2-Amino-6-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-4-(4-piperidinyl)-3-pyridinecarbonitrile hydrochloride
2-Amino-6-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-4-(4-piperidinyl)-3-pyridinecarbonitrile hydrochloride Basic information
- Product Name:
- 2-Amino-6-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-4-(4-piperidinyl)-3-pyridinecarbonitrile hydrochloride
- Synonyms:
-
- 2-Amino-6-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-4-(4-piperidinyl)-3-pyridinecarbonitrile hydrochloride
- Bayer IKK-beta inhibitor
- IKK-2 inhibitor VIII
- IKK-beta inhibitor
- 3-Pyridinecarbonitrile, 2-aMino-6-[2-(cyclopropylMethoxy)-6-hydroxyphenyl]-4-(4-piperidinyl)-, hydrochloride (1:1)
- ACHP (Hydrochloride )
- 2-amino-6-[2-(cyclopropylmethoxy)-6-oxocyclohexa-2,4-dien-1-ylidene]-4-piperidin-4-yl-1H-pyridine-3-carbonitrile
- (6Z)-2-amino-6-[2-(cyclopropylmethoxy)-6-oxocyclohexa-2,4-dien-1-ylidene]-4-piperidin-4-yl-1H-pyridine-3-carbonitrile
- CAS:
- 406209-26-5
- MF:
- C21H25ClN4O2
- MW:
- 400.91
- Mol File:
- 406209-26-5.mol
2-Amino-6-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-4-(4-piperidinyl)-3-pyridinecarbonitrile hydrochloride Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- DMSO : 50 mg/mL (124.72 mM; Need ultrasonic)
- form
- Powder
- color
- Off-white to yellow
2-Amino-6-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-4-(4-piperidinyl)-3-pyridinecarbonitrile hydrochloride Usage And Synthesis
Uses
ACHP Hydrochloride (IKK-2 Inhibitor VIII) is a highly potent and selective IKK-β inhibitor with an IC50 of 8.5 nM.
in vivo
ACHP (Compound 4j) is orally bioavailable in mice and rats and demonstrates significant in vivo activity in anti-inflammatory models (arachidonic acid-induced mouse ear edema model). ACHP has reasonable aqueous solubility (0.12 mg/mL in pH 7.4 isotonic buffer) and excellent Caco-2 permeability (Papp 62.3×10-7 cm/s), and demonstrates orally bioavailability in mice (BA: 16%) and rats (BA: 60%). The favourable bioavailability of ACHP in rats is likely due to its low clearance (0.33 L/h/kg). In an acute inflammation model, ACHP exhibits oral efficacy at 1 mg/kg in a dose-dependent manner[1].
IC 50
IKK-β: 8.5 nM (IC50); IKK-α: 250 nM (IC50)
References
[1] Murata T, et al. Synthesis and structure-activity relationships of novel IKK-beta inhibitors. Part 3: Orally active anti-inflammatory agents. Bioorg Med Chem Lett. 2004 Aug 2;14(15):4019-22. DOI:10.1016/j.bmcl.2004.05.041
[2] Sanda T, et al. Induction of cell death in adult T-cell leukemia cells by a novel IkappaB kinase inhibitor. Leukemia. 2006 Apr;20(4):590-8. DOI:10.1038/sj.leu.2404129
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