Other grades of this product :
| 7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-[(3S)-3-piperidinyl]-2H-pyrido[2,3-d][1,3]oxazin-2-one hydrochloride Basic information |
| Product Name: | 7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-[(3S)-3-piperidinyl]-2H-pyrido[2,3-d][1,3]oxazin-2-one hydrochloride | | Synonyms: | Bay 65-1942 (HCl salt);Bay 65-1942 HCl;Bay 65-1942 (hydrochloride);(S)-7-(2-(cyclopropylmethoxy)-6-hydroxyphenyl)-5-(piperidin-3-yl)-1H-pyrido[2,3-d][1,3]oxazin-2(4H)-one hydrochloride;7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-[(3S)-3-piperidinyl]-2H-pyrido[2,3-d][1,3]oxazin-2-one hydrochloride;KINK-1 hydrochloride;KINK-1 hydrochloride >=98% (HPLC);2H-Pyrido[2,3-d][1,3]oxazin-2-one,7-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-[(3S)-3-piperidinyl]-,Hydrochloride(1:1) | | CAS: | 600734-06-3 | | MF: | C22H25N3O4.ClH | | MW: | 431.917 | | EINECS: | | Product Categories: | | Mol File: | 600734-06-3.mol |
| 7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-[(3S)-3-piperidinyl]-2H-pyrido[2,3-d][1,3]oxazin-2-one hydrochloride Chemical Properties |
| storage temp. | -20°C | | form | powder | | color | white to beige | | optical activity | [α]/D -19 to -24°, c = 0.2 in DMF |
| 7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-[(3S)-3-piperidinyl]-2H-pyrido[2,3-d][1,3]oxazin-2-one hydrochloride Usage And Synthesis |
| Biochem/physiol Actions | KINK-1 (Kinase Inhibitor of NF-ΚB-1; Bay 65-1942; CmpdA; Compound A) is an ATP-competitive, IKKβ-selective IΚB kinase (IKK) inhibitor (Ki against ATP = 2 nM/IKKβ and 135 nM/IKKα) that potently inhibits IKKβ-catalyzed GST-IΚBα(1–54) phosphorylation (IC50 = 4 nM, 200 nM ATP) without affecting (IC50 >10μM) IKK3 or 27 other kinases, lipases, phosphatases, caspases, and MMPs. KINK-1 effectively inhibits NF-ΚB activation and cytokines production in various human and murine cultures (IC50 from 18 to 502 nM) and is efficacious against LPS-induced plasma TNF-α production in mice and rats in vivo (EC50 = 9.1 and 6.6 mg/kg p.o., repectively) with good pharmacokinetic profile and oral availability. KINK-1 is also shown to effectively inhibit OVA-induced lung inflammation in a rat model of asthma (ED50 <0.3 mg/kg p.o.) without adverse effects to the animals. |
| 7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-[(3S)-3-piperidinyl]-2H-pyrido[2,3-d][1,3]oxazin-2-one hydrochloride Preparation Products And Raw materials |
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![7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-[(3S)-3-piperidinyl]-2H-pyrido[2,3-d][1,3]oxazin-2-one hydrochloride](/img/600734-06-3.jpg "7-[2-(Cyclopropylmethoxy)-6-hydroxyphenyl]-1,4-dihydro-5-[(3S)-3-piperidinyl]-2H-pyrido[2,3-d][1,3]oxazin-2-one hydrochloride")
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