| Hazard Information | Back Directory | [Biological Activity]
ML204 is a potent and selective inhibitor of TRPC4/TRPC5 channels with 20-fold selectivity over TRPC6, without affecting other TRP channels and voltage-gated sodium, potassium or Ca2+ channels. | [in vitro]
ML204 inhibits TRPC4β-mediated intracellular Ca 2+ rise with an IC 50 value of 0.96 μM (HEK293 cells) and exhibits 19-fold selectivity against muscarinic receptor-coupled TRPC6 channel activation.
It blocks TRPC4β activity induced through either G i/o stimulation by μ-opioid, 5HT 1A serotonin, and M 2 muscarinic receptors or G q/11 stimulation by the endogenous M 3 -like muscarinic receptors.
It blocks LPS-induced TRPC5 channel activity.
| [in vivo]
ML204 (1 mg/kg; sc; 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: | < td class="col2"> Subcutaneous injection, twice a day, for 5 days (prior to LPS injection) | Result: | < td class="col2"> Induces mortality associated with increased hypothermia in mice with LPS-induced systemic inflammatory response. | [target]
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| Company Name: |
ChemeGen 中國
|
| Tel: |
18818260767 |
| Website: |
https://www.chemegen.com |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
| Company Name: |
MedChemExpress
|
| Tel: |
021-58955995 |
| Website: |
www.medchemexpress.com |
|
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Tags:2070015-10-8
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