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CAS No.: 1416324-85-0

CU-CPT22 Catalog No. CSN21096

Synonyms: CU-CPT22

Selective toll-like receptor 1/2 (TLR1/2) inhibitor (IC50 = 0.58 μM). Exhibits no activity at TLR2/TLR6, TLR3, TLR4 and TLR7 or a panel of 10 representative kinases. Inhibits the release of proinflammatory cytokines TNF-α and IL-1β.

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技术信息

生物活性

描述The protein complex of toll-like receptor 1 and 2 (TLR1/2) is a key regulator of cytokine responses to human cytomegalovirus, lymphocytic choriomeningitis virus, and herpes simplex virus 1. CU-CPT22 is a small-molecule inhibitor of the TLR1/2 complex with an IC50 value of 0.58 ± 0.09µM. CU-CPT22 competed with Pam₃CSK₄ for binding to TLR1/2 with a K_i value of 0.41±0.07µM. CU-CPT22 at a concentration of 0.5µM inhibited TLR1/2 signaling without affecting other TLRs. CU-CPT22 at 8µM inhibited ~60% of TNF-α and 95% of IL-1β in RAW 264.7 cells^[2]. In Otsuka-Long-Evans-Tokushima fatty rats, treatment with Cu-CPT22 significantly reduced the kidney injury molecule-1-positive area in the kidney 12 hours after myocardial infarction. Cu-CPT22-treated rats also showed significantly decreased mRNA expressions of TLR2, TLR4, MyD88, IL-1β, and CCL2 compared with vehicle-treated controls^[3].
参考文献

[1] Cheng K, Wang X, et al. Discovery of small-molecule inhibitors of the TLR1/TLR2 complex. Angew Chem Int Ed Engl. 2012;51(49):12246-9.
[2] Cheng K, Wang X, Zhang S, Yin H. Discovery of small-molecule inhibitors of the TLR1/TLR2 complex. Angew Chem Int Ed Engl. 2012 Dec 3;51(49):12246-9.
[3] Ohno K, Kuno A, Murase H, Muratsubaki S, Miki T, Tanno M, Yano T, Ishikawa S, Yamashita T, Miura T. Diabetes increases the susceptibility to acute kidney injury after myocardial infarction through augmented activation of renal Toll-like receptors in rats. Am J Physiol Heart Circ Physiol. 2017 Dec 1;313(6):H1130-H1142.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7596 mL
- 13.7981 mL
- 27.5961 mL
- 5 mM
- 0.5519 mL
- 2.7596 mL
- 5.5192 mL
- 10 mM
- 0.2760 mL
- 1.3798 mL
- 2.7596 mL

技术信息

CAS号

1416324-85-0

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H22O7

运输

蓝冰

分子量

362.37

别名

CU-CPT22

溶解度

DMSO	90.0 mg/mL (248.4 mM)
Water	insoluble
Ethanol	40.0 mg/mL (110.4 mM)

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