ML218 free base · Synonyms: ML-218 · ML 218
ML218 is a potent, selective and orally active T-type Ca 2+ channels inhibitor.
For research use only. Not for human or veterinary use.
ML218 structure
CAS No.: 1346233-68-8
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 50 mg | USD 540.00 | BP-01213-50mg | In stock | Get quote |
| 100 mg | USD 850.00 | BP-01213-100mg | In stock | Get quote |
| 250 mg | USD 1,650.00 | BP-01213-250mg | In stock | Get quote |
| 500 mg | USD 2,650.00 | BP-01213-500mg | In stock | Get quote |
Need another size or custom synthesis? Request a quote.
Description
ML218 is a potent, selective and orally active T-type Ca 2+ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor with IC50s of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. ML218 inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 has no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. ML218 can penetrate the blood-brain barrier .
Biological activity
In Vitro In plasma protein binding studies (equilibrium dialysis), ML218 possesses good free fraction in both rat and human. Intrinsic clearance experiments in liver microsomes indicated that ML218 is highly cleared in rat (CLint = 115 mL/min/kg), but low to moderately cleared in human liver microsomes (CLint = 12.7 mL/min/kg). In Vivo ML218 (0.03-30 mg/kg; oral administration; once; male Sprague-Dawley rats) treatment reverses cataleptic behavior in rats induced by a 0.75 mg/kg dose of haloperidol. Free brain and plasma concentrations of ML218 increases in a dose proportional manner across the dose range (3 mg/kg: [plasma] = 98 nM, [brain] = 1.66 μM; 10 mg/kg: [plasma] = 282 nM, [brain] = 5.03 μM; 30 mg/kg: 1.2 μM, [brain] = 17.7 μM). Noncompartmental pharmacokinetic analysis indicates ML218 (1 mg/kg, IV) has a mean residence time (MRT) of nearly 7 h, a value which is consistent with its terminal half-life (t1/2 = 7 h).
Identifiers
- SMILES
-
O=C(NC[C@@H]1[C@@]2([H])CN(CCC(C)(C)C)C[C@@]12[H])C3=CC(Cl)=CC(Cl)=C3 - InChIKey
-
GSJIGYLGKSBYBC-OSYLJGHBSA-N
Specifications
- MW (average)
- 369.3290
- Formula
- C19H26Cl2N2O
- CAS No.
- 1346233-68-8
- Physical state
- Solid
- Color
- White to off-white
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder -20℃ 3 years, 4℃ 2 years; In solvent -20℃ 1 year;
Solubility
soluble in DMSO