| 产品描述： | ML204 hydrochloride is a novel, potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca2+ channels |
| 靶点： |
TRPC4;TRPC5 |
| 体外研究： |
ML204 hydrochloride inhibits TRPC4β-mediated intracellular Ca2+ rise with an IC50 value of 0.96 μM (HEK293 cells) and exhibits 19-fold selectivity against muscarinic receptor-coupled TRPC6 channel activation. ML204 hydrochloride blocks TRPC4β activity induced through either Gi/o stimulation by μ-opioid, 5HT1A serotonin, and M2 muscarinic receptors or Gq/11 stimulation by the endogenous M3-like muscarinic receptors. ML204 hydrochloride blocks LPS-induced TRPC5 channel activity |
| 体内研究： |
ML204 hydrochloride (1 mg/kg; s.c.; twice a day; for 5 days) causes mortality associated with exacerbated hypothermia and decreases peritoneal leukocyte numbers and cytokines in LPS-injected mice. Animal Model: Nonfasted male C57BL/6 (2-3 months) Dosage: 1 mg/kg Administration: Subcutaneous injection, twice a day, for 5 days (prior to LPS injection) Result: Induces mortality associated with increased hypothermia in mice with LPS-induced systemic inflammatory response. |
| 参考文献： |
1. Miller M, et al. Identification of ML204, a novel potent antagonist that selectively modulates native TRPC4/C5 ion channels. J Biol Chem. 2011 Sep 23;286(38):33436-46. 2. Miller MR, et al. Novel Chemical Inhibitor of TRPC4 Channels. Probe Reports from the NIH Molecular Libraries Program. 3. Thomas Schaldecker, et al. Inhibition of the TRPC5 ion channel protects the kidney filter. J Clin Invest. 2013 Dec 2; 123(12): 5298–5309. 4. Domingos M S Pereira, et al. Transient Receptor Potential Canonical Channels 4 and 5 Mediate Escherichia coli-Derived Thioredoxin Effects in Lipopolysaccharide-Injected Mice. Oxid Med Cell Longev. 2018 Jun 10;2018:4904696. |
| 溶解性： |
Soluble in H2O |
| 保存条件： |
-20°C |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.805 ml |
19.027 ml |
38.055 ml |
| 5 mM |
0.761 ml |
3.805 ml |
7.611 ml |
| 10 mM |
0.381 ml |
1.903 ml |
3.805 ml |
| 50 mM |
0.076 ml |
0.381 ml |
0.761 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京