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TrkA inhibitor compound 23（TrkA-IN-23）

产品编号: DC20280 Featured
TrkA inhibitor compound 23（TrkA-IN-23）
结构式
1821484-84-7
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中国地区超过5000个高品质化合物库存
应用领域
TrkA-IN-23是一种高效，亚型选择性，外周限制性变构TrkA抑制剂，IC50为10 nM，选择性比TrkB高180倍，选择性比TrkC高70倍；在基于细胞的检测中表现出精致的TrkA选择性在392种生化激酶测定中，>95%抑制TrkA和<15%抑制；对未活化的TrkA构建体也表现出18倍的选择性（TrkA非活化酶IC50=4nM，TrkA活化酶IC50=74nM）；抑制天然成年大鼠DRG中NGF诱导的磷酸化ERK形成，IC50为57nM，在麻醉大鼠体内消除对NGF致敏皮肤施用辣椒素的敏感性；证明了U
化学性质生物活性化合物的使用COA & MSDS相关产品产品说明书
Cas No.: 1821484-84-7
名称: 5-(2,4-dichloro-5-(pyridin-2-yl)benzamido)-N-(2-hydroxy-2-methylpropyl)-1-phenyl-1Hpyrazole-3-carboxamide
别名:
SMILES: C1=CC=CC(C2=C(Cl)C=C(Cl)C(C(=O)NC3N(C4=CC=CC=C4)N=C(C(=O)NCC(C)(C)O)C=3)=C2)=N1
分子式: C26H23Cl2N5O3
分子量: 524.402
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: Compound 23 was 180-fold selective over TrkB and 70-fold selective over TrkC in cell based assays (TrkB cell IC50 1.8μM, TrkC cell IC50 0.70μM).Compound 23 exhibited exquisite TrkA selectivity with >95% inhibition of TrkA and <15% inhibition of all other kinases observed.Compound 23 was shown to inhibit NGF induced phosphorylated ERK formation in native adult rat DRGs with an IC50 ~57nM and abolished sensitization to capsaicin administration to NGFsensitised skin as demonstrated by laser Doppler imaging in vivo in anaesthetised rat (see supporting information, rat non-activated enzyme IC50 6nM).Compound 23 was studied in the UVIH model of inflammatory pain in rats whereby its effect on thermal hyperalgesia resulting from UV burn was assessed by measuring paw withdrawal latency (Figure 11). Single oral doses of 23 (1.2, 12 and 40 mg/kg) were administered 48 hours after UV treatment and paw withdrawal latency determined at 1, 3 and 6 hours post dose. Hyperalgesia was found to be significantly reversed at doses of 23 of 12 and 40 mg/kg at each of the time-points studied (p<0.01, 2-way ANOVA vs. vehicle). The positive control ibuprofen (100 mg/kg, p.o.) also reversed thermal hyperalgesia at the 1 and 3 hour time-points. No effect was seen with any dose on thermal withdrawal response on the contralateral hindpaw (data not shown). Determination of unbound plasma concentrations of 23 in animals at 6 hours post dose showed that statistically significant efficacy was observed at unbound plasma concentrations equivalent to 0.4x (12 mg/kg) and 2.7x (40 mg/kg) TrkA cell IC50 (10nM).
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
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MSDS_1031_DC20280_1821484-84-7
COA
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