ML 204
ML 204 Basic information
- Product Name:
- ML 204
- Synonyms:
-
- ML204 hydrochloride,ML-204 hydrochloride
- 4-Methyl-2-(piperidin-1-yl)quinoline hydrochloride
- CAS:
- 2070015-10-8
- MF:
- C15H19ClN2
- MW:
- 262.78
- Mol File:
- 2070015-10-8.mol
ML 204 Chemical Properties
- storage temp.
- under inert gas (nitrogen or Argon) at 2-8°C
- form
- Solid
- color
- White to off-white
ML 204 Usage And Synthesis
Uses
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[1][2].
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
| TRPC4
| TRPC5
|