MedKoo Cat#: 555651 | Name: Mevidalen free base
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Mevidalen, also known as LY3154207, is a novel, potent, and subtype selective human D1 positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC50 = 3 nM). In contrast to orthosteric agonists, LY3154207 showed a distinct pharmacological profile without a bell-shaped dose-response relationship or tachyphylaxis in preclinical models. Identification of a crystalline form of free LY3154207 from the discovery lots was not successful. Instead, a novel cocrystal form with superior solubility was discovered and determined to be suitable for development. LY3154207 is now in clinical development as a potential first-in-class D1 PAM for Lewy body dementia.

Chemical Structure

Mevidalen free base
Mevidalen free base
CAS#1638667-79-4 (free base)

Theoretical Analysis

MedKoo Cat#: 555651

Name: Mevidalen free base

CAS#: 1638667-79-4 (free base)

Chemical Formula: C24H29Cl2NO3

Exact Mass: 449.1524

Molecular Weight: 450.40

Elemental Analysis: C, 64.00; H, 6.49; Cl, 15.74; N, 3.11; O, 10.66

Price and Availability

Size Price Availability Quantity
5mg USD 750.00 2 Weeks
10mg USD 1,350.00 2 Weeks
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Synonym
LY3154207; LY-3154207; LY 3154207; Mevidalen free base
IUPAC/Chemical Name
2‑(2,6-Dichlorophenyl)-1-((1S,3R)‑5-(3-hydroxy-3-methylbutyl)-3-(hydroxymethyl)-1-methyl-3,4-dihydroisoquinolin-2(1H)‑yl)ethan-1-one
InChi Key
XHCSBQBBGNQINS-DOTOQJQBSA-N
InChi Code
InChI=1S/C24H29Cl2NO3/c1-15-18-7-4-6-16(10-11-24(2,3)30)19(18)12-17(14-28)27(15)23(29)13-20-21(25)8-5-9-22(20)26/h4-9,15,17,28,30H,10-14H2,1-3H3/t15-,17+/m0/s1
SMILES Code
O=C(N1[C@@H](C)C2=C(C(CCC(C)(C)O)=CC=C2)C[C@@H]1CO)CC3=C(Cl)C=CC=C3Cl
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
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 450.40 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.

Recalculate based on batch purity %
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
1: McCarthy AP, Svensson KA, Shanks E, Brittain C, Eastwood BJ, Kielbasa W, Biglan KM, Wafford KA. The dopamine D1 receptor positive allosteric modulator mevidalen (LY3154207) enhances wakefulness in the humanized D1 mouse and in sleep deprived healthy volunteers. J Pharmacol Exp Ther. 2021 Dec 10:JPET- AR-2021-000719. doi: 10.1124/jpet.121.000719. Epub ahead of print. PMID: 34893551. 2: Wilbraham D, Biglan KM, Svensson KA, Tsai M, Pugh M, Ardayfio P, Kielbasa W. Safety, Tolerability, and Pharmacokinetics of Mevidalen (LY3154207), a Centrally Acting Dopamine D1 Receptor-Positive Allosteric Modulator, in Patients With Parkinson Disease. Clin Pharmacol Drug Dev. 2021 Oct 19. doi: 10.1002/cpdd.1039. Epub ahead of print. PMID: 34664427. 3: Sun C, Armstrong MJ. Treatment of Parkinson's Disease with Cognitive Impairment: Current Approaches and Future Directions. Behav Sci (Basel). 2021 Apr 17;11(4):54. doi: 10.3390/bs11040054. PMID: 33920698; PMCID: PMC8073727. 4: Wilbraham D, Biglan KM, Svensson KA, Tsai M, Kielbasa W. Safety, Tolerability, and Pharmacokinetics of Mevidalen (LY3154207), a Centrally Acting Dopamine D1 Receptor-Positive Allosteric Modulator (D1PAM), in Healthy Subjects. Clin Pharmacol Drug Dev. 2021 Apr;10(4):393-403. doi: 10.1002/cpdd.874. Epub 2020 Oct 7. PMID: 33029934; PMCID: PMC8048550. 5: Hao J, Beck JP, Schaus JM, Krushinski JH, Chen Q, Beadle CD, Vidal P, Reinhard MR, Dressman BA, Massey SM, Boulet SL, Cohen MP, Watson BM, Tupper D, Gardinier KM, Myers J, Johansson AM, Richardson J, Richards DS, Hembre EJ, Remick DM, Coates DA, Bhardwaj RM, Diseroad BA, Bender D, Stephenson G, Wolfangel CD, Diaz N, Getman BG, Wang XS, Heinz BA, Cramer JW, Zhou X, Maren DL, Falcone JF, Wright RA, Mitchell SN, Carter G, Yang CR, Bruns RF, Svensson KA. Synthesis and Pharmacological Characterization of 2-(2,6-Dichlorophenyl)-1-((1S,3R)-5-(3-hydroxy-3-methylbutyl)-3-(hydroxymethyl)-1-methyl-3,4-dih ydroisoquinolin-2(1H)-yl)ethan-1-one (LY3154207), a Potent, Subtype Selective, and Orally Available Positive Allosteric Modulator of the Human Dopamine D1 Receptor. J Med Chem. 2019 Oct 10;62(19):8711-8732. doi: 10.1021/acs.jmedchem.9b01234. Epub 2019 Sep 30. PMID: 31532644. 6: Svensson KA, Hao J, Bruns RF. Positive allosteric modulators of the dopamine D1 receptor: A new mechanism for the treatment of neuropsychiatric disorders. Adv Pharmacol. 2019;86:273-305. doi: 10.1016/bs.apha.2019.06.001. Epub 2019 Jul 13. PMID: 31378255.