WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 555816
CAS#: 2007975-22-4
Description: LMN75224 is a phosphodiesterase 1 inhibitors useful for treatment of neurological and psychiatric disorder. LMN75224 was reported in WO 2016147659. This product has no formal name at the moment. For the convenience of communication, a temporary code name was therefore proposed according to MedKoo Chemical Nomenclature (see web page: https://www.medkoo.com/page/naming).
MedKoo Cat#: 555816
Name: LMN75224
CAS#: 2007975-22-4
Chemical Formula: C19H25F3N4O3
Exact Mass: 414.1879
Molecular Weight: 414.4292
Elemental Analysis: C, 55.07; H, 6.08; F, 13.75; N, 13.52; O, 11.58
Synonym: LMN75224; LMN-75224; LMN 75224;
IUPAC/Chemical Name: 3-Methyl-7-(tetrahydro-2H-pyran-4-yl)-2-[[trans-4-(trifluoromethyl)cyclohexyl]methoxy]imidazo[5,1-f][1,2,4]triazin-4(3H)-one
InChi Key: LNELWUPBSLZUIQ-MQMHXKEQSA-N
InChi Code: InChI=1S/C19H25F3N4O3/c1-25-17(27)15-10-23-16(13-6-8-28-9-7-13)26(15)24-18(25)29-11-12-2-4-14(5-3-12)19(20,21)22/h10,12-14H,2-9,11H2,1H3/t12-,14-
SMILES Code: O=C1N(C)C(OC[C@H]2CC[C@H](C(F)(F)F)CC2)=NN3C1=CN=C3C4CCOCC4
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: 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 Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
| Biological target: | DSR-141562 is a novel, orally active, and selective brain-penetrant phosphodiesterase 1 (PDE1) inhibitor. |
| In vitro activity: | TBD |
| In vivo activity: | Oral administration of DSR-141562 at 10 mg/kg slightly elevated the cGMP concentration, and it potently enhanced the increase of cGMP induced by a dopamine D1 receptor agonist in mouse brains. DSR-141562 at 3-30 mg/kg potently inhibited methamphetamine-induced locomotor hyperactivity in rats, while it had only minimal effects on the spontaneous locomotor activity. Reference: J Pharmacol Exp Ther. 2019 Dec;371(3):692-702. https://pubmed.ncbi.nlm.nih.gov/31578257/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 25.0 | 60.32 |
The following data is based on the product molecular weight 414.4292 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. Enomoto T, Tatara A, Goda M, Nishizato Y, Nishigori K, Kitamura A, Kamada M, Taga S, Hashimoto T, Ikeda K, Fujii Y. A Novel Phosphodiesterase 1 Inhibitor DSR-141562 Exhibits Efficacies in Animal Models for Positive, Negative, and Cognitive Symptoms Associated with Schizophrenia. J Pharmacol Exp Ther. 2019 Dec;371(3):692-702. doi: 10.1124/jpet.119.260869. Epub 2019 Oct 2. PMID: 31578257. |
| In vitro protocol: | TBD |
| In vivo protocol: | 1. Enomoto T, Tatara A, Goda M, Nishizato Y, Nishigori K, Kitamura A, Kamada M, Taga S, Hashimoto T, Ikeda K, Fujii Y. A Novel Phosphodiesterase 1 Inhibitor DSR-141562 Exhibits Efficacies in Animal Models for Positive, Negative, and Cognitive Symptoms Associated with Schizophrenia. J Pharmacol Exp Ther. 2019 Dec;371(3):692-702. doi: 10.1124/jpet.119.260869. Epub 2019 Oct 2. PMID: 31578257. |
