.4188 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | IRAK4-IN-1 is an interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor with an IC50 of 7 nM. |
| Target: | IC50: 7 nM (IRAK4)[1] |
| In Vivo: | Oral pharmacokinetic studies of IRAK4-IN-1 (Compound 23) show it to have high bioavailability of 73% and low plasma clearance(Clp=22 mL/min/kg) leading to a reasonable half-life of 1.3 h[1]. |
| In Vitro: | The in vitro metabolic stability profiles of IRAK4-IN-1 (Compound 23) is measured, with EC50 of 2300 nM for the rat whole blood (RWB) [1]. |
| Animal Administration: | Rats[1] In the TLR driven in vivo model, female Lewis rats are dosed with either vehicle or IRAK4-IN-1 (Compound 23; 3, 10, 30, and 100 mg/kg; p.o.) dosed at 1 h prior to stimulation with Resiquimod, R848 (5 mg/kg, IP). At 1.5 h post R848 stimulation, blood samples are obtained from the animals and cytokine levels are measured. |
| References: | [1]. Smith GF, et al. Identification of quinazoline based inhibitors of IRAK4 for the treatment of inflammation. Bioorg Med Chem Lett. 2017 Jun 15;27(12):2721-2726. |
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| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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