R1487

Name: R1487
Brand: TargetMol
SKU: T7667
Price: 1230 CNY
Availability: InStock
Rating: 5 (10 reviews)

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纯度: 99.77%

货号 T7667Cas号 449811-92-1

R1487 是一种口服生物可利用的高选择性 p38α 丝裂原活化蛋白激酶抑制剂。

R1487

一键复制产品信息

很棒

纯度: 99.77%

货号 T7667Cas号 449811-92-1

R1487 是一种口服生物可利用的高选择性 p38α 丝裂原活化蛋白激酶抑制剂。

规格	价格	库存
1 mg	¥ 1,230	现货
5 mg	¥ 2,980	现货
10 mg	¥ 4,110	现货
25 mg	¥ 6,130	现货
50 mg	¥ 7,910	现货
100 mg	¥ 11,800	现货

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COA HNMR LCMS 产品操作手册

产品介绍

R1487 AI Summary

R1487 exhibits a broad spectrum of bioactivities. It shows potent inhibitory effects on a variety of kinases and proteins, including p38alpha, P38beta, ADCK3, CSNK1epsilon, DDR1, GAK, JNK1, JNK2, JNK3, NLK, RSK2, and STK36, with Kd values ranging from 0.2 nM to 1000.0 nM. It also inhibits TNF-alpha-induced IL-6 and IL-1beta production and LPS-induced TNF-alpha and IL-6 production. The compound demonstrates analgesic activity in a rat model and has favorable pharmacokinetic properties such as a Tmax of 4.67 hr, Cmax of 4016.79 nM, a half-life of 22.5 hr, an AUC of 29400.0 ng.hr.mL-1, an oral bioavailability of 51.6%, and clearance of 3.05 mL.min-1.kg-1. While it binds extensively to plasma proteins in cynomolgus monkeys, it has low aqueous solubility and permeability in human Caco-2 cells. Additionally, R1487 reveals lower affinity for kinases such as CLK2, PLK3, CSNK1G2, PRKCZ, STK3 with Ki values exceeding 7943.28 nM, and for targets like CDC42BPA, AKT3, CDK5 with Ki values above 10000.0 nM. It shows moderate inhibitory activity against Plasmodium falciparum proliferation with potencies ranging from 9432.9 nM to 14950.2 nM. The compound has a LogD7.4 value of 2.76 and a solubility of 20400.0 nM at pH 7.4. Importantly, R1487 demonstrates potent antiviral activity, inhibiting the SARS-CoV-2 3CL-Pro protease by 92.81% at 20µM, and reducing SARS-CoV-2 induced cytotoxicity in VERO-6 cells at 10 µM with an inhibition rate of -0.09% after 48 hours. These attributes highlight its potential as an antiviral agent, particularly against SARS-CoV-2..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	R1487 is an orally bioavailable and highly selective p38α mitogen-activated protein kinase inhibitor.

化学信息

分子量	388.37
分子式	C₁₉H₁₈F₂N₄O₃
CAS No.	449811-92-1
Smiles	Cn1c2nc(NC3CCOCC3)ncc2cc(Oc2ccc(F)cc2F)c1=O
密度	1.425 g/cm3 (Predicted)

储存&溶解度

存储	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
溶解度信息	DMSO: Slightly soluble